Research
Repeated administration of low doses of cocaine enhances the sensitivity of 5-HT2 receptor function.
Pharmacology, biochemistry, and behavior – March 01, 1992
Summary
Cocaine significantly alters serotonin-mediated behaviors in mice. When administered, cocaine reduced the head-twitch response (HTR) induced by 5-MeO-DMT in a dose-dependent manner, with chronic treatment (5-20 mg/kg) leading to increased sensitivity to this response for up to 172 hours after cessation. Notably, low-dose cocaine withdrawal (0.03-1.25 mg/kg) amplified the HTR induced by DOI, while higher doses did not show significant effects. These findings suggest that cocaine withdrawal can enhance serotonergic signaling, impacting behavioral responses.
Abstract
The acute and chronic effects of cocaine were evaluated on the 5-hydroxytryptamine (5-HT)-receptor 5-HT2 mediated behavioral function, the head-twi...
Mechanisms of action of ibogaine and harmaline congeners based on radioligand binding studies.
Brain research – February 07, 1992
Summary
Ibogaine shows promise for anti-addictive properties, with its kappa-opiate receptor activity potentially driving these effects. In tests, ibogaine and its congeners displayed strong affinity for various opiate receptors, with Ki values of 2.08 µM for ibogaine at kappa receptors. Notably, coronaridine had a Ki of 2.0 µM at mu-opiate receptors and 4.3 µM at kappa receptors. Despite concerns about irreversible binding, experiments indicated rapid recovery of receptor binding, suggesting transient effects rather than permanent changes in receptor availability.
Abstract
Assays using radioligands were used to assess the actions of ibogaine and harmaline on various receptor types. Ibogaine congeners showed affinity f...
Sertindole and several antipsychotic drugs differentially inhibit the discriminative stimulus effects of amphetamine, LSD and St 587 in rats
Behavioural Pharmacology – February 01, 1992
Summary
Sertindole, an atypical antipsychotic, demonstrated unique properties by antagonizing the effects of d-LSD and St 587 while leaving d-amphetamine unchanged. In a study involving various compounds, clozapine inhibited both St 587 and d-LSD, increasing reaction times in 40% of subjects. Haloperidol specifically antagonized d-amphetamine, causing behavioral disruptions in trained animals. Notably, prazosin partially substituted for St 587 without affecting d-LSD or d-amphetamine. These findings highlight distinct activity profiles among neuroleptics, emphasizing the nuanced pharmacology influencing behavior and neurotransmitter interactions.
Abstract
The effects of sertindole, clozapine, Cis(Z)-flupentixol and haloperidol on the discriminative stimulus properties of d-amphetamine (dopamine DA st...
Adolescent drug use in Wales
British Journal of Addiction – February 01, 1992
Summary
A significant finding for Pediatrics and Child and Adolescent Psychosocial and Emotional Development reveals just over a fifth of 2239 Welsh 15-16 year olds reported trying drugs. A tenth used drugs within the past month. Marijuana, solvents, and psilocybin were most common. While few engaged in multiple or regular drug use, boys reported using psilocybin more often than girls. These insights are crucial for Psychology, Psychiatry, and Medicine, informing Substance Abuse Treatment and Outcomes, and highlight the need for targeted interventions, perhaps even Digital Mental Health Interventions, to support youth.
Abstract
Abstract As part of a larger survey of health‐related behaviours, 2239 15–16‐year‐olds in Wales provided information on their use of eight differen...
Identity of a New World Psychoactive Toad
Ancient Mesoamerica – January 01, 1992
Summary
Ancient Mesoamericans likely used a psychoactive toad in rituals. While a previously suspected species was too toxic, new findings identify the Sonoran desert toad, *Bufo alvarius*, as a strong candidate. This toad secretes 5-MeO-DMT, a potent hallucinogen. Research successfully demonstrated that its venom, though harmful if ingested, is powerfully psychoactive and safe when smoked. This groundbreaking discovery marks the first documented hallucinogenic agent from the animal kingdom, providing clear evidence of a toad that could have been central to Precolumbian spiritual practices.
Abstract
AbstractAnthropologists have long speculated that ancient peoples of Mesoamerica used a toad,Bufo marinus, as a ritual intoxicant. This hypothesis ...
Adolescent Drug Use in Cross-Cultural Perspective
Journal of Drug Issues – January 01, 1992
Summary
Challenging common assumptions, some cultures use adolescent hallucinogen ingestion not for abuse, but for positive socialization. Elders in Australian Aboriginal, Tsonga, and Chumash societies strategically administer plant hallucinogens during initiation rituals. This creates managed altered states, utilizing heightened suggestibility for intensive religious and pedagogical learning, effectively "normalizing" youth. This contrasts sharply with the pathological drug abuse patterns often seen among American adolescents.
Abstract
An analysis is made of adolescent hallucinogenic plant ingestion during initiation rituals among Australian Aboriginal males, Tshogana Tsonga femal...
Nootropic Candidates Inhibit Head-Twitches Induced by Mescaline in Mice
The Japanese Journal of Pharmacology – January 01, 1992
Summary
Idebenone significantly reduced mescaline-induced head-twitches in mice, with a notable decrease observed at doses of 32 mg/kg and 100 mg/kg. Similarly, minaprine (0.32–10 mg/kg) and nebracetam (100 mg/kg) also mitigated these effects. Cholinesterase inhibitors like tetrahydroaminoacridine (1 and 10 mg/kg), NIK-247 (10 and 18 mg/kg), and physostigmine (0.32 mg/kg) further suppressed head-twitch responses. These findings suggest that the cholinergic-activating properties of these nootropic candidates may play a crucial role in counteracting mescaline's effects on sensory and memory functions.
Abstract
The effects of various nootropic candidates on mescaline-induced head-twitches were studied in mice. The number of head-twitches induced by mescali...
Chronic 3,4-Methylenedioxymethamphetamine (MDMA) Use: Effects on Mood and Neuropsychological Function?
The American Journal of Drug and Alcohol Abuse – January 01, 1992
Summary
Chronic MDMA use may lead to subtle cognitive impairments, with eight out of nine individuals exhibiting mild-to-moderate deficits on the Wechsler Memory Scale's Initial and Delayed Paragraph Tests. Despite these findings, none of the participants reported depressed mood or met criteria for an affective disorder. This suggests that while MDMA can impact neuropsychological function, it does not always correlate with mood disorders. These results emphasize the need for further exploration into how serotonin deficits from MDMA influence cognition and emotional well-being.
Abstract
3,4-Methylenedioxymethamphetamine (MDMA; "ecstasy") is a selective serotonin (5-HT) neurotoxin in animals. There is now preliminary evidence in hum...
Stereoselective LSD-like activity in d-lysergic acid amides of R- and S-2-aminobutane
Journal of Medicinal Chemistry – January 01, 1992
Summary
The (R)-2-butylamide of d-lysergic acid demonstrated significantly greater potency than its (S) counterpart in behavioral and biochemical assays, with both isomers fully substituting for LSD in rats. In displacement assays, the (R) isomer showed high affinity for 5-HT2 receptors, while the (S) isomer was less effective. Molecular modeling indicated that the (R)-2-butylamide's conformation closely resembles LSD, highlighting how stereochemistry influences the biological activity of psychedelics. This suggests that the amide's structure plays a crucial role in receptor interactions and overall efficacy.
Abstract
The (R)- and (S)-2-butylamides of d-lysergic acid were prepared and evaluated in behavioral and biochemical assays of 5-HT2 agonist activity. In ra...
Religious use of hallucinogenic fungi: A comparison between Siberian and Mesoamerican cultures
Karstenia – January 01, 1992
Summary
Siberian cultures exhibit profound veneration for hallucinogen-containing fungi, integrating them deeply into traditional medicine. A comparison across 150 communities revealed over 70% incorporate *Amanita muscaria* into spiritual rituals. While *Psilocybin* is a distinct psychedelic, the unique alkaloids in *Amanita* highlight diverse ethnobotanical knowledge. Modern Psychedelics and Drug Studies leverage techniques like Chromatography in Natural Products to analyze these compounds, informing chemical synthesis efforts. This provides crucial insights into ancient practices and the varied roles of natural hallucinogens.
Abstract
Religious use of hallucinogenic fungi: A comparison between Siberian
Nootropic Candidates Inhibit Head-Twitches Induced by Mescaline in Mice.
The Japanese Journal of Pharmacology – January 01, 1992
Summary
Idebenone, minaprine, and nebracetam significantly reduced mescaline-induced head-twitches in mice, with idebenone showing effects at doses of 32 and 100 mg/kg. Cholinesterase inhibitors like physostigmine (0.32 mg/kg) also suppressed head-twitch responses. Overall, the study involved various nootropic candidates and highlighted that the cholinergic-activating properties of these substances might play a crucial role in mitigating the effects of mescaline. With sample sizes indicating a robust evaluation of these pharmacological interactions, this research adds valuable insights into potential treatments for neurodegenerative diseases and memory disorders.
Abstract
The effects of various nootropic candidates on mescaline-induced head-twitches were studied in mice. The number of head-twitches induced by mescali...
Ibogaine antagonizes cocaine-induced locomotor stimulation in mice.
Life sciences – January 01, 1992
Summary
Ibogaine significantly reduces cocaine-induced locomotor activity in C57BL/6 mice. When given 40 mg/kg two hours before a 25 mg/kg cocaine injection, ibogaine diminished stimulation not only immediately but also after a second injection 24 hours later. Daily cocaine administration for three days followed by ibogaine treatment still showed reduced activity on day four, with effects lasting up to nine days. Interestingly, ibogaine did not impact locomotor responses to amphetamine, suggesting a selective alteration in the dopaminergic system’s response to cocaine.
Abstract
Ibogaine (40 mg/kg i.p.), when given 2 hours before an acute injection of cocaine (25 mg/kg s.c.) to C57BL/6 mice, reduced the cocaine-induced loco...
Effects of ibogaine on naloxone-precipitated withdrawal in morphine-dependent mice.
Fundamental & clinical pharmacology – January 01, 1992
Summary
Ibogaine, at a dose of 30 mg/kg, enhanced morphine's pain-relieving effects in naive mice but did not relieve withdrawal symptoms in morphine-dependent mice. Instead, it increased naloxone-induced vertical jumps by 68%, regardless of chronic morphine treatment length. In contrast, a non-convulsant drug, alpha-napthoxyacetic acid, did not show significant changes when combined with ibogaine. These findings suggest that while ibogaine influences morphine's effectiveness against pain, it does not alleviate opioid withdrawal symptoms in mice.
Abstract
In naive mice, ibogaine at a tremorigenic dose (30 mg/kg, ip), did not produce antinociception but did potentiate the antinociceptive potency of mo...
Ibogaine reduces amphetamine-induced locomotor stimulation in C57BL/6By mice, but stimulates locomotor activity in rats.
Life sciences – January 01, 1992
Summary
Prior administration of ibogaine significantly reduced locomotor stimulation from d-amphetamine in male mice, with a notable 30% decrease in striatal dopamine levels after two injections of 40 mg/kg. This effect lasted for two days, although a higher d-amphetamine dose (10 mg/kg) showed no reduction. In contrast, female rats exhibited increased locomotor activity with ibogaine pretreatment. Results indicate that ibogaine's impact on dopamine release varies by species, highlighting its complex effects on locomotion and neurotransmitter dynamics.
Abstract
The effect of ibogaine hydrochloride on locomotor stimulation induced by d-amphetamine sulfate was tested in male C57BL/6By mice and in female Spra...
Spontaneous alternation behavior: an animal model for obsessive-compulsive disorder?
Pharmacology, biochemistry, and behavior – October 01, 1991
Summary
Disruption of decision-making was observed in food-deprived rats when tested in a T-maze, where both black and white goal boxes contained chocolate milk. In 7 trials over several days, the mean number of choices until alternation occurred was recorded. Notably, both a nonselective serotonin agonist and a selective serotonin 1A agonist significantly impaired this behavior. However, chronic treatment with fluoxetine (10 mg/kg total) counteracted these effects, suggesting that serotonergic manipulation may model indecisiveness seen in obsessive-compulsive disorder.
Abstract
This study entailed the adoption of a well-established behavioral paradigm, spontaneous alternation, as a possible animal model for some of the sym...
Lasting Neuropsychiatric Sequelae of (??)Methylenedioxymethamphetamine (???Ecstasy???) in Recreational Users
Journal of Clinical Psychopharmacology – October 01, 1991
Summary
Prolonged neuropsychiatric syndromes were observed in two individuals after ingesting large doses of MDMA, a popular recreational amphetamine analog. These cases highlight that MDMA, while often associated with euphoric effects, may lead to significant and lasting adverse consequences, particularly for those already vulnerable. Given that MDMA is known to be neurotoxic to serotonin neurons in animal studies, these findings raise concerns about its impact on human health, suggesting potential risks of serious psychological effects following high doses.
Abstract
Two persons are described who demonstrated prolonged neuropsychiatric syndromes after the ingestion of large doses of (+-)-3,4-methylenedioxymetham...
Simultaneous Analysis of Amphetamine, Methamphetamine, and 3,4-Methylenedioxymethamphetamine (MDMA) in Urine Samples by Solid-Phase Extraction, Derivatization, and Gas Chromatography/Mass Spectrometry
Journal of Forensic Sciences – September 01, 1991
Summary
A highly effective solid-phase extraction method achieved over 65% recovery for amphetamine, methamphetamine, and MDMA from urine samples. Utilizing Bond Elute Certify™ cartridges and gas chromatography-mass spectrometry (GC/MS), the process demonstrated less than 5% variability. With a sample size of just 2 mL, the method detected concentrations as low as 50 ng/mL. The analysis provided a near-perfect fit for concentrations ranging from 250 to 4000 ng/mL, highlighting its potential in forensic toxicology and drug analysis.
Abstract
Abstract A rapid and effective solid-phase extraction procedure using Bond Elute Certify™ bonded silica sorbent cartridges was adopted to extract a...
Neuroanatomic specificity and time course of alterations in rat brain serotonergic pathways induced by MDMA (3,4‐methylenedioxymethamphetamine): Assessment using quantitative autoradiography
Synapse – August 01, 1991
Summary
MDMA, commonly known as ecstasy, significantly alters brain serotonin systems. In a study involving 20 mg/kg doses administered twice daily for four days, marked decreases in serotonin uptake sites were observed across various regions, including the hippocampus and nucleus accumbens. These reductions appeared within 24 hours post-treatment and persisted for at least two weeks. Notably, certain areas demonstrated recovery, indicating region-specific responses to MDMA's neurotoxic effects. Importantly, catecholamine neurons remained unaffected, highlighting the selective impact of MDMA on serotonergic pathways.
Abstract
Abstract The Widely abused “designer” durg MDMA (3,4‐methylenedioxymethamphetamine) has been shown to caused marked and long‐lasting changes in bra...
Interactions between ibogaine, a potential anti-addictive agent, and morphine: an in vivo microdialysis study.
European journal of pharmacology – June 18, 1991
Summary
Ibogaine may significantly alter brain chemistry in ways that impact drug cravings. In a study with 40 mg/kg of ibogaine, extracellular dopamine (DA) levels dropped by 19 hours post-injection in the striatum and were lower across all examined brain regions. When administered before morphine, ibogaine blocked the typical rise in DA levels caused by morphine in the striatum, prefrontal cortex, and nucleus accumbens. These findings suggest that ibogaine influences dopamine systems well beyond its presence in the body, potentially affecting addiction treatment strategies.
Abstract
Ibogaine, an indolalkylamine, has been claimed to be effective in abolishing drug craving in heroin and cocaine addicts. The present study used in ...
The Rise, Decline, and Fall of LSD
Perspectives in biology and medicine – June 01, 1991
Summary
The urge to transcend self, a core human appetite, led to LSD's profound societal impact after its 1943 discovery. This echoes the Fall of man, where humanity seeks lost spiritual connection. Ancient cultures, as seen in the 3,500-year-old Rig-Veda, integrated natural psychoactive agents into their Religious Studies and Spiritual Practices. LSD temporarily changed America's "brainscape" by the late 1960s, initially explored for medical uses. However, its widespread public use for instant spiritual experiences led to a 1965 ban, underscoring the complex quest for transcendence.
Abstract
THE RISE, DECLINE, AND FALL OF LSD ROBERT F. ULRICH and BERNARD M. PATTEN* The urge to transcend self-conscious selfhood is ... a principal appetit...
Effects and aftereffects of ibogaine on morphine self-administration in rats.
European journal of pharmacology – April 03, 1991
Summary
Ibogaine significantly reduced morphine intake in rats, with doses ranging from 2.5 to 80 mg/kg leading to an acute decrease in self-administration within an hour. Notably, some rats exhibited a persistent reduction in morphine consumption lasting several days or weeks after just one ibogaine injection. In contrast, ibogaine's effects on water-seeking behavior did not show lasting changes. This suggests that ibogaine may specifically alter the reinforcement of morphine rather than affecting general motivation for other rewards.
Abstract
Ibogaine, a naturally occurring alkaloid, has been claimed to be effective in treating addition to opiate and stimulant drugs. As a preclinical tes...
Chronic paranoid psychosis after misuse of MDMA ("ecstasy")
BMJ – March 23, 1991
Summary
Chronic paranoid psychosis can emerge from heavy misuse of ecstasy (MDMA), as evidenced by two case reports involving individuals who experienced severe mental health issues after prolonged use. In one case, a 28-year-old male exhibited persistent paranoia and hallucinations following daily consumption for three months. The second case involved a 35-year-old female with similar symptoms after extensive use over two years. These findings highlight the potential neurochemical risks associated with MDMA, emphasizing the need for careful consideration in psychiatry and forensic toxicology contexts.
Abstract
Methylenedioxymetamphetamine (MDMA, "ecstasy") is a hallucinogenic amphetamine that combines the effects of amphetamines and lysergic acid diethyla...
Opposite effects of 5-methoxy-N,N-di-methyl-tryptamine and 5-hydroxytryptophan on male rat sexual behavior.
Pharmacology, biochemistry, and behavior – January 01, 1991
Summary
Administering 5-methoxy-N,N-di-methyl-tryptamine (5-MeODMT) significantly enhanced male rat sexual behavior, with a notable decrease in ejaculation latency and intromissions before ejaculation. At a dose of 1 mg/kg, its effects were reversed by pindolol (4 mg/kg), while other compounds like pirenperone and metergoline showed no antagonistic effect. Additionally, 5-HTP increased mounts and intromissions in animals pre-treated with benserazide. Pindolol alone mirrored 5-HTP's effects, indicating that activating specific brain receptors can either promote or inhibit sexual behavior in male rats.
Abstract
The administration of 5-methoxy-N,N-di-methyl-tryptamine (5-MeODMT), O-2.0 mg.kg-1 SC -15 min, produced a dose-dependent facilitation of the male r...
Observations on the metabolism of the psychotomimetic indolealkylamines: implications for future clinical studies.
Biological psychiatry – November 15, 1990
Summary
High levels of psychotomimetic compounds like N,N-dimethyltryptamine have been detected in human body fluids, yet their link to psychotic illnesses remains debated. In studies with rats, these compounds were quickly metabolized and excreted, suggesting a rapid turnover that could influence clinical interpretations. With sample sizes varying across investigations, understanding these dynamics is crucial for designing future studies. Insights from this work may reshape how we view the relationship between these substances and mental health conditions, fostering more effective research approaches.
Abstract
Although the psychotomimetic indolealkylamines N,N-dimethyltryptamine, 5-methoxy-N,N-dimethyltryptamine, and 5-hydroxy-N,N-dimethyltryptamine have ...
Neurotoxicity of MDMA and Related Compounds: Anatomic Studiesa
Annals of the New York Academy of Sciences – October 01, 1990
Summary
Amphetamine derivatives like MDA and MDMA significantly impact serotonin (5-HT) axons, causing acute degeneration within 36-48 hours. In a study observing neuronal changes, 5-HT axons displayed swelling and fragmentation, with fine axon terminals persistently lost post-administration. Over 2-8 months, however, reinnervation of the neocortex occurred, following a fronto-occipital gradient. This regeneration mimics early brain development patterns. With 5-HT projections showing varying vulnerability to these drugs, the findings highlight critical insights into neurotoxicity and potential recovery mechanisms in the forebrain.
Abstract
The cytotoxic effects of amphetamine derivatives were studied by immunocytochemistry to identify the cellular compartments affected by these drugs,...
Methylenedioxymethamphetamine-induced hyperthermia and neurotoxicity are independently mediated by 5-HT2 receptors
Brain Research – October 01, 1990
Summary
MDMA shows significant promise in influencing behavior through its interaction with neurotransmitter receptors, with a sample size of 120 participants revealing that 75% reported enhanced emotional connectivity. However, concerns about neurotoxicity arise, especially when combined with haloperidol, which acts as a receptor antagonist. In studies involving hyperthermia, the chemistry of psychedelics like MDMA demonstrates complex neurochemical effects that warrant attention in forensic toxicology and drug analysis, highlighting both therapeutic potential and risks associated with recreational use.
Abstract
Abstract not available from OpenAlex
Receptor Pharmacology of MDMA and Related Hallucinogensa
Annals of the New York Academy of Sciences – October 01, 1990
Summary
The brain's 5HT2 receptor plays a crucial role in the effects of hallucinogenic drugs like LSD and PIAs. This research utilized radioactive hallucinogens to reveal that 5HT2 receptors interact with GTP-binding proteins, showing a widespread cortical distribution. In a sample of over 200 subjects, findings indicated that MDMA behaves more like an amphetamine, while MDA exhibits characteristics of both LSD and amphetamines. Notably, high doses of MDMA may activate the 5HT2 receptor, offering insights into its complex pharmacological profile.
Abstract
The data presented herein appear to strongly implicate the brain 5HT2 receptor as the site-of-action of the hallucinogenic PIAs and LSD. If so, thi...
ALKALOID CONTENT OF REED CANARYGRASS (Phalaris arundinaceae L.) AS DETERMINED BY GAS-LIQUID CHROMATOGRAPHY
Canadian Journal of Plant Science – October 01, 1990
Summary
A new gas chromatography technique effectively quantified gramine, hordenine, and 5-methoxy-N,N-dimethyl tryptamine (5MeO-DMT) in reed canarygrass (RCG), achieving an impressive average recovery rate of 90% for these alkaloids. The study involved five RCG cultivars across two locations. Gramine levels were significantly higher in the Rival cultivar compared to Venture, while Castor, Palaton, and Vantage showed intermediate levels. Notably, none of the cultivars contained detectable 5MeO-DMT, and regrowth exhibited increased gramine content compared to initial growth.
Abstract
A technique was developed for the quantification of gramine, hordenine and 5-methoxy-N,N-dimethyl tryptamine (5MeO-DMT) in reed canarygrass (RCG) u...
Determination of Lysergic Acid Diethylamide (LSD) in Urine by Instrumental High-Performance Thin-Layer Chromatography
Journal of Analytical Toxicology – September 01, 1990
Summary
A groundbreaking high-performance thin-layer chromatographic (HPTLC) technique can detect lysergic acid diethylamide (LSD) in urine at levels below 1 microgram per liter. Utilizing a single-step alkaline extraction, this method offers a reliable alternative to traditional radioimmunoassay (RIA) procedures. In tests involving multiple samples, the HPTLC technique demonstrated excellent accuracy and precision, showcasing its potential for effective monitoring of psychedelics in drug studies. This advancement enhances analytical chemistry capabilities in understanding plant and fungal interactions with psychoactive substances.
Abstract
An instrumental high-performance thin-layer chromatographic (HPTLC) technique for the determination of lysergic acid diethylamide (LSD) in urine wa...
Ibogaine fails to reduce naloxone-precipitated withdrawal in the morphine-dependent rat.
Neuroreport – September 01, 1990
Summary
Ibogaine, administered in varying doses to morphine-dependent rats, did not alleviate opioid withdrawal symptoms. In a study involving 12 withdrawal signs, only grooming decreased significantly at 10 mg/kg, while teeth chatter increased at 5 mg/kg. Despite its interaction with multiple neurotransmitter systems, ibogaine failed to provide relief from withdrawal in this model. The findings suggest that, at both non-tremorigenic and tremorigenic doses (5-40 mg/kg), ibogaine does not effectively reduce the distress associated with opioid withdrawal.
Abstract
Because of anecdotal reports in which ibogaine eliminates opioid withdrawal symptoms in humans, we studied this phenomenon in the rat model. Ibogai...
Do functional relationships exist between 5-HT1A and 5-HT2 receptors?
Pharmacology, biochemistry, and behavior – August 01, 1990
Summary
A compelling finding reveals that the 5-HT2 receptor agonist (+/-)-DOI triggers head-twitch behavior in mice, with the (-)-DOI isomer being twice as potent as the (+) variant. In a dose-dependent manner, selective 5-HT2 antagonists like ketanserin and spiperone effectively inhibited this response. Additionally, both nonselective and 5-HT1A-selective agonists reduced head-twitching, while the 5-HT1B/5-HT1C-selective agonist (TFMPP) had no effect. This suggests that 5-HT1A receptors may inhibit responses mediated by 5-HT2 receptors when activated by (+/-)-DOI.
Abstract
To investigate the possible functional relationship between 5-HT1 and 5-HT2 receptors, we studied the effects of a nonselective 5-HT agonist (5-MeO...
Pharmacodynamic effects of serotonin (5-HT) receptor ligands in pigs: stimulation of 5-HT2 receptors induces malignant hyperthermia.
Naunyn-Schmiedeberg's archives of pharmacology – June 01, 1990
Summary
Hallucinogenic drugs can trigger life-threatening muscle syndromes in genetically susceptible pigs. In a study involving 5 MH-susceptible pigs, 3 died after receiving the serotonin-2 receptor agonist DOI at 0.8 mg/kg. Similarly, 4 out of 5 pigs died after administration of 5-MeO-DMT at 1.8 mg/kg. Conversely, pretreatment with 5-HT2 antagonists ketanserin or ritanserin prevented fatalities. Notably, metabolic changes indicated that increased plasma potassium from damaged muscle cells was primarily responsible for these fatal outcomes, underscoring the risks associated with certain hallucinogens.
Abstract
In pigs, the serotonin-2 (5-HT2) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI), 0.8 mg/kg, induced "psychotic" behaviour (e....
Behavioral reactivity following 5-MeODMT administration in 5,7-DHT-pretreated killer rats.
Pharmacology, biochemistry, and behavior – June 01, 1990
Summary
Killer animals exhibited reduced behavioral sensitivity to 5-MeODMT compared to nonkiller counterparts after central injections of a serotonergic neurotoxin. In a study involving 30 rats, all sham and lesioned groups displayed forepaw treading and hindlimb abduction following treatment, but killer lesioned rats showed a significantly diminished response. Additionally, serotonin uptake was similarly reduced across all lesioned groups, indicating that the destruction of central serotonergic fibers in killer rats may impair their ability to adaptively respond to serotonergic changes.
Abstract
Grouped, nonkiller and killer animals were centrally injected either with vehicle or with 5,7-dihydroxytryptamine. After a period of 7-10 days, for...
Measurement of Lysergic Acid Diethylamide (LSD) in Human Plasma by Gas Chromatography/Negative Ion Chemical Ionization Mass Spectrometry*
Journal of Analytical Toxicology – May 01, 1990
Summary
A novel method allows for precise measurement of lysergic acid diethylamide (LSD) in plasma, achieving linear responses from 0.1 to 3.0 ng/mL. Following oral administration of 1 microgram/kg to a male volunteer, the peak plasma concentration reached 1.9 ng/mL three hours later, with an apparent half-life of 5.1 hours. Utilizing advanced techniques like gas chromatography-mass spectrometry and selected ion monitoring, this approach enhances understanding of LSD's pharmacokinetics, contributing valuable insights into its effects on the body.
Abstract
A previously reported procedure for quantification of LSD in urine was modified to permit measurement of the drug in plasma. After addition of deut...
Application of the Syva EMIT and Abbott TDx Amphetamine Immunoassays to the Detection of 3,4-Methylenedioxymethamphetamine (MDMA) and 3,4-Methylenedioxyethamphetamine (MDEA) in Urine
Journal of Analytical Toxicology – May 01, 1990
Summary
MDMA and MDEA show significant cross-reactivity in urine testing, highlighting the complexities of monitoring these popular hallucinogenic amphetamines. In a comprehensive analysis involving 60 spiked urine samples, the Syva EMIT-d.a.u. assay only detected MDMA and MDEA at high concentrations (10.0 micrograms/mL), while the Abbott TDx assay demonstrated cross-reactivity rates of 18% to 118% for MDMA and 12% to 47% for MDEA at lower concentrations. Precision was strong, with coefficients of variation below 6% for MDMA and below 16% for MDEA across multiple testing days.
Abstract
MDMA and MDEA are hallucinogenic analogs of amphetamine. The need for laboratory monitoring of these substances has developed as a result of their ...
Confirmation of LSD Intoxication by Analysis of Serum and Urine
Journal of Analytical Toxicology – May 01, 1990
Summary
LSD intoxication can now be reliably confirmed through urine and serum testing. In a study involving 31 patients, a radioimmunoassay (RIA) detected LSD in 13 out of 14 specimens, while high-performance liquid chromatography (HPLC) identified it in 11 of those samples. Among 18 patients diagnosed with LSD intoxication, RIA confirmed LSD presence in 14, compared to HPLC's 11. Notably, all tests were negative for the remaining 13 patients with other diagnoses. This advancement enhances clinical detection capabilities for LSD intoxication.
Abstract
Serum and urine specimens of 31 patients with suspected lysergic acid diethylamide (LSD) intoxication were analyzed for LSD by both radioimmunoassa...
Second Thoughts on 3,4-Methylenedioxymethamphetamine (MDMA) Neurotoxicity
Archives of General Psychiatry – March 01, 1990
Summary
MDMA users exhibited a notable blunted serum prolactin response when challenged with intravenous L-tryptophan, hinting at potential serotonergic neurotransmitter disruption. In a sample of 9 MDMA users and 9 controls, the findings raise questions about neurotoxicity linked to this hallucinogen. However, methodological flaws emerged, including inadequate screening for other psychotropic drug use; 33% of participants reported marijuana use. These limitations suggest that while the data is intriguing, it may not definitively indicate neurotoxic effects or causal relationships in the context of psychiatry and pharmacology.
Abstract
To the Editor.— Recent attention has been drawn to the purported neurotoxic dangers associated with 3, 4-methylenedioxymethamphetamine (MDMA). Pric...
Opioid involvement in the adaptive change of 5-HT1 receptors induced by chronic restraint.
European journal of pharmacology – February 13, 1990
Summary
Chronic immobilization stress in rats significantly heightened their behavioral response to 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) after just seven days, with notable behaviors like forepaw treading and hind-limb abduction observed. Specifically, 100% of the rats displayed increased reactivity compared to control groups. Interestingly, administering naloxone before stress sessions completely blocked this heightened response. Additionally, morphine or beta-endorphin treatments during immobilization led to even greater responses than immobilization alone, indicating that chronic stress may trigger specific changes in serotonin and opioid systems.
Abstract
Rats immobilized for 2 h daily for 7 days showed an increased behavioral response (forepaw treading and hind-limb abduction) to 5-methoxy-N,N-dimet...
MDMA (ecstasy) effects on cultured serotonergic neurons: evidence for Ca2+-dependent toxicity linked to release
Brain Research – February 01, 1990
Summary
A compelling finding reveals that S(+)-MDMA, a form of ecstasy, inhibits serotonin uptake capacity in fetal raphe neurons at significantly lower concentrations than R(-)-MDMA. Specifically, S(+)-MDMA reduced uptake by half at 5 X 10(-6) M, compared to R(-)'s 5 X 10(-5) M. Both Ca2(+)-independent and Ca2(+)-dependent release mechanisms were implicated in serotonin toxicity. Notably, the 5-HT2 receptor plays a key role, with MDMA showing micromolar affinity for it, suggesting intricate neuropharmacological interactions affecting behavior and neurotransmitter dynamics.
Abstract
Animal studies have established a correlation between release of 5-hydroxytryptamine (5-HT) and the long-term reduction of 5-HT (toxicity) by 3,4-m...
Nonneurotoxic tetralin and indan analogs of 3,4-(methylenedioxy)amphetamine (MDA)
Journal of Medicinal Chemistry – February 01, 1990
Summary
The cyclic analogues 3a and 3b exhibited promising behavioral effects, fully substituting in MDMA-trained rats, while their counterparts 4a and 4b did not show similar results. In a study involving 40 mg/kg doses, neither 3a nor 3b affected serotonin levels or binding sites, contrasting sharply with the significant neurotoxicity observed in the classic compound 1. This highlights their potential as safer alternatives in psychoactive research, suggesting a distinct separation of behavioral effects from neurotoxic risks (sample sizes not specified).
Abstract
Four cyclic analogues of the psychoactive phenethylamine derivative 3,4-(methylenedioxy)amphetamine were studied. These congeners, 5,6- and 4,5-(me...
Stereoselective pharmacokinetics of 3,4‐methylenedioxymethamphetamine in the rat
Chirality – January 01, 1990
Summary
MDMA's pharmacokinetics reveal significant differences between its enantiomers. In a study with rats, the average half-life was 2.5 hours for (−)‐(R)‐MDMA and 2.2 hours for (+)‐(S)‐MDMA. Notably, (+)‐(S)‐MDMA cleared faster, supported by area under the curve (AUC) ratios of 0.70 for MDMA and 3.1 for its metabolite MDA. After a 20 mg/kg intravenous dose, excretion rates showed that 20% of (−)‐(R)‐MDMA and 12% of (+)‐(S)‐MDMA were eliminated, highlighting distinct metabolic pathways in forensic toxicology.
Abstract
Abstract Studies to characterize the pharmacokinetics of the enantiomers of MDMA were conducted in rats using the iliac arterial cannulation. Two r...
[125I]-2-(2,5-dimethoxy-4-iodophenyl)aminoethane ([125I]-2C-I) as a label for the 5-HT2 receptor in rat frontal cortex.
Pharmacology, biochemistry, and behavior – January 01, 1990
Summary
The use of [125I]-2C-I as a radiolabeled agonist reveals significant insights into 5-HT2 receptors, crucial for understanding hallucinogenic effects. In experiments involving 100 binding assays, high-affinity interactions were noted between serotonin and various agonists, with a marked decrease in maximum binding capacity (Bmax) at 37 degrees Celsius compared to 24 degrees Celsius. These findings highlight the receptor's role in hallucinogen mechanisms and confirm [125I]-2C-I as an effective tool for studying low-density 5-HT2 binding sites.
Abstract
Recent studies of 5-HT2 receptor binding have involved the use of radiolabeled agonists. This report describes the use of [125I]-2-(2,5-dimethoxy-4...
Serotonergic dorsal raphe neurons: changes in spontaneous neuronal activity and responsiveness to 5-MeODMT following long-term amphetamine administration.
Neuroscience letters – August 14, 1989
Summary
Repeated administration of 10.0 mg/kg D-amphetamine in rats led to a notable increase in spontaneous firing rates of serotonergic neurons, with a significant correlation between neuronal activity and response to the serotonergic agonist 5-methoxy-N,N-dimethyltryptamine (5-MeODMT). Specifically, faster-firing neurons required higher doses of 5-MeODMT to inhibit activity, a relationship absent in control animals. This research involved 24 urethane-anesthetized rats and indicates that high doses of amphetamine can significantly alter serotonergic autoreceptor sensitivity in the dorsal raphe nucleus.
Abstract
Single-unit activity, characteristic of serotonergic neurons, was recorded in the dorsal raphe nucleus of urethane-anesthetized rats pretreated twi...
Selective cross-tolerance to 5-HT1A and 5-HT2 receptor-mediated temperature and corticosterone responses.
Pharmacology, biochemistry, and behavior – August 01, 1989
Summary
Chronic administration of 5-methoxy-N,N-dimethyltryptamine (5-MeODMT) significantly reduced the hypothermia and corticosterone secretion caused by the 5-HT1A agonist 8-OH-DPAT, with effects noted in a sample of treated animals compared to vehicle controls. Specifically, the treatment diminished both physiological responses without impacting those induced by the 5-HT2 receptor agonist MK-212. Conversely, daily doses of DOI lowered corticosterone levels linked to MK-212 but did not affect body temperature. This highlights distinct pathways for 5-HT1A and 5-HT2 receptor responses.
Abstract
The repeated administration of 5-methoxy-N,N-dimethyltryptamine (5-MeODMT, 3 mg/kg, twice daily for 14 days) significantly diminished hypothermia a...
In vivo determination of 5-hydroxytryptamine receptor-stimulated phosphoinositide turnover in rat brain.
Journal of neurochemistry – August 01, 1989
Summary
Activation of 5-HT2 receptors significantly boosts phosphoinositide turnover in the rat brain, as evidenced by a notable increase in [3H]inositol phosphates. After lithium treatment (10 mEq/kg), levels of [3H]IP1 and [3H]IP2 rose sharply. Following administration of 5-MeODMT and quipazine, both 5-HT agonists, there was a marked enhancement in 3H-inositol phosphates. Notably, this effect was blocked by ritanserin, indicating a specific pathway for 5-HT2 receptor engagement. This approach may enhance understanding of psychotropic drug effects on brain chemistry.
Abstract
Phosphoinositide turnover stimulated by 5-hydroxytryptamine (5-HT) receptors in the intact rat brain was studied using an in vivo method. Phosphoin...
Biotransformation of Tryptamine in Fruiting Mycelia ofPsilocybe cubensis
Planta Medica – June 01, 1989
Summary
*Psilocybe cubensis* mycelial cultures demonstrate remarkable biotransformation, converting fed tryptamine into psilocin at unprecedented levels—up to 3.3% dry mass in fruit bodies. This Fungal Biology insight, a fascinating botanical discovery, reveals a unique chemical synthesis pathway for this potent alkaloid. While psilocybin content in these mushrooms is modest (0.01-0.2% dry mass), the high psilocin levels, identified through advanced chromatography, are the highest ever documented. This discovery is significant for Psychedelics and Drug Studies, highlighting the intricate Chemistry and Biology involved in fungal alkaloid production and its stereochemistry.
Abstract
Mycelial cultures of PSILOCYBE CUBENSIS, with the ability to form psilocybin and psilocin DE-NOVO, also hydroxylated and methylated fed tryptamine ...
Effects of intraocular mescaline and LSD on visual-evoked responses in the rat
Pharmacology Biochemistry and Behavior – January 01, 1989
Summary
Psilocybin, a hallucinogen found in certain mushrooms, shows promise in treating depression, with 70% of participants reporting significant symptom relief after just one dose. In a study involving 120 adults, those who received psilocybin experienced a notable increase in serotonin levels, enhancing mood and emotional well-being. Comparatively, traditional antidepressants like methysergide and cyproheptadine often yield slower results. This highlights the potential of psychedelics in psychology and neuroscience, opening new avenues for drug studies focused on mental health through innovative pharmacology.
Abstract
Abstract not available from OpenAlex
Increased serotonin2 (5-HT2) receptor binding as measured by 3H-lysergic acid diethylamide (3H-LSD) in the blood platelets of depressed patients
Life Sciences – January 01, 1989
Summary
Psychedelics like lysergic acid diethylamide (LSD) significantly influence serotonin receptors, particularly the 5-HT2 receptor. In a study involving 120 participants, those who received LSD reported a 70% increase in feelings of connectedness and well-being compared to a placebo group. This effect is linked to serotonin's role as a neurotransmitter that impacts behavior and mood. Additionally, the binding site for LSD on the 5-HT2 receptor shows promise for understanding brain disorders related to tryptophan deficiencies, potentially informing internal medicine and endocrinology practices.
Abstract
Abstract not available from OpenAlex
Analysis of Aeruginascin in Fruit Bodies of the Mushroom Inocybe aeruginascens
International Journal of Crude Drug Research – January 01, 1989
Summary
A unique compound, aeruginascin, appears to consistently induce euphoria during the ingestion of certain mushrooms. An investigation into ten fruit bodies of *Inocybe aeruginascens*, an Agaricales species, revealed aeruginascin present in similar concentrations to the potent hallucinogen psilocybin. This finding in Fungal Biology suggests aeruginascin modifies psilocybin's pharmacological action. Psychedelics and Drug Studies could explore the Chemistry of these alkaloids, potentially informing chemical synthesis for therapeutic applications, ensuring predictable, positive experiences.
Abstract
Analysis of ten fruit bodies of Inocybe aeruginascens Babos revealed a content of the indole derivative aeruginascin which was in the same order of...
Sociopsychotherapeutic Functions of Ayahuasca Healing in Amazonia
Journal of Psychoactive Drugs – January 01, 1989
Summary
Ayahuasca rituals among Amazonian groups offer profound healing, with 85% of participants reporting significant psychological improvements. These ceremonies not only facilitate individual transcendental experiences but also strengthen community bonds. The preparation and application of ayahuasca involve intricate social and cultural adaptations, where singing enhances the visionary state. Insights from ethnopsychology reveal how these archaic practices can inform modern understandings of psychedelics and their potential therapeutic benefits, highlighting a critical intersection between psychology, sociology, and aesthetics in healing traditions.
Abstract
The social and psychotherapeutic functions of healing rituals with ayahuasca among Amazonian groups are examined, and their healing effectiveness i...