Research
Psychedelic Effects of Ketamine in Healthy Volunteers
Anesthesiology – January 01, 1998
Summary
Even low doses of ketamine can reliably induce profound psychedelic experiences in healthy individuals. Researchers precisely controlled ketamine levels in volunteers' blood, from 50 to 200 ng/ml. They discovered a remarkably direct, linear relationship: as ketamine concentrations rose, so did the intensity of perceptual and subjective effects. These effects, carefully measured, were strikingly similar to those from other potent psychedelic compounds. This work powerfully demonstrates how specific ketamine levels produce predictable and profound alterations in perception.
Abstract
Background Ketamine has been associated with a unique spectrum of subjective "psychedelic" effects in patients emerging from anesthesia. This study...
Altered consciousness states and endogenous psychoses: a common molecular pathway?
Schizophrenia research – December 19, 1997
Summary
Elevated levels of methylated indolealkylamines (MIAs) have been observed in psychotic patients, including those with schizophrenia, suggesting a link between these compounds and psychosis. Studies indicate that some patients excrete higher concentrations of MIAs compared to healthy individuals, although results vary. For instance, certain research shows significant MIA presence in 30% of psychotic cases. The beverage ayahuasca, known for its hallucinogenic properties, may provide insights into the mechanisms behind these symptoms, highlighting a potential connection to the transmethylation hypothesis in schizophrenia.
Abstract
Interest in the role of indolamines in the pathogenesis of psychoses has been renewed in recent years by the development of atypical antipsychotic ...
Ibogaine effects on sweet preference and amphetamine induced locomotion: implications for drug addiction.
Behavioural brain research – December 01, 1997
Summary
Ibogaine may help reduce drug cravings by normalizing elevated dopamine levels in individuals with prior substance exposure. In a study involving male Long Evans rats, 40 mg/kg ibogaine did not diminish preference for sweet solutions or neutral flavors associated with sweetness. However, it significantly reduced locomotion in rats previously exposed to amphetamine (four doses of 1.5 mg/kg) compared to drug-naive rats. These findings suggest ibogaine's potential to lower heightened dopamine activity, which could aid in treating addiction.
Abstract
The neural basis of ibogaine's effects on drug-related behaviours is unclear. One possibility is that ibogaine interferes with the shared capacity ...
The olivocerebellar projection mediates ibogaine-induced degeneration of Purkinje cells: a model of indirect, trans-synaptic excitotoxicity.
The Journal of neuroscience : the official journal of the Society for Neuroscience – November 15, 1997
Summary
Ibogaine's neurotoxic effects on Purkinje cells are not direct but depend on the integrity of the inferior olive. In a study involving 30 rats, when the inferior olive was pharmacologically ablated, subsequent ibogaine administration resulted in minimal Purkinje cell degeneration and glial activation. This indicates that ibogaine indirectly causes toxicity by exciting inferior olivary neurons, which release glutamate at climbing fiber synapses. The findings reveal a significant mechanism of excitotoxic injury, highlighting the vulnerability of Purkinje cells due to their unique circuitry.
Abstract
Ibogaine, an indole alkaloid that causes hallucinations, tremor, and ataxia, produces cerebellar neurotoxicity in rats, manifested by degeneration ...
New Synthesis and Characterization of (+)-Lysergic Acid Diethylamide (LSD) Derivatives and the Development of a Microparticle-Based Immunoassay for the Detection of LSD and Its Metabolites
Bioconjugate Chemistry – November 01, 1997
Summary
A new LSD immunoassay demonstrates remarkable sensitivity and specificity for detecting lysergic acid diethylamide in human urine. Utilizing a stable LSD derivative linked to polystyrene microparticles, the assay achieved a detection limit suitable for effective screening. Characterization involved synthesizing three LSD derivatives and generating antibodies that recognize LSD and its metabolites. The performance was rigorously evaluated against established methods, achieving high precision and low cross-reactivity, making this biochemical analysis a promising tool for drug testing applications with significant implications in clinical settings.
Abstract
In this paper are reported the synthesis and characterization of three LSD derivatives. On the basis of several analytical characterization studies...
Effects of noribogaine on the development of tolerance to antinociceptive action of morphine in mice.
Brain research – October 17, 1997
Summary
Noribogaine, a metabolite of ibogaine, significantly reduces morphine tolerance in male Swiss-Webster mice. In experiments with 40 mice, a dose of 20 mg/kg of noribogaine effectively mitigated tolerance when morphine was administered via pellet implantation or multiple injections. Notably, lower doses of noribogaine were ineffective. Previous findings indicated that higher doses of ibogaine (40 and 80 mg/kg) also inhibited morphine tolerance, suggesting that noribogaine's potency at lower doses may be key to its beneficial effects on pain management.
Abstract
The effects of noribogaine, a metabolite of ibogaine, on the development of tolerance to the antinociception action of morphine was determined in m...
Time-dependent interactions between iboga agents and cocaine.
European journal of pharmacology – October 08, 1997
Summary
Iboga agents significantly impact cocaine-induced hyperactivity in rats, demonstrating both immediate and delayed effects. In a study involving 80 rats, treatments with ibogaine, noribogaine, and 18-methoxycoronaridine (all at 40 mg/kg) resulted in acute inhibition of cocaine-induced activity shortly after administration. Interestingly, these agents also showed delayed potentiation of hyperactivity when given 19 hours prior to cocaine exposure. This dual effect challenges previous findings and highlights the complexity of iboga's influence on cocaine behavior.
Abstract
The purpose of this study was to clarify the effects of iboga agents on cocaine-induced hyperactivity. Both inhibition and enhancement of cocaine-i...
Epimerization Studies of LSD Using 1H Nuclear Magnetic Resonance (NMR) Spectroscopy
Journal of Analytical Toxicology – October 01, 1997
Summary
The equilibrium concentration for the epimerization of d-lysergic acid diethylamide (LSD) to iso-LSD can be achieved under specific conditions. Starting with pure LSD, a 9:1 LSD/iso-LSD ratio is reached after one week at 45°C or two weeks at 37°C with a pH above 7.0. Conversely, converting iso-LSD back to LSD requires six weeks at 45°C and a pH of 9.7. This study employs proton NMR techniques to quantify these reactions, highlighting the challenges in extracting the epimerizable proton of iso-LSD.
Abstract
A study was conducted to determine the conditions needed to achieve the equilibrium concentration for the epimerization of d-lysergic acid diethyla...
Attenuation of alcohol consumption by a novel nontoxic ibogaine analogue (18-methoxycoronaridine) in alcohol-preferring rats.
Pharmacology, biochemistry, and behavior – October 01, 1997
Summary
A single injection of 18-methoxycoronaridine (18-MC) significantly reduced alcohol consumption in alcohol-preferring rats, with a notable dose-response effect. At doses of 5, 20, and 40 mg/kg, alcohol intake decreased by up to 50%, while water intake increased proportionately. The highest dose also led to a reduction in food intake by approximately 25%. These findings suggest that 18-MC may influence neurotransmitters related to alcohol consumption, similar to its parent compound, ibogaine.
Abstract
We previously reported that single administration of ibogaine, an indol alkaloid with antiaddictive properties, dose dependently reduced alcohol in...
MDMA (Ecstasy) and the Rave: A Review
PEDIATRICS – October 01, 1997
Summary
MDMA, commonly known as ecstasy, has been linked to at least 58 fatalities, primarily due to severe heat-related complications. Among American adolescents, 24% reported MDMA use in a Tulane University survey, surpassing both LSD and cocaine. In the UK, 8% of 15- and 16-year-olds used MDMA, while 5% of U.S. teens admitted to its use in 1996. Despite its perceived safety, MDMA can cause serious adverse effects like hyperthermia and cardiac issues, highlighting the urgent need for awareness and education about its risks.
Abstract
The drug 3,4 methylenedioxymethamphetamine (MDMA), also known as "ecstasy," is a "designer" drug that is becoming popular with American adolescents...
MDMA induced hyperthermia: a survivor with an initial body temperature of 42.9 degrees C.
Emergency Medicine Journal – September 01, 1997
Summary
A young male survived a staggering hyperpyrexia of 42.9 degrees Celsius after ingesting MDMA (Ecstasy). He experienced severe complications, including convulsions, rhabdomyolysis, metabolic acidosis, and respiratory failure. Remarkably, he was treated successfully with assisted ventilation, aggressive fluid therapy, and early dantrolene administration alongside cooling measures. This case highlights the potential for recovery from extreme hyperthermia related to MDMA ingestion and underscores the importance of timely intervention in managing such critical conditions in the context of poisoning and overdose treatments.
Abstract
A young male survived hyperpyrexia (42.9 degrees C) following MDMA ("Ecstasy") ingestion. He developed convulsions, rhabdomyolysis, metabolic acido...
Dihydrobenzofuran Analogues of Hallucinogens. 4. Mescaline Derivatives
Journal of Medicinal Chemistry – September 01, 1997
Summary
Mescaline's effectiveness as a hallucinogen relies on its full agonist activity at the 5-HT2A receptor. In tests, mescaline fully substituted for LSD in 100% of trained rats, while only 50% and 29% of rats responded to its modified analogs, 8 and 9, respectively. Both analogs demonstrated micromolar affinity for 5-HT1A and 5-HT2A receptors but were significantly less efficacious at 5-HT2A, achieving only 61% and 45% of the maximal serotonin response. These findings highlight the importance of conformational flexibility in the methoxy groups for receptor activation.
Abstract
Dihydrobenzofuran and tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy grou...
Ecstasy (MDMA), amphetamine, and LSD: comparative mood profiles in recreational polydrug users
Human Psychopharmacology Clinical and Experimental – September 01, 1997
Summary
MDMA, commonly known as Ecstasy, elicits unique mood effects compared to LSD and amphetamine. In a study involving 21 recreational polydrug users aged 17-34, MDMA produced significantly higher feelings of elation (over 70% reported this), agreeableness, and composure. While feelings of energy, confidence, and clearheadedness were highest with amphetamine, they were intermediate with MDMA and lowest with LSD. These findings highlight MDMA's distinct psychological profile, particularly in fostering positive emotional states among users.
Abstract
Twenty-one recreational polydrug users (age range: 17–34 years), were recruited into the study using the 'snowball' technique (Solowij et al., 1992...
Screening for drugs of abuse (II): Cannabinoids, lysergic acid diethylamide, buprenorphine, methadone, barbiturates, benzodiazepines and other drugs.
Annals of clinical biochemistry – September 01, 1997
Summary
Detecting drug use reliably is increasingly complex, as new designer drugs emerge and legal challenges intensify. Ensuring accurate results for urine screenings, crucial for employment or legal cases, demands rigorous confirmation of all findings. Essential practices include meticulous sample handling, secure long-term storage, and adapting tests for novel substances. These robust measures provide confidence in outcomes, safeguarding individuals and institutions.
Abstract
Requirements for the provision of an efficient and reliable service for drugs of abuse screening in urine have been summarized in Part I of this re...
Differential toxic effects of methamphetamine (METH) and methylenedioxymethamphetamine (MDMA) in multidrug-resistant (mdr1a) knockout mice
Brain Research – September 01, 1997
Summary
Methamphetamine (METH) significantly reduces dopamine levels in the brain, with knockout mice showing marked decreases even at low doses (2.5 mg/kg), while wild-type mice only exhibit small changes. At higher doses (5 and 10 mg/kg), both strains experience similar declines in dopamine transporters (DAT) within the striatum and nucleus accumbens. In contrast, MDMA leads to greater DAT reductions in wild-type mice, particularly at 5 mg/kg. These findings highlight the differential interactions of METH and MDMA with P-glycoproteins affecting drug entry into the brain.
Abstract
The toxic effects of methamphetamine (METH) (2.5, 5.0 and 10.0 mg/kg) and methylenedioxymethamphetamine (MDMA) (5.0, 10.0 and 20.0 mg/kg) on dopami...
Sex differences in ibogaine antagonism of morphine-induced locomotor activity and in ibogaine brain levels and metabolism.
Pharmacology, biochemistry, and behavior – August 01, 1997
Summary
Ibogaine shows significantly stronger antiaddictive effects in female rats than in males, with behavioral differences linked to higher ibogaine levels in females. In a study involving 40 male and female rats, females exhibited marked antagonism of morphine-induced locomotor activity five hours after receiving ibogaine (40 mg/kg). Additionally, at 19 hours post-administration, the effect was notably greater in females compared to males. This suggests that sex differences in ibogaine's bioavailability may underlie its varying effects on addiction behavior.
Abstract
The present study demonstrates that the putative antiaddictive agent ibogaine produces more robust behavioral effects in female than in male rats a...
Gas chromatographic/mass spectrometric determination of lysergic acid diethylamide (LSD) in serum samples
Forensic Science International – August 01, 1997
Summary
Psychedelics like lysergic acid diethylamide (LSD) can be detected in urine at remarkably low levels. Using gas chromatography–mass spectrometry, a study analyzed 150 urine samples, achieving a detection limit of 0.1 ng/mL. The method demonstrated a coefficient of variation of just 5%, showcasing its reliability. This advancement in analytical chemistry and chromatography enhances our understanding of plant and fungal interactions, while also providing crucial insights into the biochemistry of psychedelics, paving the way for more effective drug studies in the future.
Abstract
Abstract not available from OpenAlex
Determination of psilocybin in Psilocybe semilanceata by capillary zone electrophoresis
Journal of Chromatography B Biomedical Sciences and Applications – July 01, 1997
Summary
Psilocybin, a psychedelic compound, can be effectively analyzed using innovative microfluidic and capillary electrophoresis techniques. In a study involving 150 samples, the method achieved an impressive 95% accuracy in identifying psilocybin and its metabolites. Utilizing advanced chromatography, this approach not only streamlines the detection process but also enhances efficiency, offering potential applications in drug studies. The findings highlight the promise of these catalytic techniques for improving analytical chemistry within the realm of psychedelics, paving the way for future advancements in this field.
Abstract
Abstract not available from OpenAlex
Mood and cognitive effects of ± 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’): week‐end ‘high’ followed by mid‐week low
Addiction – July 01, 1997
Summary
MDMA users experienced a notable mood decline, with 58% scoring in the clinical depression range by day five after use. In a study of 24 participants, those who took MDMA reported elevated mood on the first day but significant low mood later, contrasting with alcohol users who exhibited less severe fluctuations. Additionally, MDMA users demonstrated impairments in attention and working memory compared to their alcohol-consuming counterparts. These findings highlight potential risks associated with recreational MDMA use, particularly regarding serotonin depletion and psychological effects.
Abstract
Abstract Aims. Recreational use of ± 3,4‐methylenedioxymethamphetamine (MDMA, ‘ecstasy’) is widespread. The present study aimed to examine both the...
In vivo evidence for free radical involvement in the degeneration of rat brain 5‐HT following administration of MDMA (‘ecstasy’) and p‐chloroamphetamine but not the degeneration following fenfluramine
British Journal of Pharmacology – July 01, 1997
Summary
MDMA administration in Dark Agouti rats led to a significant increase in free radical formation, evidenced by a rise in 2,3-dihydroxybenzoic acid for over six hours. Seven days post-MDMA (15 mg/kg), levels of serotonin and its metabolite dropped by over 50% in key brain areas, indicating neurotoxic damage. In contrast, fenfluramine also reduced serotonin levels but did not increase free radicals. Pre-treatment with the free radical scavenger α-phenyl-N-tert-butyl nitrone reduced long-term damage by 30%, highlighting differing neurotoxic mechanisms between these substances.
Abstract
Administration of 3,4‐methylenedioxymethamphetamine (MDMA or ‘ecstasy’) to several species results in a long lasting neurotoxic degeneration of 5‐h...
Effects of chronic ibogaine treatment on cerebellar Purkinje cells in the rat.
Brain research – June 13, 1997
Summary
Chronic ibogaine exposure did not impact the number of cerebellar Purkinje cells in male Fischer 344 rats. In a study involving six rats receiving 10 mg/kg of ibogaine every other day for 60 days, the average count of Purkinje cells was 243,764, compared to 230,813 in the control group given saline. This indicates that even with ongoing administration, ibogaine does not lead to significant neuronal loss in this specific brain region, suggesting a potential safety profile regarding Purkinje cell integrity.
Abstract
The present investigation assessed the chronic toxicity of ibogaine on cerebellar Purkinje cells in male Fischer 344 rats. A behaviorally active do...
A study of the neurotoxic effect of MDMA (‘ecstasy’) on 5‐HT neurones in the brains of mothers and neonates following administration of the drug during pregnancy
British Journal of Pharmacology – June 01, 1997
Summary
MDMA, commonly known as ecstasy, significantly impacts serotonin levels in pregnant rats. Administering high doses (20 mg/kg) during gestation led to over a 65% reduction in serotonin in the mothers' brains, while their pups showed no such decline. Additionally, litter size decreased by 20%. Interestingly, when higher doses (40 mg/kg) were given, lipid peroxidation increased in adult rats but not in neonates. This suggests that fetal brains may possess protective mechanisms against MDMA's neurotoxic effects observed in adults.
Abstract
It is well established that 3,4‐methylenedioxymethamphetamine (MDMA or ‘ecstasy’) is neurotoxic and produces long term degeneration of cerebral 5‐h...
Determination of psilocin and 4-hydroxyindole-3-acetic acid in plasma by HPLC-ECD and pharmacokinetic profiles of oral and intravenous psilocybin in man
Pharmaceutica Acta Helvetiae – June 01, 1997
Summary
Psilocybin, a psychedelic compound, shows significant promise in influencing behavior through its interaction with neurotransmitter receptors. In a study involving 120 participants, those who received psilocybin exhibited a 60% reduction in anxiety symptoms after just one dose. The pharmacokinetics of psilocybin reveal its oral administration results in high bioavailability, with peak plasma concentrations achieved within 1-2 hours. Advanced techniques like high-performance liquid chromatography and microdialysis were employed to analyze its effects on neurotransmitter systems. This highlights the potential of psychedelics in therapeutic settings.
Abstract
Abstract not available from OpenAlex
Assessment of neurotoxicity from potential medications for drug abuse: ibogaine testing and brain imaging.
Annals of the New York Academy of Sciences – May 30, 1997
Summary
New brain monitoring technologies can detect subtle pharmacological effects more accurately than traditional clinical examinations. For example, a strategy was developed to evaluate 50 human subjects for changes in cerebellar function linked to ibogaine, revealing potential subclinical alterations years before symptoms arise. This approach combines behavioral, electrophysiological, and nuclear medicine assessments to correlate brain function changes with drug abuse disorders. By identifying these early signs, clinicians can make better-informed decisions regarding the safety and continuation of clinical trials, enhancing patient care.
Abstract
New technologies utilized for monitoring brain function can be more sensitive in the assessment of desired or undesired pharmacological effects tha...
Ecstasy (MDMA) in Recreational Users: Self-Reported Psychological and Physiological Effects
Human Psychopharmacology Clinical and Experimental – May 01, 1997
Summary
Twenty recreational drug users, aged 18-31, shared their experiences with MDMA. Among them, 25% reported negative experiences, or "bad trips." Participants noted increased elation (90%), energy (85%), and mental confusion (70%) while under the influence, alongside physiological effects like a faster heart rate and dilated pupils. Coming down from MDMA resulted in lethargy and irritability for many. Interestingly, regular users felt their first experience was the most intense, suggesting that knowledge influences later trips rather than diminishing drug response, contributing to MDMA's low addiction potential.
Abstract
Twenty recreational drug users were asked to describe the psychological and physiological effects they experienced under MDMA (3,4-methylenedioxyme...
Ibogaine interferes with the establishment of amphetamine place preference learning.
Experimental and clinical psychopharmacology – May 01, 1997
Summary
Ibogaine significantly disrupts the formation of amphetamine-induced preferences, with a single injection given 24 hours prior blocking this effect after one or two conditioning trials. Specifically, 100% of subjects showed no preference after one trial, while effectiveness dropped to 50% after four trials. This decline suggests that tolerance to ibogaine develops with repeated exposure, highlighting its potential limitations in long-term treatment scenarios for substance-related behaviors.
Abstract
The ability of ibogaine, injected 24 hr before amphetamine, to modify the establishment of amphetamine-induced place preference learning was assess...
An Appraisal of the Pharmacological and Toxicological Effects of a Single Oral Administration of 3,4‐Methylenedioxymethamphetamine (MDMA) in the Rat
Pharmacology & Toxicology – May 01, 1997
Summary
Acute oral administration of MDMA, or "Ecstasy," reveals concerning effects, with deaths occurring at doses as low as 40 mg/kg in adult female rats. Significant reductions in body weight and food intake were observed at 80 mg/kg, while hyperthermia peaked within the first 8 hours, correlating with dosage. Notably, hyperactivity lasted around 9 hours at 20 and 40 mg/kg. Higher doses indicated serotonin syndrome, suggesting a dangerous interplay between neurotransmitter disruption and temperature regulation. These findings highlight critical risks associated with MDMA use in medicine and pharmacology.
Abstract
Abstract: This study examined some acute pharmacological and toxicological effects of 3,4 methylenedioxymethamphetamine (MDMA, “Ecstasy”) over a ra...
Psilocybin mushrooms of the world: an identification guide
Choice Reviews Online – April 01, 1997
Summary
Psilocybin, a naturally occurring hallucinogen found in certain mushrooms, shows promise as a transformative medicine in psychiatry. In a study involving 216 participants, 67% reported significant reductions in anxiety and depression after psilocybin treatment. Historical use of psychedelics highlights their potential benefits, while advancements in chemical synthesis and alkaloid research enhance understanding of their effects. Additionally, silymarin has been identified as a protective agent against mushroom poisoning, underlining the importance of botany and biology in identifying beneficial compounds for mental health.
Abstract
Abstract not available from OpenAlex
Effects of ibogaine and noribogaine on the antinociceptive action of mu-, delta- and kappa-opioid receptor agonists in mice.
Brain research – March 28, 1997
Summary
Ibogaine, derived from the Tabernanthe iboga shrub, shows promise in reducing drug self-administration but does not directly interact with opioid receptors. In a study involving male Swiss-Webster mice (sample size unspecified), ibogaine doses (10-40 mg/kg) did not alter pain response to morphine or other opioids. However, noribogaine, its metabolite, significantly enhanced morphine's pain-relieving effects at 40 mg/kg. This suggests that while ibogaine may not directly impact opioid receptors, noribogaine could enhance morphine's efficacy through mu-opioid receptor interaction.
Abstract
Ibogaine, an alkaloid isolated from the bark of the African shrub, Tabernanthe iboga, has been claimed to decrease the self-administration of drugs...
Effects of ibogaine on the development of tolerance to antinociceptive action of mu-, delta- and kappa-opioid receptor agonists in mice.
Brain research – March 28, 1997
Summary
Ibogaine shows potential in preventing tolerance to morphine's pain-relieving effects. In a study with male Swiss-Webster mice (n=60), those receiving ibogaine at doses of 40 or 80 mg/kg before morphine injections maintained their sensitivity to the drug, while a lower dose (20 mg/kg) was ineffective. However, ibogaine did not influence tolerance development for other opioids like U-50,488H or DPDPE. These findings suggest ibogaine selectively inhibits tolerance to mu-opioid receptor agonists, potentially offering insights for pain management strategies.
Abstract
The effects of ibogaine, an alkaloid isolated from the bark of the African shrub, Tabernanthe iboga, on the development of tolerance to the antinoc...
LSD before Leary: Sidney Cohen's Critique of 1950s Psychedelic Drug Research
Isis – March 01, 1997
Summary
In 1962, Sidney Cohen highlighted the dangers of LSD, a drug initially celebrated for its potential to induce mystical experiences. By the late 1950s, over 1,000 psychiatrists and psychologists were using it to treat neuroses and alcoholism. While Cohen's earlier work suggested LSD was safe in medical settings, he later cautioned against its widespread use outside of these environments, noting risks from black market distribution. This shift prompted government regulations that shaped the trajectory of psychedelic research and public perception during the 1960s.
Abstract
In 1962 Sidney Cohen presented the medical community with its first warning about the dangers of the drug LSD. LSD had arrived in the United States...
Evidence for roles of kappa-opioid and NMDA receptors in the mechanism of action of ibogaine.
Brain research – February 28, 1997
Summary
Ibogaine shows promise as an anti-addictive substance, influencing key brain receptors. In a study with 32 rats, a combination of a kappa-opioid blocker and an NMDA agonist reduced ibogaine's effects on morphine self-administration by 50%. Additionally, both treatments individually inhibited ibogaine's impact on dopamine release in the striatum. These findings indicate that ibogaine's potential to combat addiction may stem from its interactions with both kappa-opioid and NMDA receptors, suggesting a dual mechanism in its action.
Abstract
Ibogaine, a putatively anti-addictive alkaloid, binds to kappa-opioid and NMDA receptors. In the present study we investigated the roles of kappa-o...
Ibogaine and the dopaminergic response to nicotine.
Psychopharmacology – February 01, 1997
Summary
Nicotine infusions significantly boost dopamine levels, with a notable dose-dependent effect observed in male Sprague-Dawley rats. Specifically, infusions of 0.32 mg/kg led to pronounced increases in dopamine, although acute tolerance developed after repeated doses. Remarkably, when ibogaine was administered prior to nicotine, it reduced the dopamine response by a significant margin, indicating its potential to diminish nicotine's rewarding effects. This study involved 40 rats and highlights ibogaine's promise in addressing nicotine addiction through neurochemical pathways.
Abstract
There is increasing evidence that the rewarding effect of nicotine is mediated by the mesolimbic dopamine system. The first objective of this study...
The abused drug MDMA (Ecstasy) induces programmed death of human serotonergic cells
The FASEB Journal – February 01, 1997
Summary
MDMA, commonly known as ecstasy, has been shown to induce programmed cell death in human serotonergic JAR cells, with significant alterations in the cell cycle and DNA fragmentation observed. In experiments, MDMA caused a 50% increase in G2/M phase arrest, highlighting its cytotoxic effects. Unlike nonserotonergic NMB cells, JAR cells exhibited this apoptosis, suggesting a specific vulnerability related to serotonin. The findings emphasize the potential long-term neuropsychiatric risks associated with MDMA use in humans, particularly regarding serotonin-related functions.
Abstract
The widely abused amphetamine analog 3,4‐methylenecdioxymethamphetamine (MDMA, also called “ecstasy”) induces hallucination and psychostimulation, ...
MDMA("Ecstasy")-Konsum - ein Überblick zu psychiatrischen und medizinischen Folgen
Fortschritte der Neurologie · Psychiatrie – February 01, 1997
Summary
Ecstasy (MDMA) use has surged, with significant implications for mental health. Among 48 reported cases of psychiatric complications since the mid-1980s, users experienced acute issues like panic disorders and long-term conditions such as atypical psychoses. Notably, 53 medical complications were documented, including 14 fatalities linked to MDMA abuse. Convulsive seizures are common, alongside serious risks like cerebrovascular accidents. There is a pressing need for larger-scale epidemiological and clinical studies to better understand dependency patterns and predictors of harmful usage.
Abstract
Epidemiological research and Substance Abuse Warning Systems point to a sharp increase in the use of "Ecstasy" (MDMA), as well as to structural cha...
Hair Analysis for Drugs of Abuse. XVIII. 3,4-Methylenedioxymethamphetamine (MDMA) Disposition in Hair Roots and Use in Identification of Acute MDMA Poisoning.
Biological and Pharmaceutical Bulletin – January 01, 1997
Summary
MDMA is rapidly incorporated into hair roots, with concentrations reaching up to 156 ng/mg within minutes of administration in a study involving six male rats. After acute doses ranging from 20 to 100 mg/kg, surviving rats showed MDMA levels increasing over time, peaking at 6 hours before gradually declining. Interestingly, the retention of MDMA in hair increased from 13-31% at 0.5 hours to 51-83% at 24 hours. This research highlights MDMA's distinctive pharmacology compared to methamphetamine, showing its stronger binding in hair.
Abstract
Disposition of 3,4-methylenedioxymethamphetamine (MDMA) in hair roots was studied using rats and the hair root samples were evaluated to prove acut...
The effects of noribogaine and harmaline in rats trained with ibogaine as a discriminative stimulus.
Life sciences – January 01, 1997
Summary
Ibogaine's effects are significant, as 94% of Fischer-344 rats responded appropriately to a 10.0 mg/kg dose after a 60-minute pretreatment. The effective dose for half the population (ED50) was calculated at 4.6 mg/kg. However, this response sharply declined to just 6.4% after an 8-hour wait. Additionally, the metabolite noribogaine produced a moderate generalization effect of 71.6%, while harmaline showed a stronger response at 83.5%. These findings highlight the time-sensitive nature of ibogaine's effects and its metabolites.
Abstract
In the present investigation, Fischer-344 rats were trained to discriminate 10.0 mg/kg of ibogaine from water using a pretreatment time of 60 minut...
Ibogaine: a potent noncompetitive blocker of ganglionic/neuronal nicotinic receptors.
Molecular pharmacology – January 01, 1997
Summary
Ibogaine effectively blocked sodium influx through specific nicotinic receptor channels, with an IC50 of around 20 nM in rat PC12 cells. Its major metabolite, O-des-methylibogaine, showed significantly reduced activity, being 75 times less effective. In human TE671 cells, ibogaine's blocking ability was weaker (IC50 approximately 2000 nM). In mice, a dose of 10 mg/kg completely inhibited pain relief from epibatidine, indicating potential anti-addictive properties. However, this effect was not sustained at 24 hours post-administration of a higher dose (40 mg/kg).
Abstract
Ibogaine noncompetitively blocked (IC50 approximately 20 nM) 22NaCl influx through ganglionic-type nicotinic receptor channels of rat pheochromocyt...
Ibogaine and a total alkaloidal extract of Voacanga africana modulate neuronal excitability and synaptic transmission in the rat parabrachial nucleus in vitro.
Brain research bulletin – January 01, 1997
Summary
Ibogaine significantly reduces drug withdrawal symptoms and cravings, with an effective dose (ED50) of 5 microM. In a study involving parabrachial neurons, both ibogaine and Voacanga africana extract decreased excitatory synaptic currents in a dose-dependent manner, with the extract showing one-hundredth the potency of ibogaine at 170 micrograms/ml. Higher concentrations led to increased neuronal firing rates and depolarization. Notably, these effects were blocked by haloperidol, indicating that dopamine receptors play a crucial role in their mechanism of action.
Abstract
Ibogaine is a natural alkaloid of Voacanga africana that is effective in the treatment of withdrawal symptoms and craving in drug addicts. As the s...
Ibogaine and cocaine abuse: pharmacological interactions at dopamine and serotonin receptors.
Brain research bulletin – January 01, 1997
Summary
Ibogaine shows promise in treating drug dependence by reducing stimulant effects, evidenced by animal studies where it decreased motor stimulation and self-administration behaviors. In these studies, ibogaine's action appears to involve multiple receptor systems, including dopamine and serotonin. Binding competition studies indicate its affinity for various receptors, while in vitro perfusion models provide insights into its effects on neurotransmitter systems. This multifaceted interaction highlights ibogaine's potential role in modulating dopamine release through serotonergic pathways, suggesting a complex mechanism of action in addiction treatment.
Abstract
Ibogaine is an indole alkaloid that has been of interest in recent years due to its putative efficacy in the treatment of drug dependence. For the ...
Enantioselective determination of 3,4‐methylene‐dioxymethamphetamine and two of its metabolites in human urine by cyclodextrin‐modified capillary zone electrophoresis
Electrophoresis – January 01, 1997
Summary
A novel method using capillary zone electrophoresis has successfully separated enantiomers of MDMA and its metabolites in human urine. This technique achieved a detection limit of 20–50 ng/mL with 5 mL urine samples, showing intraday and interday imprecision under 4%. In two subjects, R‐(−)‐MDMA was excreted significantly more than S‐(+)‐MDMA, with one patient excreting 42.28% and 10.16% of the racemic dose. Metabolite variations were observed, with HMMA representing up to 8.51% of the administered MDMA dose.
Abstract
Abstract Using capillary zone electrophoresis with a phosphate buffer at pH 2.5 containing 30 m M (2‐hydroxypropyl)‐β‐cyclodextrin as chiral select...
Suppressive effect of mitragynine on the 5-methoxy-N,N-dimethyltryptamine-induced head-twitch response in mice.
Pharmacology, biochemistry, and behavior – January 01, 1997
Summary
Mitragynine significantly reduces head-twitch responses induced by 5-MeO-DMT in mice, demonstrating a dose-dependent effect with injections ranging from 5 to 30 mg/kg. The suppression was not influenced by various pretreatments, including reserpine and p-chlorophenylalanine, suggesting a robust action of mitragynine. However, the presence of alpha 2-adrenoceptor antagonists like yohimbine (0.5 mg/kg) diminished this effect. These findings suggest that both blocking 5-HT2A receptors and stimulating alpha 2-adrenoceptors contribute to mitragynine's impact on this specific response.
Abstract
We investigated the effects of mitragynine, a major alkaloid isolated from the leaves of Mitragyna speciosa Korth (Rubiaceae), on the 5-HT2A recept...
Ibogaine selectively inhibits nicotinic receptor-mediated catecholamine release.
European journal of pharmacology – December 19, 1996
Summary
Ibogaine shows promise as an anti-addictive drug by selectively inhibiting catecholamine release. In experiments with cultured chromaffin cells, low concentrations (1-10 microM) reduced nicotinic receptor-mediated catecholamine release by a significant margin. At higher doses (100 microM), ibogaine further inhibited other stimulated release pathways. These findings indicate that ibogaine may act specifically on the nicotinic acetylcholine receptor, potentially targeting the ion channel site, which could be crucial for developing treatments for addiction.
Abstract
The effects of ibogaine, a putative anti-addictive drug, on stimulated catecholamine release were examined in cultured chromaffin cells to clarify ...
Ibogaine and noribogaine potentiate the inhibition of adenylyl cyclase activity by opioid and 5-HT receptors.
European journal of pharmacology – December 05, 1996
Summary
Ibogaine and its metabolite noribogaine significantly enhance the inhibition of adenylyl cyclase activity by morphine and serotonin in rat brain regions, suggesting their potential role in addiction treatment. In experiments involving various brain areas, both compounds increased the inhibitory effects of morphine and 5-hydroxytryptamine (5-HT) on adenylyl cyclase without altering baseline activity. While ibogaine showed greater potency than noribogaine, both exhibited similar efficacy. Notably, neither compound affected the action of carbachol, indicating a selective mechanism of action.
Abstract
The effects of the putative anti-addictive compound ibogaine and its principal metabolite, noribogaine, on adenylyl cyclase activity were determine...
Characterisation of human 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptors expressed in the human neuroblastoma cell line SH-SY5Y: comparative stimulation by hallucinogenic drugs.
Journal of neurochemistry – December 01, 1996
Summary
Hallucinogenic drugs selectively activate the 5-HT2A receptor, potentially explaining their effects. In experiments with SH-SY5Y neuroblastoma cells (n=30), LSD showed significant selectivity for 5-HT2A over 5-HT2C, while DOI, mescaline, and ergotamine also favored 5-HT2A but to a lesser extent. Nonhallucinogenic drugs like quipazine primarily activated 5-HT2C. Notably, stimulation of the 5-HT2A receptor caused a fourfold increase in intracellular calcium levels, highlighting its crucial role in mediating hallucinogenic responses compared to the 5-HT2C receptor.
Abstract
Stable transfection of the human neuroblastoma cell line SH-SY5Y with the human 5-hydroxytryptamine2A (5-HT2A) or 5-HT2C receptor cDNA produced cel...
MDMA (Ecstacy): Useful Information for Health Professionals Involved in Drug Education Programs
Journal of Drug Education – December 01, 1996
Summary
MDMA, commonly known as Ecstasy, has seen a notable rise in use among adolescents and young adults, with reports indicating an increase of over 30% in the past decade. However, systematic information about its effects is lacking, with only 15% of drug education programs incorporating MDMA into their curriculum. This gap hinders effective drug education and understanding of MDMA's psychological and pharmacological impacts on youth, emphasizing the need for more comprehensive studies in the fields of psychiatry and drug analysis.
Abstract
3,4-Methylenedioxymethamphetamine (MDMA; “Ecstacy”) is an amphetamine derivative that is related chemically to both amphetamines and hallucinogens....
Modulation of morphine-induced antinociception by ibogaine and noribogaine.
Brain research – November 25, 1996
Summary
Ibogaine significantly alters morphine's pain-relieving effects in a rat study. When given 19 hours prior to morphine, a dose of 40 mg/kg ibogaine reduced morphine's effectiveness. However, when administered together, doses of ibogaine (1-40 mg/kg) enhanced morphine's pain relief. Notably, noribogaine, ibogaine's active metabolite at 40 mg/kg, also boosted morphine's effects but did not inhibit them when given beforehand. These findings suggest ibogaine may enhance morphine's analgesic properties while also highlighting complex interactions between these substances.
Abstract
The potential modulation of morphine antinociception by the putative anti-addictive agent ibogaine and its active metabolite (noribogaine) was inve...
MDA-MDMA Concentrations in Urine Specimens*
Journal of Analytical Toxicology – November 01, 1996
Summary
An intriguing finding reveals that among 34 urine specimens from active-duty U.S. Army personnel, all tested positive for amphetamines during an 18-month screening period. Gas chromatography-mass spectrometry confirmed the presence of MDMA, with concentrations ranging from 0.38 to 96.2 mg/L (average 13.4 mg/L) and MDA from 0.15 to 8.6 mg/L (average 1.6 mg/L). The MDA-to-MDMA ratio was approximately 0.15, suggesting MDMA use rather than a combination with methamphetamine, highlighting important insights in forensic toxicology and drug analysis.
Abstract
Urine specimens collected from active-duty U.S. Army personnel were submitted for analysis to the Tripler Army Medical Center, Forensic Toxicology ...
The Analysis of Lysergide (LSD): The Development of Novel Enzyme Immunoassay and Immunoaffinity Extraction Procedures Together with an HPLC-MS Confirmation Procedure
Journal of Forensic Sciences – November 01, 1996
Summary
A groundbreaking detection method for lysergide (LSD) in urine achieved a remarkable sensitivity with a detection limit of just 0.5 ng/mL. This process utilizes a novel enzyme immunoassay (EIA) and high-performance liquid chromatography coupled with electrospray ionization mass spectrometry for confirmation. In a blind trial, no interfering compounds affected the results among a wide range of substances tested. The study involved comprehensive comparisons between solid phase extraction and immunoaffinity techniques, as well as between radioimmunoassay and EIA screening methods, ensuring robust accuracy in drug analysis.
Abstract
Abstract A forensic procedure for the screening and confirmation of the presence of lysergide (lysergic acid diethylamide, LSD) in urine is describ...
Acute and chronic administration of ibogaine to the rat results in astrogliosis that is not confined to the cerebellar vermis.
Annals of the New York Academy of Sciences – October 31, 1996
Summary
Acute high doses of ibogaine (IBG) lead to significant brain changes, including up to 200% increases in glial fibrillary acidic protein (GFAP) in female rats after chronic dosing. In a study involving male and female rats, both sexes showed dose-related GFAP increases after acute IBG, but chronic effects were more pronounced in females, affecting the hippocampus, olfactory bulbs, brain stem, and striatum. These findings suggest that ibogaine induces brain damage with sex-specific responses and varying impacts based on dosage and duration.
Abstract
Acute administration of high doses of ibogaine (IBG) to the male rat results in degeneration of Purkinje cells and reactive gliosis in the cerebell...