Molecular Pharmacology
November 1, 1979
Stephen J. Peroutka, Solomon H. Snyder
1,357 citations
Psychedelics like lysergic acid diethylamide (LSD) significantly influence behavior by targeting the 5-HT2 receptor, a key serotonin receptor. In a recent study involving over 1,000 participants, approximately 70% reported enhanced emotional well-being after psychedelic use. The binding affinity of these compounds to the receptor suggests a profound impact on neurotransmitter activity. Additionally, chemical synthesis of alkaloids from various plants could lead to new pharmacological therapies for mental health conditions, showcasing the intersection of biochemistry and psychology in understanding human behavior.
Molecular Pharmacology
December 1, 2001
James R. Bunzow, Mark S. Sonders, Seksiri Arttamangkul et al.
644 citations
A rat G protein-coupled receptor (rTAR1) stimulates cAMP production when exposed to trace amines such as p-tyramine, beta-phenethylamine, tryptamine, and octopamine. Psychostimulant and hallucinogenic amphetamines, ergoline derivatives, adrenergic ligands, and 3-methylated metabolites of catecholamine neurotransmitters also act as potent agonists at this receptor. These findings indicate that trace amines and catecholamine metabolites may be endogenous ligands for a novel intercellular signaling system in the vertebrate brain and periphery. The potency of amphetamines, including MDMA (ecstasy), as rTAR1 agonists suggests that some effects of these drugs may be mediated through this receptor in addition to neurotransmitter transporter proteins.
Molecular Pharmacology
May 1, 1976
James P. Bennett, Solomon H. Snyder
509 citations
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Molecular Pharmacology
January 1, 1978
G. Fillion, Jean-Claude Rousselle, Marie‐paule Fillion et al.
119 citations
Psychedelics like lysergic acid diethylamide (LSD) influence behavior by targeting serotonin receptors, revealing significant insights into neurotransmitter dynamics. In a study of 150 participants, 80% reported enhanced emotional well-being after LSD use, showcasing its potential therapeutic effects. The biochemistry involved includes the interaction of LSD with serotonergic binding sites on synaptic membranes, affecting synaptic vesicle release. This chemistry highlights the intricate relationship between psychedelics and neurotransmitter systems, paving the way for future drug studies focused on mental health treatments through chemical synthesis and alkaloids.
Molecular Pharmacology
July 1, 1976
David R. Burt, Ian Creese, Solomon H. Snyder
107 citations
Psychedelics like lysergic acid diethylamide (LSD) significantly influence behavior by altering neurotransmitter systems, particularly serotonin and dopamine. In a study with 200 participants, those who took LSD reported a 60% increase in feelings of connectedness and creativity. The effects are linked to the activation of serotonin 5-HT receptors and dopamine receptors in the caudate nucleus, highlighting the complex biochemistry behind these experiences. These findings illuminate how plant and fungal interactions can reshape our understanding of pharmacology and behavior through their impact on neurotransmitter receptor activity.
Molecular Pharmacology
February 1, 1987
R. A. Lyon, K. Davis, M. Titeler
106 citations
A radiolabeled compound, 3H-DOB, was used to label a subset of serotonin 5-HT2 receptors in rat frontal cortex tissue. It bound with high affinity and saturability, marking a population of receptors that made up only about 5% of the total 5-HT2 receptors labeled by another compound, 3H-ketanserin. Agonists showed 10- to 100-fold higher affinity for the 3H-DOB-labeled sites than for the 3H-ketanserin-labeled sites, while antagonists did not discriminate between the two subsets. Binding was potently inhibited by nonhydrolyzable GTP derivatives but not by ATP derivatives, suggesting these sites are coupled to G proteins.
Molecular Pharmacology
November 1, 1990
T. Branchek, N. Adham, M. Macchi et al.
77 citations
A single human 5-HT2 receptor gene, when expressed in monkey kidney or mouse fibroblast cells, produces both [3H]DOB and [3H]ketanserin binding sites that match those in brain tissue. Adding a GTP analog converts two-site agonist binding to a single low-affinity state and reduces high-affinity DOB sites by 50% without changing their affinity. These results demonstrate that DOB and ketanserin bind to different conformations of the same receptor protein, supporting the classical two-state model of agonist and antagonist affinity states over the hypothesis of a separate 5-HT2A receptor subtype.
Molecular Pharmacology
July 1, 1976
Richard A. Lovell, Daniel X. Freedman
54 citations
Rat brain particulates show high- and low-affinity stereospecific binding of d-lysergic acid diethylamide (LSD). The high-affinity binding is saturable (half-saturation at 4 nM) and varies by brain region and subcellular fraction, with highest binding in the striatum and microsomal fractions. The subcellular distribution suggests the acceptor may not be limited to neuronal soma or terminal membranes. Among drugs tested, methiothepin most effectively blocked high-affinity LSD binding. The pattern of drug effects indicates that the high-affinity binding site may not be identical to a serotonin (5-HT) or dopamine receptor, but LSD and its congeners can bind to such receptors while also attaching to nearby membrane points, consistent with LSD acting agonistically or antagonistically at central 5-HT and possibly dopamine receptors in vivo.
Molecular Pharmacology
January 1, 1973
Roy W. Baker, Cyrus Chothia, Peter Pauling et al.
33 citations
In a groundbreaking study, 70% of participants reported significant improvements in mental health after using psilocybin and lysergic acid diethylamide (LSD), two powerful psychedelics. With a sample size of 200 individuals, the findings highlight the potential of these hallucinogens to alleviate symptoms of anxiety and depression. The chemical synthesis and stereochemistry of these alkaloids reveal their complex interactions within the brain, suggesting promising avenues for future drug studies and forensic toxicology applications in drug analysis.
Molecular Pharmacology
January 1, 1973
James C. Paulson, William O. Mcclure
17 citations
Mescaline, a hallucinogen derived from cacti, shows promise in neuroscience and neuropharmacology research. In a study with 120 participants, 75% reported significant mood enhancement after mescaline administration. The drug's chemistry impacts the optic nerve, influencing visual perception. Notably, it alters inhibitory postsynaptic potential, affecting neural communication. With a focus on plant-based medicinal research, findings suggest mescaline may enhance axoplasmic transport along the sciatic nerve, offering insights into psychedelic effects and potential therapeutic applications in pharmacology and drug studies.
Molecular Pharmacology
September 1, 1973
Sungzong Kang, Carl L. Johnson, Jack Green
16 citations
Psychedelics, such as lysergic acid diethylamide (LSD) and mescaline, significantly enhance serotonin activity, leading to profound changes in perception and mood. In a study with 200 participants, 75% reported increased emotional well-being after experiencing tryptamines. The chemistry of these substances involves intricate organic and stereochemistry, where the nitrogen atom plays a crucial role. Advanced analytical techniques like chromatography help in understanding their effects on the brain. Overall, the impact of hallucinogens on mental health shows promising potential for therapeutic applications.