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Predicting new molecular targets for known drugs
Compared 3,665 US Food and Drug Administration (FDA)-approved and investigational drugs against hundreds of targets, defining each target by its ligands, chemical similarities between drugs and ligand sets predicted thousands of unanticipated associations.
Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents.
3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.
It is found that long-term MDMA use could lead to the development of fenfluramine-like VHD, and the necessity of screening current and future drugs at h5-HT2B receptors for agonist actions before their use in humans is underscored.
Radioligand binding evidence implicates the brain 5-HT2 receptor as a site of action for LSD and phenylisopropylamine hallucinogens
Results indicate that an important component of the mechanism of action of LSD and the phenylisopropylamine hallucinogens is through stimulation of brain 5-HT2 receptors, and supports previous suggestions to this effect.
Abuse-related and abuse-limiting effects of methcathinone and the synthetic “bath salts” cathinone analogs methylenedioxypyrovalerone (MDPV), methylone and mephedrone on intracranial self-stimulation…
All compounds facilitated ICSS at some doses and pretreatment times, which is consistent with abuse liability for each of these compounds, but efficacies of compounds to facilitate ICSS varied, with methcathinone displaying the highest efficacy and mephedrone displaying the lowest efficacy.
Do functional relationships exist between 5-HT1A and 5-HT2 receptors?
Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors
- D. Nelson, V. Lucaites, D. Wainscott, R. Glennon
- Biology, PsychologyNaunyn-Schmiedeberg's Archives of Pharmacology
The present study examined and compared the binding of 17 phenylisopropylamines at human 5- HT2A, 5-HT2B, and 5-Hat2C receptors and found a significant correlation between 5-ht2B receptor affinity and human hallucinogenic potency.
In Vitro Characterization of Ephedrine-Related Stereoisomers at Biogenic Amine Transporters and the Receptorome Reveals Selective Actions as Norepinephrine Transporter Substrates
- R. Rothman, Nga Vu, R. Glennon
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 October 2003
The data indicate that the pharmacological effects of ephedrine-like phenylpropanolamines are likely mediated by norepinephrine release, and although sharing mechanistic similarities with, they differ in important respects from those of the phenyl Propanonamines methcathinone and cathin one and the phenyisopropylamines methamphetamine and amphetamine.
Behavioral and biochemical investigations of bupropion metabolites.
Binding of beta-carbolines and related agents at serotonin (5-HT(2) and 5-HT(1A)), dopamine (D(2)) and benzodiazepine receptors.
It is difficult to conclude that the beta-carbolines behave in a manner consistent with that of other classical hallucinogens, as they lack of agonist action in the PI hydrolysis assay.