Bufotenine (5-hydroxy-N,N-dimethyltryptamine) has been reported to be behaviorally inactive or only very weakly active in man and animals; this may be a consequence of its low partition coefficient and resultant inability to penetrate the blood--brain barrier. The acetyl, propionyl, butyryl, isobutyryl, and pivalyl esters of bufotenine were prepared for future pharmacological evaluation....
Using a food-reinforced two-lever operant method, rats (n = 9) were trained to discriminate 0.16 mg/kg LSD from saline. Tests for stimulus generalization in rats so trained indicated that the purported 5-HT antagonists cyproheptadine (1.25 and 10 mg/kg), methysergide (0.16 to 10 mg/kg) and mianserin (2.5 to 40 mg/kg) produced partial generalization with LSD. The hallucinogens mescaline (5 to 40...
An hallucinogen analogue, trans-2-(2,5-dimethoxy-4-methylphenyl)cyclopropylamine (DMCPA), was resolved into ints two enantiomers by fractional crystallization of salts with d- or l-O,O-dibenzoyltartaric acid. A comparison of the ORD and CD curves of the N-5-bromosalicylidene derivatives of trans-2-phenylcyclopropylamine of known absolute configuration and of the title compound established the...
Editorials1 March 1979The Paradox of Phencyclidine (PCP) AbuseRICHARD STILLMAN, M.D., ROBERT C. PETERSEN, PH.D.RICHARD STILLMAN, M.D.Search for more papers by this author, ROBERT C. PETERSEN, PH.D.Search for more papers by this authorAuthor, Article, and Disclosure Informationhttps://doi.org/10.7326/0003-4819-90-3-428 SectionsAboutPDF ToolsAdd to favoritesDownload CitationsTrack...
The hallucinogenic indoleamine drugs N,N-dimethyltryptamine (N,N-DMT), psilocybin, bufotenin, 5-methoxy-N,N-dimethyltryptamine, and N-methyltryptamine, increased rat plasma prolactin (PRL) levels. The increase in plasma PRL produced by N,N-DMT, psilocybin, and bufotenin was inhibited by methysergide, a serotonin receptor blocker. Parachlorophenylalanine (PCPA), an inhibitor of serotonin...
A methylated derivative of serotonin, O-methyl-bufotenine has been labeled with 11C on the two methyl groups of the amine function. In order to avoid the cyclization which occurs during the Eschweiler-Clarke synthesis, we adopted a milder methylation procedure, based on Borch's method using [11C]formaldehyde and sodium cyanoborohydride. Several tens of millicuries of injectable product could be...
Journal Article The influence of mescaline on the flexor reflex of the hind limb of the spinal rat Get access J Maj, J Maj Institute of Pharmacology, Polish Academy of Sciences, Cracow, Poland Correspondence: Institute of Pharmacology, Polish Academy of Sciences, Cracow, Poland Search for other works by this author on: Oxford Academic Google Scholar W Palider, W Palider Institute of...
The dopaminergic actions of various hallucinogenic drugs were assessed by examining their effects on turning behavior in rats with unilateral 6-hydroxydopamine lesions of the nigro-striatal pathway. LSD (0.1 and 0.2 mg/kg) produced strong contralateral turning, indicating that it is a potent dopamine receptor agonist, while BOL (5 mg/kg), a non-hallucinogenic congener of LSD, was found to be a...
SYNOPSIS Oral treatment of phantom limb pain in five males and two females ranging in age from 25 to 78 years with sub‐hallucinogenic doses of Iysergic acid diethyImaide (LSD‐25) resulted in improvement in pain in five patients and reduction in use of analgesics. In two of the five patients improvement was striking and in the other three, pain and analgesic use were reduced moderately. LSD...
A method in vitro designed to determine specifically the stereospecificity of tissue receptor sites was used to study the characteristics of d-lysergic acid diethylamide (LSD) binding by rat brain particulates and the effects of selectively chosen drugs. There is a high- and a low-affinity binding, and both are stereospecific. The high-affinity binding is saturable (half-saturation at 4 nM) and...