Psychopharmacology
1988
M Titeler, R A Lyon, Richard A Glennon
Alterations in brain serotonergic function have been implicated in the mechanism of action of LSD, mescaline, and other similarly acting hallucinogenic drugs of abuse such as STP (2,5-dimethoxyphenylisopropylamine; DOM). In order to test the hypothesis that the mechanism of action of LSD and phenylisopropylamine hallucinogens is through stimulation of a specific brain serotonin receptor...
Pharmacology, biochemistry, and behavior
September 1987
J A Rosecrans, R A Glennon
The behaviorally disruptive effects of the optical isomers of 1-(3,4-methylenedioxyphenyl-2-aminopropane) (MDA) and its N-methyl derivative (MDMA) were evaluated in 27 mice trained to bar-press for a liquid food reinforcement. In addition, a second study was conducted in which mice were pretreated with either saline or the 5-HT-2 antagonist, pirenpirone, prior to the administration of either...
Pharmacology, biochemistry, and behavior
March 1, 1987
Richard A Glennon, M Yousif, N Naiman et al.
The purpose of the present investigation was to examine the effect of N-monomethylation of phenylisopropylamine derivatives on amphetamine-like activity. In tests of stimulus generalization using rats trained to discriminate 1.0 mg/kg of (+)-amphetamine from saline, the N-monomethyl derivatives of 1-(X-phenyl)-2-aminopropane, where X = 2,4-dimethoxy (2,4-DMA), 3,4-dimethoxy (3,4-DMA),...
European Journal of Pharmacology
December 1, 1986
Kurt Rasmussen, Richard A Glennon, George K. Aghajanian
50 citations
The rank order of potency for the physiological effects of three phenethylamine hallucinogens in the locus coeruleus (LC) was identical to that previously shown for their 5-HT2 binding affinity [-) DOB greater than DOM greater than ( + )DOB). The behaviorally inactive positional isomer of DOB, SL-7161, did not significantly affect LC unit activity. These results offer insight into...
Pharmacology, biochemistry, and behavior
December 1, 1986
R Young, John A. Rosecrans, Richard A Glennon
10 citations
Twenty-two rats were trained to discriminate either 1.5 mg/kg of 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT) from saline in a standard two-lever operant procedure. Once responding was stable, various doses of several serotonin (5-HT) antagonists, i.e., cyproheptadine (CYP), methysergide (UML), cinanserin (CIN), and methergoline (MCE), were administered in combination with 5-OMe DMT, to assess...
Psychopharmacology
1986
R A Lyon, R A Glennon, M Titeler
3,4-Methylenedioxymethamphetamine (MDMA), 3,4-methylenedioxy-amphetamine (MDA), and their optical isomers, were assayed for their affinities at radiolabeled brain serotonin (5-HT1, 5-HT2) and dopamine (D2) binding sites. (R(-)-MDA and R(-)-MDMA displayed moderate affinities for 3H-ketanserin-labeled 5-HT2 sites (Ki = 3425 and 3310 nM, respectively) whereas the affinities for their...
Pharmacology, biochemistry, and behavior
December 1985
R A Glennon, A E Hauck
Ten rats were trained to discriminate racemic DOM (1.0 mg/kg, IP) from saline using a standard two-lever operant procedure. Once responding was stable, these animals were administered doses of lisuride and the purported 5-HT1 agonist 8-OH DPAT in tests of stimulus generalization. DOM-stimulus generalization occurred with lisuride, but not with 8-OH DPAT. These animals were also administered...
Life Sciences
December 17, 1984
Richard A Glennon, M Titeler, J D Mckenney
636 citations
The affinities (Ki values) of twenty two psycho-active agents, including LSD, 5-OMe DMT and a series of phenalkylamine derivatives, for cortical 5-HT1 and 5-HT2 binding sites were compared with two measures of behavioral activity. It was found that a significant correlation (r = 0.938) exists between the 5-HT2 binding affinities of these agents and their ED50 values as determined in tests of...
Pharmacology, biochemistry, and behavior
April 1984
R A Glennon, R Young
Rats trained to discriminate either (+)-amphetamine or (+/-)-MDA from saline in a two-lever drug discrimination task, were used to study the stimulus effects of MDA and its two optical isomers. Amphetamine-stimulus generalization occurred to S(+)-MDA, but not to its enantiomer R(-)-MDA. This, coupled with our earlier finding of DOM-stimulus generalization to R(-)-MDA but not to S(+)-MDA,...
General pharmacology
1984
R A Glennon, R Young, W Soine
Rats trained to discriminate saline from either (+)-amphetamine, (+/-)-DOM, or (+/-)-3,4-MDA in a two-lever drug discrimination paradigm were administered doses of a novel positional isomer of 3,4-MDA, i.e. 2,3-MDA. The novel isomer produced neither amphetamine-appropriate nor DOM-appropriate responding: the 3,4-MDA stimulus did, however, generalize to 2,3-MDA.
Psychopharmacology
1983
R Young, John A. Rosecrans, Richard A Glennon
25 citations
The discriminative effects of 5-methoxy-N,N-dimethyltryptamine (5-OMeDMT) were studied in rats trained to discriminate 1.5 mg/kg or 3.0 mg/kg 5-OMeDMT from saline. A series of antagonist and generalization tests revealed that (1) antagonism of the 5-OMeDMT stimulus response by the presumed serotonin antagonist BC-105 depended on the dose of 5-OMeDMT, (2) the 5-OMeDMT stimulus generalized to...
Pharmacology, biochemistry, and behavior
October 1982
Richard A Glennon, R Young
Prominent among the class of hallucinogenic phenylisopropylamines is the 2,5-dimethoxy substitution pattern; this pattern has long been recognized as being an important feature of the more potent agents within this class. The purpose of this present study was to explore the behavioral properties of a series of methoxylated phenylisopropylamines in order to determine the effect of other...
Life Sciences
June 14, 1982
R Young, John A. Rosecrans, Richard A Glennon
26 citations
Rats were trained to discriminate injections of either 5-OMe DMT (1.5 mg/kg) or LSD (0.096 mg/kg) from saline in a two-lever drug discrimination task. After stable discrimination performances were attained (greater than 85%) in each group, dose-response generalizations between the two groups of animals were examined. The results revealed that the 5-OMe DMT-stimulus response generalized to LSD...
Pharmacology, biochemistry, and behavior
April 1982
R A Glennon, R Young, J A Rosecrans
Twenty-four rats, trained to discriminate 1.0 mg/kg of (+/-)-DOM, i.e. (+/-)-2,5-dimethoxy-4-methylphenylisopropylamine, from saline under a VI-15 schedule of reinforcement, were challenged with a series of DOM homologs. The agents examined included the 4-ethyl (DOET), -propyl (DOPR), -butyl (DOBU), -tertiary butyl (DOTB) and -amyl (DOAM) derivatives as well as the R(-)- and S(+)-isomers of...
Pharmacology, biochemistry, and behavior
April 1982
R A Glennon, R Young, J A Rosecrans
Rats trained to discriminate racemic 2,5-dimethoxy-4-methylphenylisopropylamine, (+/-)-DOM (1.0 mg/kg), from saline in a two-lever drug discrimination task were challenged with the optimal isomers of DOM as well as with several related agents which represent minor molecular modifications of the DOM structure. Generalization of the (+/-)-DOM stimulus was found to occur to R(-)-DOM, S(+)-DOM,...
Life Sciences
February 1, 1982
Richard A Glennon, R Young, F Benington et al.
8 citations
Rats, trained to discriminate 1.5 mg/kg of the hallucinogenic agent 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT) from saline in a two-lever drug discrimination task, were challenged with various doses of the 4-methoxy, 4-methylthio and 5-methylthio derivatives of DMT. The 5-OMe DMT cue was found to generalize to all three of these agents; the order of potency is 5-OMe greater than 5-SMe greater...
European Journal of Pharmacology
December 17, 1981
Richard A Glennon, John A. Rosecrans, R Young
21 citations
Rats were trained to discriminate injections of 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT, 3.0 mg/kg) a hallucinogenic agent for which a serotonergic mechanism has been implicated, from saline in a two-lever drug discrimination task. After reliable levels of accuracy (greater than or equal to 85%) were attained, the ability of the 5-OMe DMT cue to generalize to 36 substituted...
Pharmacology, biochemistry, and behavior
March 1981
R A Glennon, D L Doot, R Young
Using an isolated rat fundus preparation, the 4-methyl (DOM), ethyl (DOET), propyl (DOPR) butyl (DOBU), tertiary butyl (DOTB) and amyl (DOAM) derivatives of 2,5-dimethoxy-phenylisopropylamine (2,5-DMA) were found to possess quite similar serotonin receptor affinities (pA2 - 7.02-7.22). The fundus preparation could not be used to determine pD2 values because all of the compounds were found to...
Journal of Medicinal Chemistry
November 1, 1980
Richard A Glennon, E. Schubert, John M. Jacyno et al.
33 citations
Several 7-substituted derivatives of N,N-dimethyltryptamine (DMT) were prepared and evaluated in the rat fundus serotonin receptor assay and in a behavioral (discriminative stimulus) assay in rats. Both 7-Me- and 5-OMe-7-Me-DMT possess a higher pA2, and 5,7-(OMe)2-DMT a lower pA2, than that of DMT itself. Like DMT, all three of these compounds produce behavioral effects in rats which are...
Psychopharmacology
1980
Richard A Glennon, R Young, John A. Rosecrans et al.
46 citations
A choice between two levers in an operant chamber was used to train 24 rats, under a variable-interval 15 s schedule of sweetened milk reinforcement, to discriminate a hallucinogenic (psychotomimetic) agent, 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT), from saline administration. The 5-OMe DMT stimulus generalized in a dose-related manner to each of 14 tryptamine related analogs. With the...
Journal of Medicinal Chemistry
November 1, 1979
Richard A Glennon, Peter K. Gessner, Damodar D. Godse et al.
17 citations
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....
Journal of Pharmaceutical Sciences
July 1, 1979
Richard A Glennon, Lemont B. Kier, Alexander T. Shulgin
29 citations
The hallucinogenic (psychotomimetic) potency of 10 mescaline analogs was examined by molecular connectivity analysis. Potencies could be described by a two-term relating equation, which explained 94% of the variance in activity, on the basis of structural variation, 2,5-Dimethoxy substitution as well as the nature of the 4-position substituent played an important role in determining...
Chemischer Informationsdienst
December 26, 1978
Richard A Glennon, Stephen M. Liebowitz, Elizabeth C. Mack
AbstractDie Phenalkylamine (I) und bzw. Tryptamine (II) werden auf pharmakologische Wirkung untersucht.
Journal of Medicinal Chemistry
1978
Richard A Glennon, Stephen M. Liebowitz, Elizabeth C. Mack
35 citations
Hallucinogenic phenylalkylamine and N,N-dimethyltryptamine analogues are known to affect serotonergic systems both in vivo and in vitro. Using a rat stomach fundus model, the 5-HT receptor binding affinities of several of these analogues were determined and compared. The most behaviorally potent analogues examined, DOB, DOM, and 5-methoxy-N,N-dimethyltryptamine, were found to possess rather...