Abstract
Drug and Alcohol Dependence 60 (2000) 121–132
Binding of b-carbolines and related
agents at serotonin (5-HT2
and 5-HT1A), dopamine (D2) and benzodiazepine receptors
Richard A. Glennon a,*, Malgorzata Dukat a, Brian Grella a, Seoung-Soo Hong
a,
Luca Costantino a, Milt Teitler b, Carol Smith b, Chris Egan b, Katherine
Davis b,
Mariena V. Mattson c
a Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth
Uni6ersity, Box 980540, Richmond,
VA 23298 0540, USA
b Department of Pharmacology, Albany Medical College, Albany, NY 12208, USA
c Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digesti6e
and Kidney Diseases, National Institute of Health,
Bethesda, MD 20892 -0815, USA
Received 18 July 1999; accepted 17 November 1999
Abstract
A large series of b-carbolines was examined for their ability to bind at [3H]agonist-labeled
5-HT2A serotonin receptors. Selected
b-carbolines were also examined at 5-HT2C serotonin receptors, 5-HT1A serotonin
receptors, dopamine D2 receptors, and
benzodiazepine receptors. Indolealkylamines and phenylisopropylamines were
also evaluated in some of these binding assays. The
b-carbolines were found to bind with modest affinity at 5-HT2A receptors,
and affinity was highly dependent upon the presence
of ring substituents and ring saturation. The b-carbolines displayed little
to no affinity for 5-HT1A serotonin receptors, dopamine
D2 receptors and, with the exception of b-CCM, for benzodiazepine receptors.
Examples of b-carbolines, indolealkylamines (i.e.
N,N-dimethyltryptamine analogs), and phenylisopropylamines have been previously
shown to produce common stimulus effects
in animals trained to discriminate the phenylisopropylamine hallucinogen DOM
(i.e. 1-(2,5-dimethoxy-4-methylphenyl)-2-
aminopropane) from vehicle. Although the only common receptor population that
might account for this action is 5-HT2A, on the
basis of a lack of enhanced affinity for agonist-labeled 5-HT2A receptors,
as well as on their lack of agonist action in the PI
hydrolysis assay, it is difficult to conclude that the b-carbolines behave
in a manner consistent with that of other classical
hallucinogens. © 1999 Elsevier Science Ireland Ltd. All rights reserved.
Keywords: b-carbolines; Harmaline; Harmine; Hallucinogens; Dimethyltryptamine
(DMT); 1-(2,5-Dimethoxy-4-methylphenyl)-2-aminopropane
(DOM); Serotonin receptors; Dopamine receptors; Benzodiazepine receptors;
PI hydrolysis
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