Synthesis and serotonin receptor binding properties of 5-substituted 3-(1′,2′,5′,6′-tetrahydropyridin-3′-yl) indoles |
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Authors: | T. Dahlgren R. L. Dean L. A. Gharat A. M. Johansson G. Lambert H. B. Li D. L. Nelson Y. Yang A. R. Martin |
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Affiliation: | Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ 85721, U.S.A. |
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Abstract: | A semi-rigid 5-hydroxytryptamine (5-HT) analogue, RU28253 [5-methoxy-3-(1′,2′,5′,6′-tetrahydropyridin-3′-yl) indole], is a potent 5-HT1 and 5-HT2 agonist. It is isomeric to RU24969 [5-methoxy-3-(1′,2′,5′,6′-tetrahydropyridin-4′-yl) indole], a conformationally restricted 5-HT homologue, which has been extensively used in the study and classification of 5-HT receptors. A series of RU28253 derivatives with diverse substituents on indole 5-position were synthesized and their dissociation constants determined at the 5-HT1 and 5-HT2 receptors. |
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