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Bioorg Med Chem Lett. 2000 Dec 18;10(24):2697-9.

2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.

Author information

1
Merck Sharp & Dohme Research Laboratories, Thle Neuroscience Research Centre, Harlow, Essex, UK. graeme_stevenson@merck.com

Abstract

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD2 receptors can be controlled by suitable C-2 aryl groups.

PMID:
11133071
DOI:
10.1016/s0960-894x(00)00557-6
[Indexed for MEDLINE]

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