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

G I Stevenson; A L Smith; S Lewis; S G Michie; J G Neduvelil; S Patel; R Marwood; S Patel; J L Castro

doi:10.1016/s0960-894x(00)00557-6

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

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2697-9. doi: 10.1016/s0960-894x(00)00557-6.

Authors

G I Stevenson¹, A L Smith, S Lewis, S G Michie, J G Neduvelil, S Patel, R Marwood, S Patel, J L Castro

Affiliation

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

PMID: 11133071
DOI: 10.1016/s0960-894x(00)00557-6

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.

MeSH terms

Animals
Binding, Competitive
Humans
Rats
Receptors, Dopamine D2 / metabolism
Receptors, Serotonin / metabolism
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / pharmacology
Structure-Activity Relationship
Tryptamines / chemical synthesis
Tryptamines / pharmacology*

Substances

Receptors, Dopamine D2
Receptors, Serotonin
Serotonin Antagonists
Tryptamines