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GR38032F, a novel selective 5HT sub(3) receptor antagonist

The classification of 5-hydroxytryptamine (5HT) receptors into "D" and "M" types by Gaddum and Picarelli (1957) has been extended by further sub-classification. The authors report the pharmacological properties of GR38032F (1,2,3,9-tetrahydro-9-methyl-3((2-methyl-1H-imidazol-l-yl...

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Bibliographic Details
Main Authors: Brittain, R T, Butler, A, Coates, I H, tune, D H, Hagan, R, Hill, J M, Humber, D C, Humphrey, PPA, Ireland, S J
Format: Conference Proceeding
Language:English
Online Access:Get full text
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Summary:The classification of 5-hydroxytryptamine (5HT) receptors into "D" and "M" types by Gaddum and Picarelli (1957) has been extended by further sub-classification. The authors report the pharmacological properties of GR38032F (1,2,3,9-tetrahydro-9-methyl-3((2-methyl-1H-imidazol-l-yl)methyl)- 4H-carbazol-4-one, HCl.2H sub(2)0) which has potent and selective antagonist actions at 5HT sub(3) receptors. GR38032F is a potent, highly selective, competitive antagonist at 5HT sub(3)-receptors. Its selectivity of action is reflected in a wide margin of safety. GR38032F has the clinical potential for markedly improving the treatment of certain psychiatric and gastrointestinal disorders.
ISSN:0007-1188