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Blockade of Human Atrial 5-HT4 Receptors by GR 113808

A J Kaumann

Br J Pharmacol. 1993 Nov;110(3):1172-4.

PMID: 8298805

Abstract:

1. The mode of antagonism of 5-hydroxytryptamine (5-HT)-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist GR 113808 ([1-[2-methylsulphonylamino ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate) was investigated on isolated preparations of human right atrium. 2. GR 113808 caused concentration-dependent (2-100 nM) surmountable antagonism of the effects of 5-HT with a pKB (M) of 8.8. 3. The affinity of GR 113808 for human atrial 5-HT4 receptors, together with its high selectivity for 5-HT4 receptors comprise useful properties for investigating the question of 5-HT4 receptor subtypes.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP144625514 GR 113808 GR 113808 144625-51-4 Price
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