Blockade of human atrial 5-HT4 receptors by GR 113808.
Br J Pharmacol
; 110(3): 1172-4, 1993 Nov.
Article
em En
| MEDLINE
| ID: mdl-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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antagonistas da Serotonina
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Sulfonamidas
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Coração
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Indóis
Limite:
Adult
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Aged
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Female
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Humans
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Male
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Middle aged
Idioma:
En
Ano de publicação:
1993
Tipo de documento:
Article