Pharmacological characterization and determination of pharmacokinetic and pharmacodynamic relationship of PF-00885706, a novel partial agonist selective for the 5-HT(4) receptor.

The pharmacological profile of PF-00885706, a selective 5-HT(4) receptor partial agonist, was investigated. PF-00885706 displayed a high binding affinity for the human 5-HT(4d) receptor with a K(i) of 3.7 nM that translates to functional agonist activity in vitro with EC(50) values of 4.

In vitro and in vivo pharmacological characterization of PF-01354082, a novel partial agonist selective for the 5-HT(4) receptor.

The pharmacological profile of PF-01354082, a selective 5-HT(4) receptor partial agonist, was investigated. PF-01354082 displayed high affinity for human 5-HT(4d) and dog 5-HT(4h) receptors in binding studies, having Ki values of 2.0 nM and 4.

Pharmacological characterization of 5-Hydroxytryptamine-receptor subtypes in circular muscle from the rat stomach.

5-Hydroxytryptamine (5-HT) modulates gastric motility and gastric emptying via a variety of 5-HT receptor subtypes. However, regional and functional differences among 5-HT receptor subtypes in the rat stomach are not fully investigated. Thus, we aimed to characterize 5-HT receptor subtypes involved in the 5-HT-induced contractions in the isolated antral, corporal and fundic circular muscles of the rat stomach by measuring the contractile force.