A potent and selective 5-HT4
antagonist, with a pKi
of 9.1 at 5-HT4
receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT1A, 2C, 3
receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo
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RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.
Central 5-HT4 receptors
Eglen et al.
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