1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3-[[1-[2-methylsulphonylamino]ethyl]piperidin-4-yl]propan-1-one hydrochloride

Uses

RS 39604 Hydrochloride is a potent, selective and orally active 5-HT4 receptor antagonist.

Definition

ChEBI: RS 39604 hydrochloride is a hydrochloride salt obtained by mixing equimolar amounts of RS 39604 with hydrochloric acid. 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 and D1, D2, M1, M2, AT1, B1 and alpha1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies. It has a role as a serotonergic antagonist. It contains a RS 39604(1+).

Biological Activity

A potent and selective 5-HT 4 antagonist, with a pK i of 9.1 at 5-HT 4 receptors in guinea pig striatal membranes and greater than 1000-fold selectivity over 5-HT 1A, 2C, 3 and D 1 , D 2 , M 1 , M 2 , AT 1, B 1 and α 1C receptors. The ketone group gives RS 39604 a relatively long half life; it is also orally active and so suitable for in vivo studies.

IC 50

5-HT₄ Receptor: 9.1 (pKi)

storage

Store at RT