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RS 39604 hydrochloride
Other Information:
Sold
with the permission of Roche Bioscience
Chemical Name:1-[4-Amino-5-chloro-2-(3,5-dimethoxyphenyl)methyloxy]-3
-[1-[2-methylsulphonylamino]ethyl]piperidin-4-yl]propan
-1-one hydrochloride
Biological Activity:
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 α1C receptors. The ketone group gives RS 39604 a relatively long half life;
it is also orally active and so suitable for in vivo studies.
Hegdeat al (1995) RS 39604: a potent, selective and orally
active 5-HT4 receptor antagonist. Br.J.Pharmacol. 115
1087. Eglenet al (1995) Central 5-HT4 receptors. TiPS
16 391.
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
