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Chemical Name:(2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-pip
eridinyl)ethyl]pyrrolidine hydrochloride
Biological Activity:
Potent and selective 5-HT7 receptor
antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A,
5-HT5A and 5-HT1B and < 6.0 for 5-HT1A,
5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A,
5-HT2B, 5-HT2C, 5-HT4 and 5-HT6
receptors respectively). Brain penetrant in vivo.
Lovell et al (2000) A novel, potent, and selective
5-HT7 antagonist:
(R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl)pyrrolidine-1-sulfonyl)phenol
(SB-269970). J.Med.Chem. 43 342. Haganet al (2000)
Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist. Br.J.Pharmacol. 130
539. Koganet al (2002) DR4004, a putative 5-HT7 receptor antagonist, also has functional activity at
the dopamine receptor. Eur.J.Pharmacol. 449 105.
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.
