SB-269970 Hydrochloride

A selective 5-HT₇ receptor antagonist. Extremely potent in vivo and in vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT₇ receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT₇ antagonist in animal models. SB-269970 is an analogue of SB-258719 and has been shown to have at least 100 fold selectivity versus all other 5-HT receptor subtypes except the human 5-HT_5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT_7A, 5-HT_5A and 5-HT_1B).

Primary Target
5-HT₇

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Tokarski, K. et al. 2012. Pharmacol. Rep.64, 256.
Thomas. D. R. et al. 2000. Br. J. Pharmacol.130, 409.
Lovell, P. J. et al. 2000. J. Med. Chem.43, 342.

Forbes, I. T. et al. 1998. J. Med. Chem.41, 655.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)