Biochem/physiol Actions

Primary Target5-HT₇

General description

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).

Legal Information

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

Other Notes

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

Packaging

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)