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-HT5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B).
Biochem/physiol Actions
Primary Target
5-HT₇
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Forbes, I. T. et al. 1998. J. Med. Chem.41, 655.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51294909
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5064150001
