Sigma-Aldrich Sb-269970 Hydrochloride

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

DMSO: soluble

Storage Temp.

2-8°C

Inchi

1S/C18H28N2O3S.ClH/c1-15-7-11-19(12-8-15)13-9-16-4-3-10-20(16)24(22,23)18-6-2-5-17(21)14-18;/h2,5-6,14-16,21H,3-4,7-13H2,1H3;1H/t16-;/m1./s1

Inchi Key

XQCJOYZLWFNDIO-PKLMIRHRSA-N

General Description

A selective 5-HT₇receptor antagonist. Extremely potentin vivoandin vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT₇receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT₇antagonist 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_5Areceptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT_7A, 5-HT_5Aand 5-HT_1B).

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