SB-269970 hydrochloride

• CAT Number: I002897
• CAS Number: 261901-57-9
• Molecular Formula: C18H28N2O3S • HCl
• Molecular Weight: 389
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: 3 years -20C powder
• IC50: 8.3 (pKi for 5-HT7)
• InChIKey: XQCJOYZLWFNDIO-PKLMIRHRSA-N

SB269970 HCl (CAT: I002897) is a potent antagonist of the 5-HT7A receptor with a pKi value of 8.9. It exhibits more than 50-fold binding selectivity over the 5-HT5A receptor and more than 250-fold selectivity over the 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors. Additionally, it has been shown to block adrenergic α2 receptors in guinea pig vas deferens. SB-269970 has been employed to target the 5-HT7 receptor in the investigation of cognitive deficits resembling those seen in schizophrenia.

Reference

[1]. http://www.ncbi.nlm.nih.gov/pubmed/10821781
[2]. Roberts C, et al. The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies. Br J Pharmacol. 2001 Apr;132(7):1574-80.
[3]. Roberts C, et al. The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies. Br J Pharmacol. 2001 Apr;132(7):1574-80.
[4]. Monti JM, et al. The serotonin 5-HT7 receptor agonist LP-44 microinjected into the dorsal raphe nucleus suppresses REM sleep in the rat. Behav Brain Res. 2008 Aug 22;191(2):184-9.