SB 271046 Hydrochloride_product_DataBase

Bioactivity	SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM)[1].
Invitro	SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].
In Vivo	SB 271046 Hydrochloride (10 mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose[1]. Animal Model:
Name	SB 271046 Hydrochloride
CAS	209481-24-3
Formula	C20H23Cl2N3O3S2
Molar Mass	488.45
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Routledge C, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612.

PeptideDB