SB271046( —— )

Catalog No. M17426 CAS No. 209481-20-9

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Datasheet

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Product Name

SB271046
Note

Research use only, not for human use.
Brief Description

SB271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
Description

SB271046 is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
In Vitro

In functional studies on human 5-HT6 receptors SB 271046 competitively antagonized 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71.
In Vivo

SB 271046 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. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB 271046 (EC50 of 0.16?μM) and brain concentrations of 0.01-0.04?μM at Cmax.
Synonyms

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Pathway

Cell Cycle/DNA Damage
Target

GPR
Recptor

5-HT6
Research Area

——
Indication

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1. Routledge C, et al. Br J Pharmacol, 2000, 130(7), 1606-1612.

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