SB-224289 hydrochloride 是一种选择性的 5-HT1B receptor 拮抗剂，具有抗焦虑作用。

SB-224289 hydrochloride is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.

SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay.SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A[1]. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist(pEC50 of 7.9±0.1). SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices[3].

SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus[3].

180084-26-8

C32H33ClN4O3

557.08

SB-224289A

DMSO:8.1mg/mL (14.5mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years