sb-277011 dihydrochloride

SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).

SB 699551 dihydrochloride 是一种5-ht5a 受体拮抗剂。

SB-277011 (SB-277011A) 是多巴胺 D3 受体的特异性拮抗剂，对 D3 受体、D2 受体、5-HT1D 和 5-HT1B 的 pKi 值分别为 8.0、6.0、5.0 和 <5.2。

SB-747651A dihydrochloride是一种与ATP竞争性相互作用的抑制剂，特别针对丝裂原和应激激活激酶1 (MSK1)，IC50值为11 nM。此化合物还能抑制PRK2、RSK1、p70S6K和ROCK-II等酶的活性。因其对上述激酶的抑制作用，SB-747651A dihydrochloride在炎症研究中显示出潜力。

SB-277011 hydrochloride (SB-277011A hydrochloride) 是一种可口服且具有选择性、强效性和脑渗透性的多巴胺 D3 受体(D3R) 拮抗剂，在大鼠中诱导的射精延迟。SB-277011 hydrochloride 可用于研究神经系统疾病。

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg kg i.p., and 2.0 mg kg p.o. SB 242084 (0.1-1 mg kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor).

SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively).