sb 242084 dihydrochloride hydrate

SB 242084 是5-HT2C 选择性抑制剂，pKi 值9.0，是一种精神活性药物和研究化学品。

Pramipexole dihydrochloride hydrate (Mirapex) 是选择性的，具有血脑屏障 (BBB) 渗透性的 D2 型多巴胺受体激动剂，对 D2 型受体、D2、D3、D4亚型受体的 Ki 分别为 2.2 nM、3.9 nM、0.5 nM、1.3 nM，可用于研究帕金森综合症和腿多动综合征。

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

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 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].

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. in vivo: Mean change

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).

Quinacrine is a compound that is commonly used as an anti-protozoal agent. It inhibits voltage-dependent sodium channels (IC50: 3.3 μM） and suppresses aldehyde oxidase (IC50: 3.3 μM). Quinacrine prevents misfolding of prion protein (EC50: 0.3 μM). As an e

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).

BMS-433771 dihydrochloride hydrate 是一种有效的呼吸道合胞病毒 (RSV) 抑制剂，具有口服活性。BMS-433771 dihydrochloride hydrate 对 A 组和 B 组RSV 均有效，EC50均值为 20 nM。BMS-433771 dihydrochloride hydrate 可用于呼吸道疾病的研究。

Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) 是一种长效的钙离子通道拮抗剂。Mibefradil dihydrochloride hydrate 通过对低电压激活 (T) 钙通道的亲和力高于对高电压激活 (L) 钙通道的亲和力来发挥作用。Mibefradil dihydrochloride hydrate 能够降压药。

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

Cefotiam (SCE-963) dihydrochloride hydrate，一种肠外头孢菌素类抗生素，对革兰氏阳性菌和革兰氏阴性菌展示出广谱活性。

Nitracrine (dihydrochloride hydrate) 抑制RNA合成，通过共价且可逆地结合DNA，在体内形成共价加合物。作为1-nitroacridine衍生物，这种化合物显示出有效的缺氧选择性活性和抗肿瘤作用，同时具有显著的细胞毒性。