SB-616234-A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB-616234-A 是一种选择性、口服生物可利用的 5-HT1B 受体拮抗剂，具有抗焦虑和抗抑郁活性。

SB-616234-A is a selective and orally bioavailable antagonist of 5-HT1B receptor, with anxiolytic and antidepressant activity.(In Vitro):SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2). Similarly, rat and guinea pig striatal 5-HT1B receptors affinity (pKi) of 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively).(In Vivo):SB-616234-A reverses the agonist of 5-HT1/7 receptor, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively.a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors caused by SB-616234A (0.3-30 mg/kg p.o.) with an ED50 of 2.83 ± 0.39 mg/kg p.o.

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively).

SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively. SB-616234-A (0.3-30 mg/kg p.o.) causes a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED50 of 2.83 ± 0.39 mg/kg p.o.

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Endocrinology/Hormones

5-HT Receptor

Potassium channel

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908601-49-0

574.12

C32H36ClN5O3

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (17.42 mM)

Cl.COc1cc2CCN(C(=O)c3ccc(cc3)-c3ccc(cc3C)-c3noc(C)n3)c2cc1N1C[C@H](C)N[C@H](C)C1

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(-20℃)

With Ice Pack

≥ 2 years