SB-616234-A is a selective and orally bioavailable5-HT1B receptorantagonist, with anxiolytic and antidepressant activity.

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pK_i8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pK_i6.6 ± 0.1). Similarly, affinity (pK_i) 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 pA₂value 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 pK_Bof 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)^[2].

SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED₅₀of 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 ED₅₀of 1.0 and 3.3 mg/kg i.p., respectively^[1]. 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 ED₅₀of 2.83 ± 0.39 mg/kg p.o^[1].

574.11

Solid

C₃₂H₃₆ClN₅O₃

908601-49-0

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 10 mg/mL(17.42 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。