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抑制剂描述:

产品名称:Iodopravadoline(AM-630)

产品别名:见爱必信官网

英文别名:Iodopravadoline(AM-630)

靶点:Cannabinoid Receptor

CAS:164178-33-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

AM630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 μM and 31.2 nM, respectively.

溶解性:DMSO : 50 mg/mL (99.14 mM)

体外研究:

The AM251 and AM630-evoked Ca2+?influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC50 for AM251 and AM630 are 7.37 μM and 15.6 μM, respectively. AM251 and AM630 activate TRPA1 in TG sensory neurons. AM630 is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). AM251 and AM630 activation of TRPA1 is modulated by TRPV1. AM630 (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. AM630 (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner. AM630 (1 μM) blocks the CP-55,940 dose response with EC50 of 170 nM at human and EC50 of 110 nM at rat cannabinoid CB2 receptor.

体内研究:AM630 (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box compared with vehicle group. AM630 increases anxiety since the time spent in the light box is reduced compared with its corresponding control group. AM630 (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used.?

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