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抑制剂描述:

产品名称:Capsazepine

产品别名:见爱必信官网

英文别名:Capsazepine

靶点:TRP Channel

CAS:138977-28-3

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:

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

溶解性:DMSO : ≥ 50 mg/mL (132.66 mM)

体外研究:

Capsazepine(CPZ) at a concentration of 94.2 μg/ml (IC50 concentration of capsazepine) exhibits a statistically significant inhibition of osteoclast growth and proliferation. Capsazepine converts the NKA into Na-ATPase. CPZ inhibits K+-dependent activity but allows Na-ATPase associated with Na+ transport. CPZ has no effect on Na-ATPase measured in the absence of K+. CPZ also inhibits para-nitrophenyl phosphatase activity, albeit with a lower affinity. CPZ strongly reduces the steady-state EP level and the Na+ affinity for phosphorylation decreased 3-fold after CPZ treatment. In summary, CPZ blocks an Na+/K+ cycle in the NKA but leaves an Na+ cycle intact, reducing the transport stoichiometry of the pump. Capsazepine inhibits osteoclast formation and bone resorption in a dose dependent manner in bone marrow-osteoblast co-cultures and RANKL generated osteoclast cultures. Capsazepine also suppresses RANKL induced IκB and ERK1/2 phosphorylation and causes apoptosis of mature osteoclasts and also inhibits alkaline phosphatase activity and bone nodule formation in calvarial osteoblast cultures.

体内研究:In mice, the TRPV1 antagonist capsazepine blocks morphine tolerance and dependence in mice. Acute capsazepine treatment (5 mg/kg, i.p.) potentiates the antinociceptive effects of morphine, as measured by the hot-plate test. Repeated co-treatment of capsazepine (2.5 mg/kg, i.p.) with morphine attenuates the development of tolerance to the antinociceptive effect of morphine. The development of morphine dependence is also reduced by capsazepine (1.25 or 2.5 mg/kg, i.p.). Capsazepine (1 mg/kg/day) inhibits ovariectomy induced bone loss in mice and histomorphometric analysis shows inhibitory effects on indices of bone resorption and bone formation.

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