213027-19-1
物理化學(xué)性質(zhì)
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pKi: 9.9 (Histamine H3 receptor)
Ki: 0.47 nM (Rat histamine H3 receptor)
Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pK i of 9.9 and a K i of 0.47 nM for rat histamine H3 receptor. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC 50 of 0.23 nM. Cipralisant increases the basal [ 35 S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC 50 , 5.6 nM).
Cipralisant (GT-2331) acts as an antagonist of histamine H3 receptor, and blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake at 10 mg/kg via oral administration in rats.