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Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder.
Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 13,900 | 8-10周 | |
50 mg | ¥ 18,300 | 8-10周 | |
100 mg | ¥ 23,500 | 8-10周 |
产品描述 | Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder. |
靶点活性 | H3 receptor (rat):(ki)0.47 nM, H3 receptor:(pki)9.9 |
体外活性 | Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro and potently inhibits forskolin-induced cAMP accumulation (EC50: 0.23 nM). Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50: 5.6 nM) [2]. |
体内活性 | Cipralisant (10 mg/kg, p.o.) blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake in rats [2]. |
别名 | GT-2331 |
分子量 | 216.32 |
分子式 | C14H20N2 |
CAS No. | 213027-19-1 |
密度 | 1.03g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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