Cipralisant (GT-2331) 在体内是一种具有口服活性、低毒、有效、选择性、高亲和力的histamine H3 receptor的拮抗剂，在体外是histamine H3 receptor的激动剂，对于histamine H3 receptor，其pKi为 9.9，对大鼠histamine H3 receptor的Ki为 0.47 nM。Cipralisant 有研究注意缺陷多动障碍的潜力。
| 生物活性 | Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinityhistamine H3 receptorfull antagonist in vivo, and an agonist in vitro, with apKiof 9.9 forhistamine H3 receptorand aKiof 0.47 nM for rathistamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research[1][2][3][4]. |
| IC50& Target[3][4] | H3receptor 9.9 (pKi) | rat H3receptor 0.47 nM (Ki) |
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体外研究
(In Vitro) | Cipralisant behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[3].
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体内研究
(In Vivo) | Cipralisant (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg[2].
Cipralisant (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking[3].
Cipralisant promotes wakefulness in the rat. Cipralisant potently and significantly improves performance in the repeated acquisition model, in line with its high affinity for the rat H3 receptor and good CNS penetration. Cipralisant does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose[2]. Cipralisant behaves as a partial agonist in a rat brain synaptosome model[3].
| Animal Model: | Male SHR pups (35–50 g)[2] | | Dosage: | 0.3~30 mg/kg | | Administration: | S.c. | | Result: | Significantly enhanced performance of the SHR pups in a dose-related manner at 1 mg/kg. |
| Animal Model: | Male Sprague-Dawley rats[3] | | Dosage: | 10 and 30 mg/kg | | Administration: | P.o. | | Result: | Achieved greater brain exposure and water intake was monitored for 60 min after administration. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(924.56 mM;Need ultrasonic) 配制储备液 | 1 mM | 4.6228 mL | 23.1139 mL | 46.2278 mL | | 5 mM | 0.9246 mL | 4.6228 mL | 9.2456 mL | | 10 mM | 0.4623 mL | 2.3114 mL | 4.6228 mL |
*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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
