Cipralisant (GT-2331) (Synonyms: GT-2331) |
| Catalog No.GC31269 |
Cipralisant (GT-2331) (GT-2331) est un antagoniste complet des récepteurs de l'histamine H3 À faible toxicité, puissant, sélectif et À haute affinité in vivo, et un agoniste in vitro, avec un pKi de 9,9 pour le récepteur de l'histamine H3 et un Ki de 0,47 nM pour le récepteur de l'histamine H3 de rat.
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Cas No.: 213027-19-1
Sample solution is provided at 25 µL, 10mM.
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Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.
Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pKi of 9.9[1] and a Ki of 0.47 nM for rat histamine H3 receptor[2]. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC50 of 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].
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[2].
[1]. Tedford CE, et al. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur J Pharmacol. 1998 Jun 26;351(3):307-11. [2]. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006 Jan 4;529(1-3):40-6.
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