Datasheet Inhibitors / / Screening Libraries A DRUG SCREENING EXPERT

Product Name : Cipralisant Catalog Number : T14970 CAS Number : 213027-19-1 Molecular Formula : C14H20N2 Molecular Weight : 216.32

Description: Cipralisant is a selective H3 in vivo, and an in vitro (pKi: 9.9 for ; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder.

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

Histamine H3 receptor （pki）9.9 Receptor (IC50) Rat histamine H3 receptor （ki）0.47 nM

In vitro Activity 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]. In vivo Activity Cipralisant (10 mg/kg, p.o.) blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake in rats [2].

Reference 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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