Cipralisant maleate (C09-1119-925)

Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pK i of 9.9 for histamine H3 receptor and a K i of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research.In VitroCipralisant (maleate) behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (maleate) (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant (maleate) works as a potent full histamine H3 receptor agonist. Cipralisant (maleate) increases the basal [ 35 S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC 50 , 5.6 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoCipralisant (maleate) (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg. Cipralisant (maleate) (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking. Cipralisant (maleate) promotes wakefulness in the rat. Cipralisant (maleate) 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 (maleate) does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose. Cipralisant (maleate) behaves as a partial agonist in a rat brain synaptosome model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SHR pups (35–50 g)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 ratsDosage: 10 and 30 mg/kg Administration: P.o. Result: Achieved greater brain exposure and water intake was monitored for 60 min after administration.Form:Solid. Specification: 0.99 Molecular Formula: C18H24N2O4 Molecular Weight: 332.39 PubChem CID: 6450822 Isomeric SMILES: CC(C)(C)CCC#C[C@@H]1C[C@H]1C2=CN=CN2.C(=C/C(=O)O)/C(=O)O