Cipralisant
Names
Biological Activity
[Description]:
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.
[Related Catalog]:
[Target]
pKi: 9.9 (Histamine H3 receptor)[1] Ki: 0.47 nM (Rat histamine H3 receptor)[2]
[In Vitro]
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].
[In Vivo]
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].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.03g/cm3
[ Boiling Point ]:
386.7ºC at 760 mmHg
[ Molecular Formula ]:
C14H20N2
[ Molecular Weight ]:
216.32200
[ Flash Point ]:
188.5ºC
[ Exact Mass ]:
216.16300
[ PSA ]:
28.68000
[ LogP ]:
3.34290
[ Vapour Pressure ]:
7.72E-06mmHg at 25°C
[ Index of Refraction ]:
1.536