Irdabisant (hydrochloride)

Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment[1][2].

Product Specifications

CAS Number

[1005398-61-7]

Product Name Alternative

CEP-26401 (hydrochloride)

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/irdabisant-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2.[H]Cl

Molecular Formula

C18H24ClN3O2

Molecular Weight

349.86

References & Citations

[1]Hudkins RL, et al. Discovery and characterization of 6-{4-[3- (R) -2-methylpyrrolidin-1-yl) propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant) : a potent, selective histamine H3 receptor inverse agonist. J Med Chem. 2011 Jul 14;54 (13) :4781-92.|[2]Raddatz R, et al. CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities. J Pharmacol Exp Ther. 2012 Jan;340 (1) :124-33.