1005398-61-7
Chemical Structure
Irdabisant hydrochloride
Synonym(s): CEP-26401 hydrochloride
- CAS No.: 1005398-61-7
- Formula:C18H24ClN3O2
- Molecular Weight:349.86
IUPAC Name: (R)-6-(4-(3-(2-methylpyrrolidin-1-yl)propoxy)phenyl)pyridazin-3(2H)-one hydrochloride
InChIKey: WJUJICMNSMPLLG-PFEQFJNWSA-N
SMILES: C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2.[H]Cl
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
