935840-35-0
Chemical Structure
PF-03654764
- CAS No.: 935840-35-0
- Formula:C20H28F2N2O
- Molecular Weight:350.45
IUPAC Name: (1r,3r)-3-fluoro-3-(3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl)-N-isobutylcyclobutane-1-carboxamide
InChIKey: DJRDLCHHQYHQQK-UKIBZPOASA-N
SMILES: O=C([C@@H]1C[C@@](C2=CC(F)=C(CN3CCCC3)C=C2)(F)C1)NCC(C)C
Biological Activity: PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research[1][2].
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PF-03654764 | 99.0% | PF-03654764 is an orally active, selective histamine H3 receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research. | ||||||||||||||||||||
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- [1]. Travis T Wager, et al. Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem. 2011 Nov 10;54(21):7602-20. [Content Brief]
- [2]. Michelle L North, et al. Add-on histamine receptor-3 antagonist for allergic rhinitis: a double blind randomized crossover trial using the environmental exposure unit. Allergy Asthma Clin Immunol. 2014 Jul 3;10(1):33. [Content Brief]
Keywords
