| Identification | Back Directory | [Name]
PF-03654764 | [CAS]
935840-35-0 | [Synonyms]
PF-03654764
Cyclobutanecarboxamide, 3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]-N-(2-methylpropyl)-, trans- | [Molecular Formula]
C20H28F2N2O | [MDL Number]
MFCD32701918 | [MOL File]
935840-35-0.mol | [Molecular Weight]
350.45 |
| Chemical Properties | Back Directory | [Boiling point ]
478.1±45.0 °C(Predicted) | [density ]
1.15±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
15.91±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
PF-03654764 (10 mL/kg; oral; 14 days) has a Cmax of 8057 ng/mL and an AUC0-24 of 67400 ng h/mL in Sprague-Dawley rats[1].
PF-03654764 (1 mL/kg; oral; 7 days) has a Cmax of 6302 ng/mL and an AUC0-24 of 18175 ng h/mL in beagle dogs[1].
| [IC 50]
human H3 receptor: 1.2 nM (Ki); rat H3 receptor: 7.9 nM (Ki); human H3 receptor: 8.98 (pKi); rat H3 receptor: 8.10 (pKi) | [References]
[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. DOI:10.1021/jm200939b
[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. DOI:10.1186/1710-1492-10-33 |
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