PF-03654764

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].

Product Specifications

CAS Number

[935840-35-0]

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/pf-03654764.html

Purity

99.0

Solubility

10 mM in DMSO

Smiles

O=C([C@@H]1C[C@@](C2=CC(F)=C(CN3CCCC3)C=C2)(F)C1)NCC(C)C

Molecular Formula

C20H28F2N2O

Molecular Weight

350.45

References & Citations

[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.|[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.