PF-03654746

PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis[1]. PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) [2].

Product Specifications

CAS Number

[935840-31-6]

UNSPSC

12352005

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Inflammation/Immunology; Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/pf-03654746.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C18H24F2N2O

Molecular Weight

322.39

References & Citations

[1]Stokes JR, et al. The effects of an H3 receptor antagonist (PF-03654746) with fexofenadine on reducing allergic rhinitis symptoms. J Allergy Clin Immunol. 2012 Feb;129 (2) :409-12, 412.e1-2.|[2]Brioni JD, et al. Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. J Pharmacol Exp Ther. 2011 Jan;336 (1) :38-46.