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PF-03654746 

Cat. No. M30935
PF-03654746  Structure
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Biological Activity

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. PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD).

Chemical Information
Molecular Weight 322.39
Formula C18H24F2N2O
CAS Number 935840-31-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xueqian Peng, et al. Nat Commun. Structural basis for recognition of antihistamine drug by human histamine receptor

[2] Aarti Sawant-Basak, et al. Xenobiotica. Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy

[3] Jean-Dominique Gallezot, et al. J Cereb Blood Flow Metab. Determination of receptor occupancy in the presence of mass dose: [11C]GSK189254 PET imaging of histamine H3 receptor occupancy by PF-03654746

[4] Jeffrey R Stokes, et al. J Allergy Clin Immunol. The effects of an H3 receptor antagonist (PF-03654746) with fexofenadine on reducing allergic rhinitis symptoms

[5] Travis T Wager, et al. J Med Chem. 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)cyclobuta䲧癐Ỵ癑㧀癏羹瘸盋

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Keywords: PF-03654746  supplier, Histamine Receptor, inhibitors, activators

 
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