Afacifenacin

Modify Date: 2024-07-06 14:00:02

Afacifenacin Structure
Afacifenacin structure
Common Name Afacifenacin
CAS Number 877606-63-8 Molecular Weight 481.50900
Density N/A Boiling Point N/A
Molecular Formula C27H26F3N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Afacifenacin


Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB)[1][2].

 Names

Name (4S)-4-phenyl-3-[1-[[3-(trifluoromethoxy)phenyl]methyl]piperidin-4-yl]-1,4-dihydroquinazolin-2-one
Synonym More Synonyms

 Afacifenacin Biological Activity

Description Afacifenacin (SMP-986) is a potent and orally active muscarinic receptor antagonist. Afacifenacin inhibits the bladder afferent pathway through the sodium-channel blockade, increasing volume, and reducing the frequency of urination and incontinence. Afacifenacin has the potential for the research of overactive bladder (OAB)[1][2].
Related Catalog
In Vivo Afacifenacin (0.3, 1, 3 mg/kg; Intragastric administration) 显着增加脑梗死大鼠的膀胱容量和降低排尿压力 (MP)[2]。 Animal Model: Male Sprague-Dawley rats (cerebral infarction model)[2] Dosage: 0.3, 1, 3 mg/kg Administration: Intragastric administration Result: Significantly increased bladder capaticy and reduced micturition pressure (MP) without affecting residual urinary volume (RUV).
References

[1]. Yeo EK, et al. New therapies in the treatment of overactive bladder. Expert Opin Emerg Drugs. 2013 Sep;18(3):319-37.  

[2]. Natsuko Goto, et al. Dual inhibition of Na+-channel and muscarinic receptor by SMP-986 efficiently improved voiding function compared to anti-muscarinic agents in two conscious rat models of detrusor overactivity. The Journal of Urology. 2008, 179, 129.

 Chemical & Physical Properties

Molecular Formula C27H26F3N3O2
Molecular Weight 481.50900
Exact Mass 481.19800
PSA 48.30000
LogP 5.51170

 Synonyms

UNII-XQU62QZ74P
Afacifenacin