133099-04-4 Usage
Description
Darifenacin is a novel muscarinic M3 selective antagonist used for the once-daily oral treatment of urinary incontinence and overactive bladder. It has a higher level of M3 selectivity than previously marketed antimuscarinic agents, making it more effective in treating overactive bladder symptoms.
Uses
Used in Pharmaceutical Industry:
Darifenacin is used as a medication for the treatment of overactive bladder. It works by blocking the muscarinic M3 receptors in the bladder, which are primarily responsible for bladder muscle contractions. This helps to reduce the symptoms of urinary incontinence and overactive bladder.
Used in Urology:
Darifenacin is used as a therapeutic agent for patients suffering from overactive bladder. Its high selectivity for M3 receptors makes it a more effective treatment option compared to other muscarinic agents, providing better control over bladder contractions and reducing the frequency of urination.
Brand Names:
Enablex (Novartis) and Emselex.
Originator
Pfizer (US)
Clinical Use
Symptomatic treatment of urinary incontinence,frequency or urgency
Drug interactions
Potentially hazardous interactions with other drugsAnti-arrhythmics: increased risk of antimuscarinic
side effects with disopyramideAntifungals: concentration increased by ketoconazole
- avoid; avoid with itraconazole.Antivirals: avoid with fosamprenavir, atazanavir,
indinavir, lopinavir, ritonavir, saquinavir and
tipranavir.Calcium-channel blockers: avoid with verapamilCiclosporin: avoid concomitant use.
Metabolism
After an oral dose, darifenacin is subject to extensive
first-pass metabolism and has a bioavailability of about
15-19%. Darifenacin is metabolised in the liver by the
cytochrome P450 isoenzymes CYP2D6 and CYP3A4.
Most of a dose is excreted as metabolites in the urine and
faeces.
Check Digit Verification of cas no
The CAS Registry Mumber 133099-04-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,0,9 and 9 respectively; the second part has 2 digits, 0 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 133099-04:
(8*1)+(7*3)+(6*3)+(5*0)+(4*9)+(3*9)+(2*0)+(1*4)=114
114 % 10 = 4
So 133099-04-4 is a valid CAS Registry Number.
InChI:InChI=1/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1
133099-04-4Relevant articles and documents
Synthesis of Arylethylamines via C(sp3)-C(sp3) Palladium-Catalyzed Cross-Coupling
Lippa, Rhys A.,Battersby, David J.,Murphy, John A.,Barrett, Tim N.
, p. 3583 - 3604 (2021/02/27)
Substituted arylethylamines represent a key structural motif in natural, pharmaceutical, and agrochemical compounds. Access to such scaffolds has been the subject of long-standing synthetic interest. Herein, we report the synthesis of such scaffolds via a palladium-catalyzed C(sp3)-C(sp3) coupling between (chloromethyl)aryls and air-/moisture-stable N,N-dialkylaminomethyltrifluoroborate salts. Rapid hit identification was achieved using microscale high-throughput experimentation and was followed by millimolar-scale reaction parameter optimization. A range of structurally and electronically varied arylethylamine products were obtained in moderate to excellent yields (27-96%, >60 examples). The reaction mechanism is proposed to proceed via formation of a trialkylbenzylammonium species prior to oxidative addition.
Novel Polymorphs of Darifenacin Free Base and its Hydrobromide Salt
-
Page/Page column 7, (2010/08/18)
The present invention provides a novel and stable amorphous form of darifenacin free base, process for preparation, pharmaceutical compositions, and method of treating thereof. The present invention further provides a novel and stable polymorphic form of darifenacin hydrobromide, process for preparation, pharmaceutical compositions, and method of treating thereof.
NOVEL PROCESS FOR THE PREPARATION OF (3SM-[2-(2 J-DIHYDRO-5- BENZOFURANYL?ETHYL]-α.α -DIPHENYL-3-PYRROLIDINEACETAMIDE HYDROBROMIDE
-
, (2009/11/29)
The present invention is directed to a novel, industrially viable and cost effective process for manufacturing (3 S)- 1 -[2-(2,3-Dihydro-5-benzofuranyl)ethyl]-a,a-diphenyl-3-pyrrolidineacetamide hydrobromide also known as Darifenacin hydrobromide.