Darifenacin - CAS 133099-04-4
Catalog number: 133099-04-4
Category: Inhibitor
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Darifenacin hydrobromide is an antispasmodic muscarinic antagonist, selective for blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. Darifenacin hydrobromide has 9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4. Darifenacin is used clinically to treat urinary incontinence and overactive bladder syndrome.
UK-88525; UK 88525; UK88525
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1. Synthesis and Properties of Molecular Imprints of Darifenacin: The Potential of Molecular Imprinting for Bioanalysis
R. E Verm*, R. J. Goody. Chromatographia Vol. 50, No. 7/8, October 1999
A molecularly imprinted polymer has been developed which subsequently demonstrated an ability to selectively retain darifenacin (UK-88,525-S) from aqueous acetonitrile when used as a stationary phase in HPLC columns and as a packing in solid-phase extraction cartridges. The imprinted polymer is applicable to a wide range of analytical methods including extraction from plasma, purification ofradiolabelled UK-88,525, chiral separations and separation of metabolites and structural analogues. The polymer is able to extract darifenacin directly from a protein-precipitated human plasma/acetonitrile (1:1 v/v) mixture with 100 % recovery. The imprinted polymer can also effect a repurification of 14C-labelled darifenacin.
2. Dose response with darifenacin, a novel once-daily M3 selective receptor antagonist for the treatment of overactive bladder: results of a fixed dose study
Simon Hill, Vik Khullar, Jean-Jacques Wyndaele, Karine Lheritier. Int Urogynecol J (2006) 17: 239–247
Darifenacin is a novel agent that shows high selectivity for human muscarinic M3 receptors in vitro. Preliminary studies have confirmed that darifenacin has aclinical profile consistentwith its M3 selective andM1- and M2-sparing properties as it conveys pronounced urodynamic efficacy with no evidence of cognitive impairment or cardiac effects. The aim of the present study was to further evaluate the efficacy, tolerability, and safety of varying doses of darifenacin in patients with OAB.
3. Time-to-effect with darifenacin in overactive bladder: a pooled analysis
Vik Khullar & Jenelle Foote & Yodit Seifu & Mathias Egermark. Int Urogynecol J (2011) 22:1573–1580
Clinical studies with darifenacin, a highly selective M3-receptor antagonist, have demonstrated its efficacy and safety in patients with OAB during 12 weeks of treatment and in long-term use. Pooled efficacy data from three phase III studies have been published for week 12, whereas this analysis specifically evaluates efficacy data for the earlier study visits of weeks 2 and 6. In addition, a retrospective analysis was performed to examine data from the earliest available timepoints of these studies to determine when the drug effect first becomes apparent for the two available doses of darifenacin (7.5 and 15 mg). The improvements observed at week 2 were then calculated as percentages of the final treatment effect observed at the end of the study to describe the progress of treatment effect over time.
4. Darifenacin
A Viewpoint by Francois Haab. Drugs Aging 2004; 21 (13): 893-894
As predicted by its M3 selectivity, darifenacin appears to be well tolerated, with cardiovascular and nervous system event rates similar to placebo; this is also the case for the incidence of blurred vision. Dry mouth still occurs with darifenacin, although at a lower incidence than with oxybutynin. Notably, the drug has no cognitive function effects in elderly patients; these data appear to be the first of their kind amongst the antimuscarinics. This safety profile, together with strong clinical efficacy, positions darifenacin as a valuable treatment for the symptoms of overactive bladder. Whether this profile translates into significant clinical advantages will hopefully become clear following the longer-term use of darifenacin in general practice.
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CAS 133099-04-4 Darifenacin

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