| Name | Darifenacin hydrobromide |
| Description | Darifenacin hydrobromide (UK-88525) is a selective muscarinic receptor antagonist used to treat urinary incontinence and overactive bladder syndrome. |
| In vitro | Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat. [1] Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6?μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6. [2] |
| In vivo | Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55%. [1] Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers. [3] Darifenacin (7.5 mg and 15 mg, daily) reduces the number of incontinence episodes per week from baseline by 67.7% and 72.8% respectively compared with 55.9% with placebo in patients with overactive bladder (OAB). Darifenacin (7.5 mg and 15 mg, daily) also shows significantly superior to placebo for improvements in micturition frequency, bladder capacity, frequency of urgency, severity of urgency and number of incontinence episodes leading to a change in clothing or pads in patients with overactive bladder (OAB). [4] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.53 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (183.99 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | UK88525 | UK 88525 | Muscarinic acetylcholine receptor | mAChR | M3 mAChR | Inhibitor | inhibit | Darifenacin hydrobromide | Darifenacin Hydrobromide | Darifenacin |
| Inhibitors Related | Adiphenine hydrochloride | Nanofin | Forskolin | Pilocarpine Hydrochloride | Clozapine N-Oxide | Pilocarpine nitrate | Urethane | Ribavirin | D-Menthol | Amitriptyline hydrochloride | Choline chloride | Propoxur |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Failed Clinical Trials Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Approved Drug Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Bioactive Compounds Library Max |
United States
