DarifenacinM3 receptor antagonist and antimuscarinic agents CAS# 133099-04-4 |
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Quality Control & MSDS
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| Cas No. | 133099-04-4 | SDF | Download SDF |
| PubChem ID | 72054 | Appearance | Powder |
| Formula | C28H30N2O2 | M.Wt | 426.55 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | UK-88525 | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | 2-[1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide | ||
| SMILES | C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5 | ||
| Standard InChIKey | HXGBXQDTNZMWGS-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.
IC50 value: 8.9 (pKi) [1]
Target: M3 receptor
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]. References: | |||||
Darifenacin Dilution Calculator
Darifenacin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3444 mL | 11.722 mL | 23.4439 mL | 46.8878 mL | 58.6098 mL |
| 5 mM | 0.4689 mL | 2.3444 mL | 4.6888 mL | 9.3776 mL | 11.722 mL |
| 10 mM | 0.2344 mL | 1.1722 mL | 2.3444 mL | 4.6888 mL | 5.861 mL |
| 50 mM | 0.0469 mL | 0.2344 mL | 0.4689 mL | 0.9378 mL | 1.1722 mL |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2344 mL | 0.4689 mL | 0.5861 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Darifenacin is a selectivity M3 receptor antagonist and newer antimuscarinic agents. Darifenacin is indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency and frequency in adults.
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'Tamsulosin and Darifenacin' Versus 'Tamsulosin Monotherapy' for 'BPH with Accompanying Overactive Bladder'.[Pubmed:26266159]
J Clin Diagn Res. 2015 Jun;9(6):PC08-11.
PURPOSE: To evaluate the efficacy/safety of 'tamsulosin and Darifenacin' (TD) vs. 'tamsulosin and placebo' (TP) for patients with symptomatic benign prostrate hyperplasia (BPH) with accompanying overactive bladder (OAB) symptoms. MATERIALS AND METHODS: This study included symptomatic patients of BPH with one or more of the following OAB symptoms; micturition frequency >8, nocturnal frequency > 2, urgency > 1 per 24 hour between November 2012 and February 2014. After protocol approval by ethics committee and obtaining informed consent, patients were randomly assigned to receive tamsulosin 0.4mg plus placebo (TP) (n=30) or tamsulosin 0.4 mg plus Darifenacin 7.5 mg (TD) (n=30) for 8 weeks. The mean change from baseline in urinary frequency and incontinence episodes/24 hour (primary end points), and nocturnal frequency; mean change in PVR and changes in IPSS (secondary end points) were compared between groups at 0/eight week using voiding diary and ultrasonography. RESULTS: The mean change in frequency, incontinence, nocturnal frequency/24 hour and IPSS (International prostrate symptom score) were (-4.83 vs. -3.93, p=0.023), (-1.50 vs. 1.08, p=0.001), (-2.20 vs. -1.87, p<0.001) and (-7.90 vs. -6.27, p<0.001) in the TD/TP group respectively (significant). Apart from some minor side effects (12 vs. 9) all interventions appeared to be safe and well tolerated. The mean change in the PVR (Postvoid residual) was marginal (+10.84ml and -16.93) and the incidence of urinary retention was 13% and 3% in the TD and TP groups respectively (p=0.35). CONCLUSION: Treatment with tamsulosin and Darifenacin for 8 weeks is an effective and safe treatment modality in select patients of BPH with accompanying OAB symptoms.
Treatment of Overactive Bladder in the Elderly Female: The Case for Trospium, Oxybutynin, Fesoterodine and Darifenacin.[Pubmed:26391900]
Drugs Aging. 2015 Oct;32(10):809-19.
Overactive bladder (OAB) is a common constellation of lower urinary tract storage symptoms that causes a significant impact on a person's quality of life. The elderly may be disproportionally impacted by these symptoms due to concomitant poor mobility, comorbid conditions such as diabetes and heart failure, and polypharmacy. While behavioral modification and pelvic floor muscle training should be considered first-line treatment options, pharmacotherapy remains the backbone of the therapeutic regimen. Trospium, oxybutynin, fesoterodine, and Darifenacin all have unique properties that may confer certain advantages in the elderly population. The hydrophilicity and quaternary amine structure of trospium may limit its ability to cross the blood-brain barrier and thus minimize impact on cognition in the elderly. In its oral form, oxybutynin may have the most significant effect on cognition; however, the transdermal preparations may be favorable in the elderly population due to the ability to avoid first-pass metabolism and its limited antimuscarinic adverse effects. Fesoterodine may be the most extensively studied OAB medication in the elderly population. Darifenacin has a strong affinity for the M3 receptor in the bladder, while having a weak affinity for the M1 receptor commonly found in the brain. It must be noted that all muscarinic receptor antagonists are associated with common adverse effects to some degree, and frequent re-evaluation of the elderly patient is necessary to confirm the proper benefit-to-risk profile.
An evaluation of the efficacy of solifenacin and darifenacin for prevention of catheter related bladder discomfort: a prospective, randomized, placebo controlled, double blind study.[Pubmed:27188787]
Minerva Anestesiol. 2016 May 18. pii: R02Y9999N00A16051801.
BACKGROUND: Urinary catheterization during surgical interventions causes postoperative catheter related bladder discomfort (CRBD). Antimuscarinic agents are the mainstay of treatment for overactive bladder (OAB). As the symptoms of CRBD mimic to OAB, so we designed this study to assess the efficacy of solifenacin and Darifenacin for prevention of CRBD. METHODS: Ninety patients of either sex undergoing elective spine surgery and requiring urinary catheterization were randomly assigned into three groups to receive oral solifenacin 5 mg (Group S), Darifenacin 7.5 mg (Group D) and placebo (Group C) 1 hour prior to induction of anesthesia. Anesthesia technique was identical in all the groups. Catheter related bladder discomfort (CRBD) was evaluated in 4-point scale (1 = no discomfort, 2 = mild, 3 = moderate, 4 = severe), on arrival (0 hour) and at 1, 2, and 6 hours postoperatively. Patients were provided patient-controlled analgesia with fentanyl for postoperative pain relief. RESULTS: There were no significant differences in demographic profile and fentanyl requirements (P >0.05). The prevalence and severity of CRBD were significantly less in the group D and group S compared with the group C at all time intervals (P <0.05). CONCLUSION: Pretreatment with oral solifenacin or Darifenacin reduces catheter-related bladder discomfort with no clinically relevant significant side effects.
Evaluation of the efficacy of solifenacin and darifenacin for prevention of catheter-related bladder discomfort: a prospective, randomized, placebo-controlled, double-blind study.[Pubmed:27607187]
Minerva Anestesiol. 2016 Aug;82(8):867-73.
BACKGROUND: Urinary catheterization during surgical interventions causes postoperative catheter-related bladder discomfort (CRBD). Antimuscarinic agents are the mainstay of treatment for overactive bladder (OAB). As the symptoms of CRBD mimic to OAB, so we designed this study to assess the efficacy of solifenacin and Darifenacin for prevention of CRBD. METHODS: Ninety patients of either sex undergoing elective spine surgery and requiring urinary catheterization were randomly assigned into three groups to receive oral solifenacin 5 mg (Group S), Darifenacin 7.5 mg (Group D) and placebo (Group C) 1 hour prior to induction of anesthesia. Anesthesia technique was identical in all the groups. Catheter-related bladder discomfort (CRBD) was evaluated in 4-point scale (1 = no discomfort, 2 = mild discomfort, 3 = moderate discomfort, 4 = severe discomfort), on arrival (0 hour) and at 1, 2, and 6 hours postoperatively. Patients were provided patient-controlled analgesia with fentanyl for postoperative pain relief. RESULTS: There were no significant differences in demographic profile and fentanyl requirements (P>0.05). The prevalence and severity of CRBD were significantly less in the group D and group S compared with the group C at all time intervals (P<0.05). CONCLUSIONS: Pretreatment with oral solifenacin or Darifenacin reduces catheter-related bladder discomfort with no clinically relevant significant side effects.
