Home Bromides 133099-07-7
133099-07-7,MFCD08141803
Catalog No.:AA00146E

133099-07-7 | 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide hydrobromide

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10mg
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25mg
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50mg
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100mg
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250mg
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1g
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$61.00   $43.00
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5g
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25g
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00146E
Chemical Name:
2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide hydrobromide
CAS Number:
133099-07-7
Molecular Formula:
C28H31BrN2O2
Molecular Weight:
507.4619
MDL Number:
MFCD08141803
SMILES:
NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2.Br
Properties
Computed Properties
 
Complexity:
607  
Covalently-Bonded Unit Count:
2  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
33  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
7  

Literature

Title: Pharmacokinetics and toxicity of antimuscarinic drugs for overactive bladder treatment in females.

Journal: Expert opinion on drug metabolism & toxicology 20121101

Title: Identification and structural elucidation of two process impurities and stress degradants in darifenacin hydrobromide active pharmaceutical ingredient by LC-ESI/MS(n).

Journal: The Analyst 20120807

Title: Benefits and harms of pharmacologic treatment for urinary incontinence in women: a systematic review.

Journal: Annals of internal medicine 20120619

Title: Role of M2 and M3 muscarinic acetylcholine receptor subtypes in activation of bladder afferent pathways in spinal cord injured rats.

Journal: Urology 20120501

Title: Contractions of the mouse prostate elicited by acetylcholine are mediated by M(3) muscarinic receptors.

Journal: The Journal of pharmacology and experimental therapeutics 20111201

Title: Urothelial/lamina propria spontaneous activity and the role of M3 muscarinic receptors in mediating rate responses to stretch and carbachol.

Journal: Urology 20111201

Title: Time-to-effect with darifenacin in overactive bladder: a pooled analysis.

Journal: International urogynecology journal 20111201

Title: Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers.

Journal: Neurourology and urodynamics 20111101

Title: A comprehensive non-clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder.

Journal: British journal of clinical pharmacology 20110801

Title: Evaluation of brain anticholinergic activities of urinary spasmolytic drugs using a high-throughput radio receptor bioassay.

Journal: Journal of the American Geriatrics Society 20110301

Title: Patient experience with darifenacin - results of a short-term community-based survey in managing overactive bladder.

Journal: Current medical research and opinion 20110201

Title: Activation state of the M3 muscarinic acetylcholine receptor modulates mammalian odorant receptor signaling.

Journal: Science signaling 20110111

Title: Overactive bladder drugs and constipation: a meta-analysis of randomized, placebo-controlled trials.

Journal: Digestive diseases and sciences 20110101

Title: Patient satisfaction with the benefits of overactive bladder treatment: exploration of influencing factors and development of a satisfaction assessment instrument.

Journal: Neurourology and urodynamics 20110101

Title: Loss of muscarinic and purinergic receptors in urinary bladder of rats with hydrochloric acid-induced cystitis.

Journal: Urology 20101001

Title: Noninvasive evaluation of brain muscarinic receptor occupancy of oxybutynin, darifenacin and imidafenacin in rats by positron emission tomography.

Journal: Life sciences 20100731

Title: Comparison of selective M3 and nonselective muscarinic receptor antagonists on gastrointestinal transit and bowel habits in humans.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20100701

Title: Comparison of human and porcine gastric clasp and sling fiber contraction by M2 and M3 muscarinic receptors.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20100401

Title: Immunoglobulins from scleroderma patients inhibit the muscarinic receptor activation in internal anal sphincter smooth muscle cells.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20091201

Title: Anticholinergic drug use for overactive bladder in Sweden: a nationwide pharmacoepidemiological study.

Journal: International urogynecology journal and pelvic floor dysfunction 20091101

Title: Listening to the patient: a flexible approach to the use of antimuscarinic agents in overactive bladder syndrome.

Journal: BJU international 20091001

Title: Quantitative analysis of the loss of muscarinic receptors in various peripheral tissues in M1-M5 receptor single knockout mice.

Journal: British journal of pharmacology 20090401

Title: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa.

Journal: The Journal of pharmacology and experimental therapeutics 20090301

Title: In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder.

Journal: British journal of pharmacology 20090301

Title: Psychometric validation of the overactive bladder satisfaction with treatment questionnaire (OAB-SAT-q).

Journal: Neurourology and urodynamics 20090101

Title: Use of antimuscarinics in the elderly.

Journal: TheScientificWorldJournal 20090101

Title: Differential pharmacological effects of antimuscarinic drugs on heart rate: a randomized, placebo-controlled, double-blind, crossover study with tolterodine and darifenacin in healthy participants > or = 50 years.

Journal: Journal of cardiovascular pharmacology and therapeutics 20081201

Title: Preserving cognitive function for patients with overactive bladder: evidence for a differential effect with darifenacin.

Journal: International journal of clinical practice 20081101

Title: Darifenacin treatment for overactive bladder in patients who expressed dissatisfaction with prior extended-release antimuscarinic therapy.

Journal: International journal of clinical practice 20081101

Title: Human urine with solifenacin intake but not tolterodine or darifenacin intake blocks detrusor overactivity.

Journal: International urogynecology journal and pelvic floor dysfunction 20081001

Title: Choice of antimuscarinic agents for overactive bladder in the older patient: focus on darifenacin.

Journal: Clinical interventions in aging 20080901

Title: Interstitial granulomatous dermatitis associated with darifenacin.

Journal: Journal of drugs in dermatology : JDD 20080901

Title: Clinical relevance of health-related quality of life outcomes with darifenacin.

Journal: BJU international 20080701

Title: Activated cholinergic signaling provides a target in squamous cell lung carcinoma.

Journal: Cancer research 20080615

Title: A journey to continence: a case study of overactive bladder syndrome.

Journal: Urologic nursing 20080601

Title: A comparison of the efficacy of darifenacin alone vs. darifenacin plus a Behavioural Modification Programme upon the symptoms of overactive bladder.

Journal: International journal of clinical practice 20080401

Title: The effect of darifenacin on overactive bladders in female and male rabbits.

Journal: International urology and nephrology 20080101

Title: Long-term benefits of darifenacin treatment for patient quality of life: results from a 2-year extension study.

Journal: Neurourology and urodynamics 20080101

Title: Long-term darifenacin treatment for overactive bladder in patients aged 65 years and older: analysis of results from a 2-year, open-label extension study.

Journal: Current medical research and opinion 20071101

Title: Comparative in vivo uroselectivity profiles of anticholinergics, tested in a novel anesthetized rabbit model.

Journal: European journal of pharmacology 20071031

Title: Darifenacin treatment of patients >or= 65 years with overactive bladder: results of a randomized, controlled, 12-week trial.

Journal: Current medical research and opinion 20071001

Title: [The recommendations of the Polish Gynecologic Society regarding the use of darifenacin, selective muscarinic antagonists in the treatment of overactive bladder].

Journal: Ginekologia polska 20071001

Title: Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve.

Journal: European urology 20070901

Title: Editorial comment on: effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve.

Journal: European urology 20070901

Title: Editorial comment on: effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve.

Journal: European urology 20070901

Title: Cholinergic activation of phasic activity in the isolated bladder: possible evidence for M3- and M2-dependent components of a motor/sensory system.

Journal: BJU international 20070901

Title: Pharmacologic management of overactive bladder.

Journal: Clinical interventions in aging 20070901

Title: Human idiopathic and neurogenic overactive bladders and the role of M2 muscarinic receptors in contraction.

Journal: European urology 20070801

Title: Update on drugs for overactive bladder syndrome.

Journal: Drug and therapeutics bulletin 20070601

Title: M3 muscarinic receptor antagonists inhibit small cell lung carcinoma growth and mitogen-activated protein kinase phosphorylation induced by acetylcholine secretion.

Journal: Cancer research 20070415

Title: [Treatment of overactive bladder in elderly and old people].

Journal: Der Urologe. Ausg. A 20070401

Title: Darifenacin: a muscarinic M3-selective receptor antagonist for the treatment of overactive bladder.

Journal: Expert opinion on pharmacotherapy 20070301

Title: Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder.

Journal: The Journal of urology 20070201

Title: M2 mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors.

Journal: Neurourology and urodynamics 20070101

Title: Pharmacological characterization of a new antimuscarinic agent, solifenacin succinate, in comparison with other antimuscarinic agents.

Journal: Biological & pharmaceutical bulletin 20070101

Title: [Darifenacine--Emselex].

Journal: Journal de pharmacie de Belgique 20070101

Title: In vivo demonstration of M3 muscarinic receptor subtype selectivity of darifenacin in mice.

Journal: Life sciences 20061214

Title: New developments in the treatment of urinary incontinence.

Journal: Minerva urologica e nefrologica = The Italian journal of urology and nephrology 20061201

Title: Treatment of overactive bladder in the aging population: focus on darifenacin.

Journal: Clinical interventions in aging 20061201

Title: Long-term treatment with darifenacin for overactive bladder: results of a 2-year, open-label extension study.

Journal: BJU international 20061101

Title: Darifenacin: Pharmacology and clinical usage.

Journal: The Urologic clinics of North America 20061101

Title: Treatment of the overactive bladder syndrome with muscarinic receptor antagonists: a matter of metabolites?

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20061101

Title: Differential effects of the antimuscarinic agents darifenacin and oxybutynin ER on memory in older subjects.

Journal: European urology 20060801

Title: [Anticholinergics for overactive bladder: does subtype selectivity play a role?].

Journal: Der Urologe. Ausg. A 20060701

Title: Regulation of bladder muscarinic receptor subtypes by experimental pathologies.

Journal: Autonomic & autacoid pharmacology 20060701

Title: Dose response with darifenacin, a novel once-daily M3 selective receptor antagonist for the treatment of overactive bladder: results of a fixed dose study.

Journal: International urogynecology journal and pelvic floor dysfunction 20060501

Title: Using anticholinergics to treat overactive bladder: the issue of treatment tolerability.

Journal: The American journal of medicine 20060301

Title: M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. I. Normal rat bladder.

Journal: The Journal of pharmacology and experimental therapeutics 20060201

Title: M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. II. Denervated rat bladder.

Journal: The Journal of pharmacology and experimental therapeutics 20060201

Title: New drugs 06, part I.

Journal: Nursing 20060201

Title: Efficacy, tolerability and safety of darifenacin, an M(3) selective receptor antagonist: an investigation of warning time in patients with OAB.

Journal: International journal of clinical practice 20060101

Title: The clinical pharmacokinetics of darifenacin.

Journal: Clinical pharmacokinetics 20060101

Title: Pharmacodynamic effects of darifenacin, a muscarinic M selective receptor antagonist for the treatment of overactive bladder, in healthy volunteers.

Journal: BJU international 20051101

Title: Treatment of overactive bladder in the older patient: pooled analysis of three phase III studies of darifenacin, an M3 selective receptor antagonist.

Journal: European urology 20050901

Title: Efficacy and tolerability of darifenacin, a muscarinic M3 selective receptor antagonist (M3 SRA), compared with oxybutynin in the treatment of patients with overactive bladder.

Journal: World journal of urology 20050901

Title: QT and QTc interval with standard and supratherapeutic doses of darifenacin, a muscarinic M3 selective receptor antagonist for the treatment of overactive bladder.

Journal: Journal of clinical pharmacology 20050901

Title: Solifenacin and darifenacin for overactive bladder.

Journal: Obstetrics and gynecology 20050801

Title: Comparison of darifenacin and oxybutynin in patients with overactive bladder: assessment of ambulatory urodynamics and impact on salivary flow.

Journal: European urology 20050701

Title: Darifenacin in the treatment of overactive bladder.

Journal: International journal of clinical practice 20050701

Title: Effects of ageing on muscarinic receptor subtypes and function in rat urinary bladder.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20050701

Title: Darifenacin in the treatment of overactive bladder.

Journal: Drugs of today (Barcelona, Spain : 1998) 20050701

Title: New treatment options for overactive bladder.

Journal: South Dakota journal of medicine 20050601

Title: A pooled analysis of three phase III studies to investigate the efficacy, tolerability and safety of darifenacin, a muscarinic M3 selective receptor antagonist, in the treatment of overactive bladder.

Journal: BJU international 20050501

Title: Increased warning time with darifenacin: a new concept in the management of urinary urgency.

Journal: The Journal of urology 20050401

Title: Solifenacin and darifenacin for overactive bladder.

Journal: The Medical letter on drugs and therapeutics 20050314

Title: An investigation of dose titration with darifenacin, an M3-selective receptor antagonist.

Journal: BJU international 20050301

Title: Assessment of cognitive function of the elderly population: effects of darifenacin.

Journal: The Journal of urology 20050201

Title: New drugs: palifermin, eszopiclone, and darifenacin hydrobromide.

Journal: Journal of the American Pharmacists Association : JAPhA 20050101

Title: [Overactive bladder].

Journal: Krankenpflege Journal 20050101

Title: Mechanisms mediating cholinergic antral circular smooth muscle contraction in rats.

Journal: World journal of gastroenterology 20041115

Title: Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder.

Journal: Expert opinion on investigational drugs 20041101

Title: Preview of new drugs for overactive bladder and incontinence: darifenacin, solifenacin, trospium, and duloxetine.

Journal: Current urology reports 20041001

Title: Elevating our therapeutic expectations in overactive bladder.

Journal: Journal of the American Academy of Nurse Practitioners 20041001

Title: In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats.

Journal: European journal of pharmacology 20040525

Title: Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder.

Journal: European urology 20040401

Title: Assessment of the relative in vivo potency of the hydroxylated metabolite of darifenacin in its ability to decrease salivary flow using pooled population pharmacokinetic-pharmacodynamic data.

Journal: British journal of clinical pharmacology 20040201

Title: Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells.

Journal: Life sciences 20040102

Title: Darifenacin: in the treatment of overactive bladder.

Journal: Drugs & aging 20040101

Title: Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability.

Journal: British journal of clinical pharmacology 20031201

Title: Pharmacological effects of darifenacin on human isolated urinary bladder.

Journal: Pharmacology 20031201

Title: Update on overactive bladder: pharmacologic approaches on the horizon.

Journal: Current urology reports 20031001

Title: M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20020801

Title: Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists.

Journal: European journal of pharmacology 19980522

Title: Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors.

Journal: Journal of receptor and signal transduction research 19970101

Title: Hegde SS, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol, 1997, 120(8), 1409-1418.

Title: Miller DW, et al. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn, 2011, 30(8), 1633-1638.

Title: Iijima K, et al. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol, 2007, 52(3), 842-847.

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Tags:133099-07-7 Molecular Formula|133099-07-7 MDL|133099-07-7 SMILES|133099-07-7 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide hydrobromide