200,000+ products from a single source!

sales@angenechem.com

Home > Bromides > 133099-07-7

133099-07-7

133099-07-7 | 3-Pyrrolidineacetamide, 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-, hydrobromide (1:1), (3S)-

CAS No: 133099-07-7 Catalog No: AG001496 MDL No:MFCD08141803

Product Description

Catalog Number:
AG001496
Chemical Name:
3-Pyrrolidineacetamide, 1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α,α-diphenyl-, hydrobromide (1:1), (3S)-
CAS Number:
133099-07-7
Molecular Formula:
C28H31BrN2O2
Molecular Weight:
507.4619
MDL Number:
MFCD08141803
IUPAC Name:
2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide;hydrobromide
InChI:
InChI=1S/C28H30N2O2.BrH/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);1H/t25-;/m1./s1
InChI Key:
UQAVIASOPREUIT-VQIWEWKSSA-N
SMILES:
NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2.Br
EC Number:
603-705-7
UNII:
CR02EYQ8GV

Properties

Complexity:
607  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
2  
Defined Atom Stereocenter Count:
1  
Defined Bond Stereocenter Count:
0
Exact Mass:
506.157g/mol
Formal Charge:
0
Heavy Atom Count:
33  
Hydrogen Bond Acceptor Count:
3  
Hydrogen Bond Donor Count:
2  
Isotope Atom Count:
0
Molecular Weight:
507.472g/mol
Monoisotopic Mass:
506.157g/mol
Rotatable Bond Count:
7  
Topological Polar Surface Area:
55.6A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0

Literature

Title Journal
Pharmacokinetics and toxicity of antimuscarinic drugs for overactive bladder treatment in females. Expert opinion on drug metabolism & toxicology 20121101
Identification and structural elucidation of two process impurities and stress degradants in darifenacin hydrobromide active pharmaceutical ingredient by LC-ESI/MS(n). The Analyst 20120807
Benefits and harms of pharmacologic treatment for urinary incontinence in women: a systematic review. Annals of internal medicine 20120619
Role of M2 and M3 muscarinic acetylcholine receptor subtypes in activation of bladder afferent pathways in spinal cord injured rats. Urology 20120501
Contractions of the mouse prostate elicited by acetylcholine are mediated by M(3) muscarinic receptors. The Journal of pharmacology and experimental therapeutics 20111201
Urothelial/lamina propria spontaneous activity and the role of M3 muscarinic receptors in mediating rate responses to stretch and carbachol. Urology 20111201
Time-to-effect with darifenacin in overactive bladder: a pooled analysis. International urogynecology journal 20111201
Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourology and urodynamics 20111101
A comprehensive non-clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder. British journal of clinical pharmacology 20110801
Evaluation of brain anticholinergic activities of urinary spasmolytic drugs using a high-throughput radio receptor bioassay. Journal of the American Geriatrics Society 20110301
Patient experience with darifenacin - results of a short-term community-based survey in managing overactive bladder. Current medical research and opinion 20110201
Activation state of the M3 muscarinic acetylcholine receptor modulates mammalian odorant receptor signaling. Science signaling 20110111
Overactive bladder drugs and constipation: a meta-analysis of randomized, placebo-controlled trials. Digestive diseases and sciences 20110101
Patient satisfaction with the benefits of overactive bladder treatment: exploration of influencing factors and development of a satisfaction assessment instrument. Neurourology and urodynamics 20110101
Loss of muscarinic and purinergic receptors in urinary bladder of rats with hydrochloric acid-induced cystitis. Urology 20101001
Noninvasive evaluation of brain muscarinic receptor occupancy of oxybutynin, darifenacin and imidafenacin in rats by positron emission tomography. Life sciences 20100731
Comparison of selective M3 and nonselective muscarinic receptor antagonists on gastrointestinal transit and bowel habits in humans. American journal of physiology. Gastrointestinal and liver physiology 20100701
Comparison of human and porcine gastric clasp and sling fiber contraction by M2 and M3 muscarinic receptors. American journal of physiology. Gastrointestinal and liver physiology 20100401
Immunoglobulins from scleroderma patients inhibit the muscarinic receptor activation in internal anal sphincter smooth muscle cells. American journal of physiology. Gastrointestinal and liver physiology 20091201
Anticholinergic drug use for overactive bladder in Sweden: a nationwide pharmacoepidemiological study. International urogynecology journal and pelvic floor dysfunction 20091101
Listening to the patient: a flexible approach to the use of antimuscarinic agents in overactive bladder syndrome. BJU international 20091001
Quantitative analysis of the loss of muscarinic receptors in various peripheral tissues in M1-M5 receptor single knockout mice. British journal of pharmacology 20090401
Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. The Journal of pharmacology and experimental therapeutics 20090301
In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. British journal of pharmacology 20090301
Psychometric validation of the overactive bladder satisfaction with treatment questionnaire (OAB-SAT-q). Neurourology and urodynamics 20090101
Use of antimuscarinics in the elderly. TheScientificWorldJournal 20090101
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 of cardiovascular pharmacology and therapeutics 20081201
Preserving cognitive function for patients with overactive bladder: evidence for a differential effect with darifenacin. International journal of clinical practice 20081101
Darifenacin treatment for overactive bladder in patients who expressed dissatisfaction with prior extended-release antimuscarinic therapy. International journal of clinical practice 20081101
Human urine with solifenacin intake but not tolterodine or darifenacin intake blocks detrusor overactivity. International urogynecology journal and pelvic floor dysfunction 20081001
Choice of antimuscarinic agents for overactive bladder in the older patient: focus on darifenacin. Clinical interventions in aging 20080901
Interstitial granulomatous dermatitis associated with darifenacin. Journal of drugs in dermatology : JDD 20080901
Clinical relevance of health-related quality of life outcomes with darifenacin. BJU international 20080701
Activated cholinergic signaling provides a target in squamous cell lung carcinoma. Cancer research 20080615
A journey to continence: a case study of overactive bladder syndrome. Urologic nursing 20080601
A comparison of the efficacy of darifenacin alone vs. darifenacin plus a Behavioural Modification Programme upon the symptoms of overactive bladder. International journal of clinical practice 20080401
The effect of darifenacin on overactive bladders in female and male rabbits. International urology and nephrology 20080101
Long-term benefits of darifenacin treatment for patient quality of life: results from a 2-year extension study. Neurourology and urodynamics 20080101
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. Current medical research and opinion 20071101
Comparative in vivo uroselectivity profiles of anticholinergics, tested in a novel anesthetized rabbit model. European journal of pharmacology 20071031
Darifenacin treatment of patients >or= 65 years with overactive bladder: results of a randomized, controlled, 12-week trial. Current medical research and opinion 20071001
[The recommendations of the Polish Gynecologic Society regarding the use of darifenacin, selective muscarinic antagonists in the treatment of overactive bladder]. Ginekologia polska 20071001
Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. European urology 20070901
Editorial comment on: effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. European urology 20070901
Editorial comment on: effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. European urology 20070901
Cholinergic activation of phasic activity in the isolated bladder: possible evidence for M3- and M2-dependent components of a motor/sensory system. BJU international 20070901
Pharmacologic management of overactive bladder. Clinical interventions in aging 20070901
Human idiopathic and neurogenic overactive bladders and the role of M2 muscarinic receptors in contraction. European urology 20070801
Update on drugs for overactive bladder syndrome. Drug and therapeutics bulletin 20070601
M3 muscarinic receptor antagonists inhibit small cell lung carcinoma growth and mitogen-activated protein kinase phosphorylation induced by acetylcholine secretion. Cancer research 20070415
[Treatment of overactive bladder in elderly and old people]. Der Urologe. Ausg. A 20070401
Darifenacin: a muscarinic M3-selective receptor antagonist for the treatment of overactive bladder. Expert opinion on pharmacotherapy 20070301
Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder. The Journal of urology 20070201
M2 mediated contractions of human bladder from organ donors is associated with an increase in urothelial muscarinic receptors. Neurourology and urodynamics 20070101
Pharmacological characterization of a new antimuscarinic agent, solifenacin succinate, in comparison with other antimuscarinic agents. Biological & pharmaceutical bulletin 20070101
[Darifenacine--Emselex]. Journal de pharmacie de Belgique 20070101
In vivo demonstration of M3 muscarinic receptor subtype selectivity of darifenacin in mice. Life sciences 20061214
New developments in the treatment of urinary incontinence. Minerva urologica e nefrologica = The Italian journal of urology and nephrology 20061201
Treatment of overactive bladder in the aging population: focus on darifenacin. Clinical interventions in aging 20061201
Long-term treatment with darifenacin for overactive bladder: results of a 2-year, open-label extension study. BJU international 20061101
Darifenacin: Pharmacology and clinical usage. The Urologic clinics of North America 20061101
Treatment of the overactive bladder syndrome with muscarinic receptor antagonists: a matter of metabolites? Naunyn-Schmiedeberg's archives of pharmacology 20061101
Differential effects of the antimuscarinic agents darifenacin and oxybutynin ER on memory in older subjects. European urology 20060801
[Anticholinergics for overactive bladder: does subtype selectivity play a role?]. Der Urologe. Ausg. A 20060701
Regulation of bladder muscarinic receptor subtypes by experimental pathologies. Autonomic & autacoid pharmacology 20060701
Dose response with darifenacin, a novel once-daily M3 selective receptor antagonist for the treatment of overactive bladder: results of a fixed dose study. International urogynecology journal and pelvic floor dysfunction 20060501
Using anticholinergics to treat overactive bladder: the issue of treatment tolerability. The American journal of medicine 20060301
M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. I. Normal rat bladder. The Journal of pharmacology and experimental therapeutics 20060201
M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. II. Denervated rat bladder. The Journal of pharmacology and experimental therapeutics 20060201
New drugs 06, part I. Nursing 20060201
Efficacy, tolerability and safety of darifenacin, an M(3) selective receptor antagonist: an investigation of warning time in patients with OAB. International journal of clinical practice 20060101
The clinical pharmacokinetics of darifenacin. Clinical pharmacokinetics 20060101
Pharmacodynamic effects of darifenacin, a muscarinic M selective receptor antagonist for the treatment of overactive bladder, in healthy volunteers. BJU international 20051101
Treatment of overactive bladder in the older patient: pooled analysis of three phase III studies of darifenacin, an M3 selective receptor antagonist. European urology 20050901
Efficacy and tolerability of darifenacin, a muscarinic M3 selective receptor antagonist (M3 SRA), compared with oxybutynin in the treatment of patients with overactive bladder. World journal of urology 20050901
QT and QTc interval with standard and supratherapeutic doses of darifenacin, a muscarinic M3 selective receptor antagonist for the treatment of overactive bladder. Journal of clinical pharmacology 20050901
Solifenacin and darifenacin for overactive bladder. Obstetrics and gynecology 20050801
Comparison of darifenacin and oxybutynin in patients with overactive bladder: assessment of ambulatory urodynamics and impact on salivary flow. European urology 20050701
Darifenacin in the treatment of overactive bladder. International journal of clinical practice 20050701
Effects of ageing on muscarinic receptor subtypes and function in rat urinary bladder. Naunyn-Schmiedeberg's archives of pharmacology 20050701
Darifenacin in the treatment of overactive bladder. Drugs of today (Barcelona, Spain : 1998) 20050701
New treatment options for overactive bladder. South Dakota journal of medicine 20050601
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. BJU international 20050501
Increased warning time with darifenacin: a new concept in the management of urinary urgency. The Journal of urology 20050401
Solifenacin and darifenacin for overactive bladder. The Medical letter on drugs and therapeutics 20050314
An investigation of dose titration with darifenacin, an M3-selective receptor antagonist. BJU international 20050301
Assessment of cognitive function of the elderly population: effects of darifenacin. The Journal of urology 20050201
New drugs: palifermin, eszopiclone, and darifenacin hydrobromide. Journal of the American Pharmacists Association : JAPhA 20050101
[Overactive bladder]. Krankenpflege Journal 20050101
Mechanisms mediating cholinergic antral circular smooth muscle contraction in rats. World journal of gastroenterology 20041115
Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder. Expert opinion on investigational drugs 20041101
Preview of new drugs for overactive bladder and incontinence: darifenacin, solifenacin, trospium, and duloxetine. Current urology reports 20041001
Elevating our therapeutic expectations in overactive bladder. Journal of the American Academy of Nurse Practitioners 20041001
In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats. European journal of pharmacology 20040525
Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder. European urology 20040401
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. British journal of clinical pharmacology 20040201
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. Life sciences 20040102
Darifenacin: in the treatment of overactive bladder. Drugs & aging 20040101
Population pharmacokinetic modelling of darifenacin and its hydroxylated metabolite using pooled data, incorporating saturable first-pass metabolism, CYP2D6 genotype and formulation-dependent bioavailability. British journal of clinical pharmacology 20031201
Pharmacological effects of darifenacin on human isolated urinary bladder. Pharmacology 20031201
Update on overactive bladder: pharmacologic approaches on the horizon. Current urology reports 20031001
M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland. Naunyn-Schmiedeberg's archives of pharmacology 20020801
Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists. European journal of pharmacology 19980522
Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors. Journal of receptor and signal transduction research 19970101

© 2019 Angene International Limited. All rights Reserved.