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170105-16-5,MFCD09833703
Catalog No.:AA00ABHM

170105-16-5 | Imidafenacin

Pack Size
Purity
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25mg
98%(HPLC)
in stock  
$43.00   $30.00
- +
100mg
98%(HPLC)
in stock  
$78.00   $55.00
- +
250mg
98%
in stock  
$112.00   $78.00
- +
1g
98%(HPLC)
in stock  
$239.00   $167.00
- +
5g
98%(HPLC)
in stock  
$715.00   $500.00
- +
10g
98%(HPLC)
in stock  
$1,191.00   $834.00
- +
25g
98%(HPLC)
in stock  
$2,143.00   $1,500.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00ABHM
Chemical Name:
Imidafenacin
CAS Number:
170105-16-5
Molecular Formula:
C20H21N3O
Molecular Weight:
319.4002
MDL Number:
MFCD09833703
SMILES:
NC(=O)C(c1ccccc1)(c1ccccc1)CCn1ccnc1C
Properties
Computed Properties
 
Complexity:
395  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
24  
Hydrogen Bond Acceptor Count:
2  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
6  
XLogP3:
2.7  

Downstream Synthesis Route
542-69-8    170105-16-5   
1-butyl-3-(3-carbamoyl-3,3-diphenyl-propyl)-2-methyl-3<i>H</i>-imidazol-1-ium;iodide 

[1]Miyachi,Hiroyuki;Kiyota,Hiromi;Uchiki,Hideharu;Segawa,Mitsuru[BioorganicandMedicinalChemistry,1999,vol.7,#6,p.1151-1161]

100-39-0    170105-16-5   
1-benzyl-3-(3-carbamoyl-3,3-diphenyl-propyl)-2-methyl-3<i>H</i>-imidazol-1-ium;bromide 

[1]Miyachi,Hiroyuki;Kiyota,Hiromi;Uchiki,Hideharu;Segawa,Mitsuru[BioorganicandMedicinalChemistry,1999,vol.7,#6,p.1151-1161]

75-03-6    170105-16-5   
3-(3-carbamoyl-3,3-diphenyl-propyl)-1-ethyl-2-methyl-3<i>H</i>-imidazol-1-ium;iodide 

[1]Miyachi,Hiroyuki;Kiyota,Hiromi;Uchiki,Hideharu;Segawa,Mitsuru[BioorganicandMedicinalChemistry,1999,vol.7,#6,p.1151-1161]

107-08-4    170105-16-5   
3-(3-carbamoyl-3,3-diphenyl-propyl)-2-methyl-1-propyl-3<i>H</i>-imidazol-1-ium;iodide 

[1]Miyachi,Hiroyuki;Kiyota,Hiromi;Uchiki,Hideharu;Segawa,Mitsuru[BioorganicandMedicinalChemistry,1999,vol.7,#6,p.1151-1161]

[1]CurrentPatentAssignee:KYORINHOLDINGS,INC.-US5932607,1999,A

[2]Miyachi,Hiroyuki;Kiyota,Hiromi;Uchiki,Hideharu;Segawa,Mitsuru[BioorganicandMedicinalChemistry,1999,vol.7,#6,p.1151-1161]

[3]Miyachi,Hiroyuki;Kiyota,Hiromi;Segawa,Mitsuru[BioorganicandMedicinalChemistryLetters,1999,vol.9,#20,p.3003-3008]

[4]CurrentPatentAssignee:HENANFURENMEDICALTECHDEV;KAIFENGPHARMACEUTICALGROUP;FURENMEDICINEGROUP-CN105399678,2016,ALocationinpatent:Paragraph0014;0015

Literature

Title: Characterization of muscarinic receptor binding by the novel radioligand, [(3)H]imidafenacin, in the bladder and other tissues of rats.

Journal: Journal of pharmacological sciences 20160701

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

Journal: Expert opinion on drug metabolism & toxicology 20121101

Title: Characterization of bladder selectivity of antimuscarinic agents on the basis of in vivo drug-receptor binding.

Journal: International neurourology journal 20120901

Title: Excitatory effect of propiverine hydrochloride on urethral activity in rats.

Journal: International journal of urology : official journal of the Japanese Urological Association 20120601

Title: Neurogenic bladder.

Journal: Advances in urology 20120101

Title: Effect of imidafenacin on nocturia and sleep disorder in patients with overactive bladder.

Journal: Urologia internationalis 20120101

Title: [Investigation of pharmacokinetics of crushed imidafenacin 0.1-mg tablet after single oral administration in healthy men].

Journal: Hinyokika kiyo. Acta urologica Japonica 20111201

Title: Effect of oxybutynin and imidafenacin on central muscarinic receptor occupancy and cognitive function: a monkey PET study with [(11)C](+)3-MPB.

Journal: NeuroImage 20110901

Title: In vivo bladder selectivity of imidafenacin, a novel antimuscarinic agent, assessed by using an effectiveness index for bladder capacity in rats.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20110901

Title: Quantitative analysis of pseudopolymorphic transformation of imidafenacin by application of a novel combination of near-infrared spectroscopy and a humidity-controlled 96-well plate.

Journal: The Journal of pharmacy and pharmacology 20110701

Title: Antimuscarinics suppress adenosine triphosphate and prostaglandin E2 release from urothelium with potential improvement in detrusor overactivity in rats with cerebral infarction.

Journal: The Journal of urology 20110601

Title: Selective binding of bladder muscarinic receptors in relation to the pharmacokinetics of a novel antimuscarinic agent, imidafenacin, to treat overactive bladder.

Journal: The Journal of pharmacology and experimental therapeutics 20110201

Title: [Efficacy and safety of imidafenacin in female patients with urge and mixed urinary incontinence].

Journal: Hinyokika kiyo. Acta urologica Japonica 20110101

Title: Immediate effect on overactive bladder symptoms following administration of imidafenacin.

Journal: Urologia internationalis 20110101

Title: An overview of the clinical use of antimuscarinics in the treatment of overactive bladder.

Journal: Advances in urology 20110101

Title: The efficacy and safety of propiverine hydrochloride in patients with overactive bladder symptoms who poorly responded to previous anticholinergic agents.

Journal: Advances in urology 20110101

Title: Comparative Evaluation of the Safety and Efficacy of Long-Term Use of Imidafenacin and Solifenacin in Patients with Overactive Bladder: A Prospective, Open, Randomized, Parallel-Group Trial (the LIST Study).

Journal: Advances in urology 20110101

Title: Application of a novel combination of near-infrared spectroscopy and a humidity-controlled 96-well plate to the characterization of the polymorphism of imidafenacin.

Journal: The Journal of pharmacy and pharmacology 20101101

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

Journal: Life sciences 20100731

Title: The add-on effect of solifenacin for patients with remaining overactive bladder after treatment with tamsulosin for lower urinary tract symptoms suggestive of benign prostatic obstruction.

Journal: Advances in urology 20100101

Title: A randomized, double-blind, placebo- and propiverine-controlled trial of the novel antimuscarinic agent imidafenacin in Japanese patients with overactive bladder.

Journal: International journal of urology : official journal of the Japanese Urological Association 20090501

Title: Comparison of the effect of anti-muscarinic agents on bladder activity, urinary ATP level, and autonomic nervous system in rats.

Journal: Biomedical research (Tokyo, Japan) 20090401

Title: Suspected differential interactions of digoxin with imidafenacin and propantheline; some thoughts for introspection.

Journal: Drug metabolism and pharmacokinetics 20090101

Title: Response to 'Suspected differential interactions of digoxin with imidafenacin and propantheline; some thoughts for introspection'.

Journal: Drug metabolism and pharmacokinetics 20090101

Title: Long-term safety, tolerability, and efficacy of the novel anti-muscarinic agent imidafenacin in Japanese patients with overactive bladder.

Journal: International journal of urology : official journal of the Japanese Urological Association 20081001

Title: A randomized, double-blind, placebo-controlled phase II dose-finding study of the novel anti-muscarinic agent imidafenacin in Japanese patients with overactive bladder.

Journal: International journal of urology : official journal of the Japanese Urological Association 20080901

Title: Validation and application of a 96-well format solid-phase extraction and liquid chromatography-tandem mass spectrometry method for the quantitation of digoxin in human plasma.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20080615

Title: [Pharmacological and clinical profile of imidafenacin developed as a new therapeutic agent for overactive bladder].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20080501

Title: Effect of itraconazole on the pharmacokinetics of imidafenacin in healthy subjects.

Journal: Journal of clinical pharmacology 20080301

Title: Absolute bioavailability of imidafenacin after oral administration to healthy subjects.

Journal: British journal of clinical pharmacology 20080201

Title: No effect of imidafenacin, a novel antimuscarinic drug, on digoxin pharmacokinetics in healthy subjects.

Journal: Drug metabolism and pharmacokinetics 20080101

Title: Population pharmacokinetic analysis of a novel muscarinic receptor antagonist, imidafenacin, in healthy volunteers and overactive bladder patients.

Journal: Drug metabolism and pharmacokinetics 20080101

Title: Development and validation of bioanalytical methods for imidafenacin (KRP-197/ONO-8025) and its metabolites in human urine by using liquid chromatography-tandem mass spectrometry.

Journal: Biomedical chromatography : BMC 20070901

Title: Absorption, metabolism, and excretion of [14C]imidafenacin, a new compound for treatment of overactive bladder, after oral administration to healthy male subjects.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20070901

Title: Synthesis of the metabolites of 4-(2-methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide (KRP-197/ONO-8025).

Journal: Chemical & pharmaceutical bulletin 20070701

Title: Development and validation of bioanalytical methods for Imidafenacin (KRP-197/ONO-8025) and its metabolites in human plasma by liquid chromatography-tandem mass spectrometry.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20070615

Title: Drug-drug interactions in the metabolism of imidafenacin: role of the human cytochrome P450 enzymes and UDP-glucuronic acid transferases, and potential of imidafenacin to inhibit human cytochrome P450 enzymes.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20070201

Title: Effects of imidafenacin (KRP-197/ONO-8025), a new anti-cholinergic agent, on muscarinic acetylcholine receptors. High affinities for M3 and M1 receptor subtypes and selectivity for urinary bladder over salivary gland.

Journal: Arzneimittel-Forschung 20070101

Title: Pharmacological effects of imidafenacin (KRP-197/ONO-8025), a new bladder selective anti-cholinergic agent, in rats. Comparison of effects on urinary bladder capacity and contraction, salivary secretion and performance in the Morris water maze task.

Journal: Arzneimittel-Forschung 20070101

Title: Pharmacological effects of KRP-197 on the human isolated urinary bladder.

Journal: Urologia internationalis 20030101

Title: Biomimetic oxidation of 2-methylimidazole derivative with a chemical model system for cytochrome P-450.

Journal: Chemical & pharmaceutical bulletin 20020801

Title: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional.

Journal: Autonomic & autacoid pharmacology 20020601

Title: Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: discovery of potent and subtype-selective antimuscarinic agents.

Journal: Bioorganic & medicinal chemistry 19990601

Title: Miyachi H, et al. Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: discovery of potent and subtype-selective antimuscarinic agents. Bioorg Med Chem. 1999 Jun;7(6):1151-61.

Title: Yamazaki T, et al. Imidafenacin has no influence on learning in nucleus basalis of Meynert-lesioned rats. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1095-102.

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