CAS 170105-16-5|Imidafenacin

Introduction：Basic information about CAS 170105-16-5|Imidafenacin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Imidafenacin BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Imidafenacin
CAS Number	170105-16-5	Molecular Weight	319.400
Density	1.1±0.1 g/cm3	Boiling Point	579.7±50.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₁N₃O	Melting Point	/
MSDS	USA	Flash Point	304.4±30.1 °C

Names

Name	4-(2-methylimidazol-1-yl)-2,2-diphenylbutanamide
Synonym	More Synonyms

Imidafenacin BiologicalActivity

Description	Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).IC50 value: 0.3 nM(M3) [1]in vitro: KRP-197 showed equipotent anti-M2 and anti-M3 activity and decreased subtype-selectivity [1]. in vivo: Intraduodenal administration of KRP-197 (0.04±0.30 mg/kg) inhibited bladder contraction dose-dependently, and the ED30 value was 0.11 mg/kg. The inhibitory action of KRP-197 on the bladder contraction was 19 times as potent as that of oxybutynin. KRP-197 showed preventive action againstthe decrease in bladder capacity induced by carbachol(ED50 0.074 mg/kg, intragastric administration), andthe potency of the inhibitory action was 15-fold greaterthan that of oxybutynin [1]. The learning-inhibitory doses of intravenous oxybutynin hydrochloride and tolterodine tartrate were 0.3 and 3 mg/kg in sham-operated rats and 0.1 and 1 mg/kg in nbM-lesioned rats, respectively. Thus, the learning impairments by those antimuscarinics were more sensitive in nbM-lesioned rats than in sham-operated rats. On the other hand, intravenous administration of imidafenacin had no influence on learning in either case of the rats. In normal rats, however, intracerebroventricular administration of imidafenacin impaired learning to the same degree as that of oxybutynin hydrochloride [2].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch Areas >>Neurological Disease
References	[1]. 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. [2]. 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.

Description

Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).IC50 value: 0.3 nM(M3) [1]in vitro: KRP-197 showed equipotent anti-M2 and anti-M3 activity and decreased subtype-selectivity [1]. in vivo: Intraduodenal administration of KRP-197 (0.04±0.30 mg/kg) inhibited bladder contraction dose-dependently, and the ED30 value was 0.11 mg/kg. The inhibitory action of KRP-197 on the bladder contraction was 19 times as potent as that of oxybutynin. KRP-197 showed preventive action againstthe decrease in bladder capacity induced by carbachol(ED50 0.074 mg/kg, intragastric administration), andthe potency of the inhibitory action was 15-fold greaterthan that of oxybutynin [1]. The learning-inhibitory doses of intravenous oxybutynin hydrochloride and tolterodine tartrate were 0.3 and 3 mg/kg in sham-operated rats and 0.1 and 1 mg/kg in nbM-lesioned rats, respectively. Thus, the learning impairments by those antimuscarinics were more sensitive in nbM-lesioned rats than in sham-operated rats. On the other hand, intravenous administration of imidafenacin had no influence on learning in either case of the rats. In normal rats, however, intracerebroventricular administration of imidafenacin impaired learning to the same degree as that of oxybutynin hydrochloride [2].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch Areas >>Neurological Disease

References

[1]. 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.

[2]. 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.

Chemical & Physical Properties

Density	1.1±0.1 g/cm3
Boiling Point	579.7±50.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₁N₃O
Molecular Weight	319.400
Flash Point	304.4±30.1 °C
Exact Mass	319.168457
PSA	61.90000
LogP	2.42
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.603
InChIKey	SQKXYSGRELMAAU-UHFFFAOYSA-N
SMILES	Cc1nccn1CCC(C(N)=O)(c1ccccc1)c1ccccc1
Storage condition	2-8℃

Synonyms

1H-Imidazole-1-butanamide, 2-methyl-α,α-diphenyl-

Imidafenacin

[14C]-Imidafenacin

4-(2-Methyl-imidazol-1-yl)-2,2-diphenyl-butyramide

Staybla

4-(2-methyl-1-imidazolyl)-2,2-diphenylbutyramide

Imidafenacin (JAN/INN)

4-(2-Methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide

Uritos (TN)

Uritos

Staybla (TN)

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