(AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE

Modify Date: 2024-01-13 19:01:17

(AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE Structure
(AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE structure
Common Name (AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE
CAS Number 244277-89-2 Molecular Weight 384.55
Density N/A Boiling Point 744.6ºC at 760 mmHg
Molecular Formula C24H36N2O2 Melting Point N/A
MSDS N/A Flash Point 404.1ºC

 Use of (AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE


J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation[1][2].

 Names

Name but-2-enedioic acid,(2R)-2-cyclopentyl-2-hydroxy-N-[1-(4-methylpent-3-enyl)piperidin-4-yl]-2-phenylacetamide

  Biological Activity

Description J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation[1][2].
Related Catalog
In Vivo J-104129 (10 mg/kg; p.o.; single) 在大鼠中表现出持续超过 10 h 的持久支气管扩张作用[1][2]。 J-104129 (p.o.) 在大鼠中拮抗 ACh 诱导的支气管收缩,ED50 值为 0.58 mg/kg[1]。 Animal Model: Male Sprague-Dawley rats[1][2]. Dosage: 10 mg/kg Administration: Oral administration; single. Result: Exhibited bronchodilatory activity.
References

[1]. Mitsuya M, et al. J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors. Bioorg Med Chem. 1999 Nov;7(11):2555-67.  

[2]. Morihiro Mitsuya, et al. Discovery of a muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors among 2-[(1S,3S)-3-sulfonylaminocyclopentyl]phenylacetamide derivatives. Bioorg Med Chem. 2000, 8(4): 825-832.

 Chemical & Physical Properties

Boiling Point 744.6ºC at 760 mmHg
Molecular Formula C24H36N2O2
Molecular Weight 384.55
Flash Point 404.1ºC
Exact Mass 500.28900
PSA 127.17000
LogP 4.04190
Vapour Pressure 2.77E-23mmHg at 25°C