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

Names

[ CAS No. ]:
244277-89-2

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

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]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Research Areas >> Others
Signaling Pathways >> GPCR/G Protein >> mAChR

[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

Related Compounds