244277-89-2

244277-89-2 structure

Name: (AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE
Chemical Name: but-2-enedioic acid,(2R)-2-cyclopentyl-2-hydroxy-N-[1-(4-methylpent-3-enyl)piperidin-4-yl]-2-phenylacetamide
CAS Number: 244277-89-2
Molecular Formula: C₂₄H₃₆N₂O₂
Molecular Weight: 384.55
Create Date: 2016-10-22 12:22:57
Modify Date: 2024-01-13 19:01:17
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].

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

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.