244277-89-2

Usage

Uses

J 104129 is a mAChR M3 antagonist.

Biological Activity

Potent M 3 muscarinic receptor antagonist that displays ~ 120-fold selectivity over M 2 receptors (K i values are 4.2, 19 and 490 nM for human M 3 , M 1 and M 2 receptors respectively). Exhibits > 250-fold bronchial selectivity; inhibits ACh-induced bronchoconstriction but not ACh-induced bradycardia (K B values are 3.3 and 170 nM for rat trachea M 3 and rat right atria M 2 receptors respectively).

Upstream product

• 116907-30-3 (2R,5R)-2-(tert-butyl)-5-phenyl-1,3-dioxolan-4-one 
• 427-49-6 2-cyclopentyl-2-hydroxy-2-phenylacetic acid 
• 185030-43-7 1-(4-methyl-3-pentenyl)-4-aminopiperidine 
• 41979-39-9 4-piperidone hydrochloride 
• 2270-59-9 1-bromo-4-methylpent-3-ene 
• 203321-74-8 1-(4-methyl-3-pentenyl)-4-piperidone 
• 64471-43-8 (S)-α-cyclopentyl-α-hydroxy-α-phenylacetic acid 
• 185030-18-6 N-(piperidin-4-yl)-2-cyclopentyl-2-hydroxy-2-phenylacetamide 
• 930-30-3 cyclopent-2-enone 
• 64471-45-0 (2R)-2-cyclopentyl-2-hydroxy-2-phenylacetic acid 

Relevant academic research and scientific papers

Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129

A diastereoselective synthesis of J-104129 (1) was developed. A key step of this synthesis was Michael addition of enolate generated from cis-chiral dioxolane 2 to cyclopentenone, followed by hydrogenolysis of the resultant enol triflate 4. A mixture of c

J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors

A new class of 4-acetamidopiperidine derivatives has been synthesized and investigated for human muscarinic receptor subtype selectivity. Introduction of a hydrocarbon chain of appropriate length into the piperidine nitrogen of the racemic N-(piperidin-4-

1,4-di-substituted piperidine derivatives

This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula ?I! STR1 and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group or a five- or six-membered heteroaromatic group having one or two hetero atoms selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom in which one or two optional hydrogen atoms on the ring may be replaced by substituent groups selected from the group consisting of a halogen atom and a lower alkyl group; R1 represents a cycloalkyl group of 3 to 6 carbon atoms or a cycloalkenyl group of 3 to 6 carbon atoms; R2 represents a saturated or unsaturated aliphatic hydrocarbon radical of 5 to 15 carbon atoms; and X represents O or NH. These compounds have selective antagonistic activity against the muscarinic M3 receptors and can hence be used safely with a minimum of side effects.