| Identification | Back Directory | [Name]
(AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE | [CAS]
244277-89-2 | [Synonyms]
J 104129 FUMARATE
(αR)-α-Cyclopentyl-α-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamidefumarate
Benzeneacetamide, α-cyclopentyl-α-hydroxy-N-[1-(4-methyl-3-penten-1-yl)-4-piperidinyl]-, (αR)-
(AR)-A-CYCLOPENTYL-A-HYDROXY-N-[1-(4-METHYL-3-PENTENYL)-4-PIPERIDINYL]BENZENEACETAMIDE FUMARATE | [Molecular Formula]
C24H36N2O2 | [MDL Number]
MFCD09753272 | [MOL File]
244277-89-2.mol | [Molecular Weight]
384.55 |
| Hazard Information | Back Directory | [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). | [in vivo]
J-104129 (10 mg/kg; p.o.; single) shows durable bronchodilatory action lasting over 10 h in rats[1][2].
J-104129 (p.o.) antagonizes ACh-induced bronchoconstriction with an ED50 value of 0.58 mg/kg in rats[1]. | Animal Model: | Male Sprague-Dawley rats[1][2]. | | Dosage: | 10 mg/kg | | Administration: | Oral administration; single. | | Result: | Exhibited bronchodilatory activity. |
| [storage]
Store at -20°C |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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