| Identification | Back Directory | [Name]
11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE | [CAS]
123548-16-3 | [Synonyms]
AQ-RA 741
11-[[4-[4-(Diethylamino)butyl]piperidin-1-yl]acetyl]-11H-pyrido[2,3-b][1,4]benzodiazepin-6(5H)-one
11-(2-(4-(4-(Diethylamino)butyl)piperidin-1-yl)acetyl)-5H-benzo[e]pyrido[3,2-b][1,4]diazepin-6(11H)-one
5,11-Dihydro-11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE | [Molecular Formula]
C27H37N5O2 | [MDL Number]
MFCD00884623 | [MOL File]
123548-16-3.mol | [Molecular Weight]
463.61 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at RT | [solubility ]
<46.36mg/ml in 1eq. HCl; <46.36mg/ml in ethanol; <46.36mg/ml in DMSO | [form ]
solid | [color ]
White |
| Hazard Information | Back Directory | [Uses]
AQ-RA 741 acts as a potent and highly specific muscarinic M2 receptor antagonist, with potential application towards the development of bronchodilator anti-muscarinic agents for humans. | [Definition]
ChEBI: 11-[2-[4-[4-(diethylamino)butyl]-1-piperidinyl]-1-oxoethyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one is a benzodiazepine. | [Biological Activity]
High affinity, selective muscarinic M 2 receptor antagonist (pK i values are 8.3, 7.7 and 6.82 for M 2 , M 1 and M 3 receptors, respectively). In vivo, displays cardioselectivity over intestinal, tracheal and bladder muscarinic receptors; inhibits vagally and agonist-induced bradycardia. | [storage]
Store at RT | [References]
[1]. doods h, entzeroth m and mayer n. cardioselectivity of aq-ra 741, a novel tricyclic antimuscarinic drug. eur j pharmacol, 1991, 192(1):147-52.
[2]. gomeza j, shannon h, kostenis e, et al. pronounced pharmacologic deficits in m2 muscarinic acetylcholine receptor knockout mice. proc natl acad sci u s a, 1999, 96(4):1692-7. |
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