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11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE

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11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE Basic information

Product Name:
11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE
Synonyms:
  • 11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE
  • AQ-RA 741
  • 11-(2-(4-(4-(Diethylamino)butyl)piperidin-1-yl)acetyl)-5H-benzo[e]pyrido[3,2-b][1,4]diazepin-6(11H)-one
  • 11-[[4-[4-(Diethylamino)butyl]piperidin-1-yl]acetyl]-11H-pyrido[2,3-b][1,4]benzodiazepin-6(5H)-one
  • 5,11-Dihydro-11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
  • 6H-Pyrido[2,3-b][1,4]benzodiazepin-6-one, 11-[2-[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro-
  • AQ-RA 741, M2 antagonist
CAS:
123548-16-3
MF:
C27H37N5O2
MW:
463.61
Product Categories:
  • Acetylcholine receptor
  • Muscarinic
Mol File:
123548-16-3.mol
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11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE Chemical Properties

Boiling point:
602.7±50.0 °C(Predicted)
Density 
1.132±0.06 g/cm3(Predicted)
storage temp. 
Store at RT
solubility 
<46.36mg/ml in 1eq. HCl; <46.36mg/ml in ethanol; <46.36mg/ml in DMSO
form 
solid
pka
11.29±0.20(Predicted)
color 
White
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11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE Usage And Synthesis

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.

11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONESupplier

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11-[[4-[4-(DIETHYLAMINO)BUTYL]-1-PIPERIDINYL]ACETYL]-5,11-DIHYDRO-6H-PYRIDO[2,3-B][1,4]BENZODIAZEPIN-6-ONE(123548-16-3)Related Product Information