| AQ-RA 741M2 antagonist,selective and high affinity |

Sample solution is provided at 25 µL, 10mM.
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Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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Chemical structure


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| Cas No. | 123548-16-3 | SDF | Download SDF |
| Chemical Name | 11-(2-(4-(4-(diethylamino)butyl)piperidin-1-yl)acetyl)-5H-benzo[e]pyrido[3,2-b][1,4]diazepin-6(11H)-one | ||
| Canonical SMILES | O=C(CN1CCC(CCCCN(CC)CC)CC1)N2C3=CC=CC=C3C(NC4=CC=CN=C24)=O | ||
| Formula | C27H37N5O2 | M.Wt | 463.62 |
| Solubility | <46.36mg l="" in="" 1eq.="" hcl;="">46.36mg><46.36mg l="" in="" ethanol;="">46.36mg><46.36mg l="" in="" dmso="">46.36mg> | Storage | Store at RT |
| Physical Appearance | White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AQ-RA 741 is a potent and selective M2 antagonist, with high affinity for cardiac M2 sites (pKi = 8.30) [1].
The M2 muscarinic receptor subtype is involved in the regulation of heart rate, mediating muscarinic receptor-dependent movement, antinociceptive responses and temperature control [2].
In radioligand binding studies, the affinity of AQ-RA 741 for cardiac M2 sites, cortical M1 sites and grandular M3 sites are of pKi values of 8.30, 7.70 and 6.82, respectively. That means AQ-RA 741 showed high affinity for cardiac M2 sites, compared to that for cortical M1 sites and grandular M3 sites. Functional studies showed that AQ-RA 741 is a competitive antagonist. It has a 60 to 87-fold higher affinity to bind cardiac muscarinic receptors than to bind muscarinic receptors in tracheal, intestinal or bladder smooth muscle [1].
M2 selectivity of AQ-RA 741 was also confirmed by in vivo experiments. In rats, guinea-pigs and cats, vagally or agonist-induced bradycardia (?log ID50 = 7.24–7.53 i.v.) were preferentially inhibited by AQ-RA 741. The ratio range of observed potencies between effects mediated by cardiac and other muscarinic receptor was between 9- and greater than 100-fold. These results concluded that AQ-RA 741 is of remarkable in vivo selectivity as a potent and selective M2 antagonist [1].
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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