Description
AQ-RA 741 is a potent and selective M2 antagonist, with high affinity for cardiac M2 sites (pKi = 8.30) . The M2 muscarinic receptor subtype is involved in the regulation of heart rate, mediating muscarinic receptor-dependent movement, antinociceptive responses and temperature control . 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 . 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 .
Product information
CAS Number: 123548-16-3
Molecular Weight: 463.61
Formula: C27H37N5O2
Chemical Name: 2-(2-{4-[4-(diethylamino)butyl]piperidin-1-yl}acetyl)-2,4,9-triazatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-10-one
Smiles: CCN(CCCCC1CCN(CC(=O)N2C3=NC=CC=C3NC(=O)C3=CC=CC=C23)CC1)CC
InChiKey: BCUGCHZRMKTPMU-UHFFFAOYSA-N
InChi: InChI=1S/C27H37N5O2/c1-3-30(4-2)17-8-7-10-21-14-18-31(19-15-21)20-25(33)32-24-13-6-5-11-22(24)27(34)29-23-12-9-16-28-26(23)32/h5-6,9,11-13,16,21H,3-4,7-8,10,14-15,17-20H2,1-2H3,(H,29,34)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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