AF-DX 116

AF-DX 116 is an antagonist of M2 muscarinic acetylcholine receptors (Ki = 0.2 µM). It is selective for cardiac M2 over salivary gland M3 receptors (Ki = 5.01 µM) but also binds sympathetic ganglia M1 receptors (Ki = 0.81 µM). AF-DX 116 (0.1 µM) increases vagus nerve stimulation-induced increases in perfusion pressure by 50% in isolated perfused rat hearts. It increases systolic blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress when administered intravenously at doses of 50, 100, and 200 µg/kg.Formal Name: 11-[2-[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one. CAS Number: 102394-31-0. Molecular Formula: C24H31N5O2. Formula Weight: 421.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 25 mM. SMILES: O=C1NC(C=CC=N2)=C2N(C(CN3CCCCC3CN(CC)CC)=O)C4=C1C=CC=C4. InChi Code: InChI=1S/C24H31N5O2/c1-3-27(4-2)16-18-10-7-8-15-28(18)17-22(30)29-21-13-6-5-11-19(21)24(31)26-20-12-9-14-25-23(20)29/h5-6,9,11-14,18H,3-4,7-8,10,15-17H2,1-2H3,(H,26,31). InChi Key: UBRKDAVQCKZSPO-UHFFFAOYSA-N.