AF-DX 116

毒蕈碱型M2受体拮抗剂(Ki=0.2µM)；对心脏M2受体的选择性优于唾液腺M3受体(Ki=5.01µM)，但也与交感神经节M1受体结合(Ki=0.81µM)；在0.1µM浓度下，可使大鼠离体灌注心脏中迷走神经刺激引起的灌注压升高50%；在50、100和200µg/kg浓度下，可使反复冷应激引起的低血压大鼠模型中的收缩压和心率升高。A muscarinic M2 receptor antagonist (Ki = 0.2 µM); selective for cardiac M2 over salivary gland M3 receptors (Ki = 5.01 µM) but also binds sympathetic ganglia M1 receptors (Ki = 0.81 µM); increases vagus nerve stimulation-induced increases in perfusion pressure by 50% in isolated perfused rat hearts at 0.1 µM; increases systolic blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress at 50, 100, and 200 µg/kg.分子式C24H31N5O2分子量421.5O=C1NC(C=CC=N2)=C2N(C(CN3CCCCC3CN(CC)CC)=O)C4=C1C=CC=C4