AF-DX 116

AF-DX 116 is an antagonist of M₂ muscarinic acetylcholine receptors (K_i = 0.2 µM).¹ It is selective for cardiac M₂ over salivary gland M₃ receptors (K_i = 5.01 µM) but also binds sympathetic ganglia M₁ receptors (K_i = 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.² 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.³

WARNING This product is not for human or veterinary use.

1. Doods, H.N., Mathy, M.-J., Davidesko, D., et al. Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors. J. Pharmacol. Exp. Ther. 242(1), 257-262 (1987).

2. Bognar, I.T., Beinhauer, B., Kann, P., et al. Different muscarinic receptors mediate autoinhibition of acetylcholine release and vagally-induced vasoconstriction in the rat isolated perfused heart. Naunyn Schmiedebergs Arch. Pharmacol. 341(4), 279-287 (1990).

3. Hata, T., Itoh, E., Funakami, Y., et al. Blood pressure and heart rate are increased by AF-DX 116, a selective M2 antagonist, in autonomic imbalanced and hypotensive rats caused by repeated cold stress. Jpn. J. Pharmacol. 85(3), 313-321 (2001).