BMS-182874 (dimethyla minoanalogue 11) is an antagonist of the ETA ,with IC50 value of 0.150 μM and Ki of 0.055 μM in vsm-A10 cells, and with a KB value of 0.520 μM in rabbit carotid artery rings[1].
BMS 182874 (100 μM/kg, p.o.; a single oral) makes arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h makes arterial pressure is still 12% below the control level[1].
References:
[1]. Abdullaha M, et.al. Methoxy-naphthyl-Linked N-Benzyl Pyridinium Styryls as Dual Cholinesterase Inhibitors: Design, Synthesis, Biological Evaluation, and Structure-Activity Relationship. ACS Omega. 2023 May 9;8(20):17591-17608.
















