MT-1207 is an antagonist of α1A-, α1B-, and α1D-adrenergic receptors and the serotonin (5-HT) receptor subtype 5-HT2A (IC50s = <0.1, 0.15, 1.4, and 0.27 nM, respectively).1 It is selective for these receptors over a panel of 87 receptors, ion channels, and enzymes at 1 ?M but does inhibit α2A- and α2B-adrenergic and 5-HT1A, 5-HT1B, 5-HT2B, and 5-HT2C receptors (IC50s = 18.1, 4.89, 4.68, 41, 11.5, and 26 nM, respectively), among others. MT-1207 induces relaxation of isolated rat aortic rings precontracted with epinephrine, potassium chloride, norepinephrine, or 5-HT in a concentration-dependent manner. It decreases systolic and diastolic blood pressure and heart rate in spontaneously hypertensive rats and two kidney-one clip (2K-1C) renal hypertensive dogs when administered at doses of 10 and 4 mg/kg, respectively.
References:
[1]. Xu, T.Y., Wang, P., Tian, J.S., et al.Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agentActa. Pharmacol. Sin.42(6)885-897(2021).