MT-1207 (hydrochloride)

MT-1207 is an antagonist of α_1A-, α_1B-, and α_1D-adrenergic receptors and the serotonin (5-HT) receptor subtype 5-HT_2A (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 µM but does inhibit α2A- and α2B-adrenergic and 5-HT_1A, 5-HT_1B, 5-HT_2B, and 5-HT_2C 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.

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1. Xu, T.Y., Wang, P., Tian, J.S., et al. Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. Acta. Pharmacol. Sin. 42(6), 885-897 (2021).