MT-1207 (free base)

MT-1207 free base is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 has IC₅₀ values of <0.1 nM, 0.15 nM, 1.40 nM, and 0.27 nM for α1A, α1B, α1D, and 5-HT2A, respectively. MT-1207 free base induces vasodilation, improves baroreflex sensitivity, and reduces heart rate in isolated hearts. MT-1207 free base lowers blood pressure, protects the heart, brain, and kidneys, improves cognition, delays stroke, reduces mortality, and lowers uric acid without impairing renal function in SHR/2K1C/2K2C models. MT-1207 free base exhibits high plasma protein binding, resistance to plasma esterases, and NADPH-dependent hepatic metabolism. MT-1207 free base can be used for research related to hypertension^[1][2][3]. In Vitro:MT-1207 free base binds stably to α_1A, α_1B, α_1D, 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors through hydrogen bonds, hydrophobic interactions, and van der Waals forces^[1].
MT-1207 (0.1 nM-1 μM) free base effectively inhibits adrenergic α_1A, α_1B, α_1D and 5-HT_2A receptors with high binding affinity^[3].
MT-1207 (1-100 nM; 60 min) free base is a potent multi-target antagonist of α1-adrenoceptor subtypes and 5-HT_2A receptors in CHO cell membranes^[2].
MT-1207 (10-1000 ng/mL; 30 min) free base exhibits extremely high plasma protein binding rates in Sprague-Dawley rat, beagle dog, cynomolgus monkey, and human plasma^[2].
MT-1207 (1 μg/mL; 0-120 min) free base exhibits strong plasma stability in human, Sprague-Dawley rat, Beagle dog, and cynomolgus monkey plasma, and is resistant to enzymatic hydrolysis by plasma esterases^[2].
MT-1207 (10 μM; 0-120 min) free base undergoes rapid NADPH-dependent metabolism in rat, beagle dog, cynomolgus monkey, and human liver microsomes^[2].
MT-1207 (0.2 ng/mL-2000 μg/mL; 20 min) free base does not significantly inhibit CYP3A4, CYP2C9, CYP1A2, and CYP2C19 in human liver microsomes, but exhibits a certain degree of CYP2D6 inhibition at higher concentrations^[2]. In Vivo:MT-1207 (10 mg/kg/d; p.o.; daily; 9 weeks) free base significantly lowers BP in 2K2C rats without causing reflex HR increase^[1].
MT-1207 (10-20 mg/kg/d; p.o.; daily; 3 days to 9 weeks) free base reverses renal dysfunction and reduces uric acid levels in 2K2C rats^[1].
MT-1207 (10 mg/kg/d; p.o.; daily; 2 weeks) free base exerts uric acid-lowering effects in a hyperuricemia model^[1].
MT-1207 (10-20 mg/kg/d; p.o.; 9 weeks) free base ameliorates cognitive dysfunction in 2K2C rats^[1].
MT-1207 (10-20 mg/kg/d; p.o.; 9 weeks) free base exhibits cardiovascular and renal protective effects in 2K2C rats^[1].
MT-1207 (10 mg/kg/d; p.o.; lifelong) free base reduces mortality and extends lifespan in 2K2C rats^[1].
MT-1207 (1 mg/kg; i.v.) free base blocks α1 and 5-HT₂ receptors in vivo^[1].
MT-1207 (10 mg/kg/day; p.o.; 4 months) free base stably lowers blood pressure, improves baroreflex sensitivity, and provides renal and cardiovascular organ protection^[3].
MT-1207 (10 mg/kg/day; p.o.; approximately 8 months) stably lowers blood pressure free base and improves survival in stroke-prone SHR by delaying the onset of stroke and death^[3].
MT-1207 (10 mg/kg; p.o.; daily; 9 weeks) free base effectively lowers blood pressure without impairing renal function in the 2K2C renovascular hypertensive rat model^[2].
MT-1207 (2.5-10 mg/kg; p.o.; single dose) free base effectively lowers blood pressure in rats without causing the side effect of orthostatic hypotension^[2].
MT-1207 (250-1000 mg/kg; p.o.; single dose) free base is well tolerated in SD rats, with a maximum tolerated dose exceeding 1000 mg/kg^[2].
MT-1207 (10-100 mg/kg; p.o.; once daily; 13 weeks) free base is tolerated at all dose levels over 13 consecutive weeks, with a no-observed-adverse-effect level (NOAEL) of 100 mg/kg^[2].
MT-1207 (1.25-20 mg/kg; p.o.; single dose) free base produces a rapid, dose-dependent antihypertensive effect without inducing reflex tachycardia^[3].
MT-1207 (0.25-6 mg/kg; p.o.; single dose) free base dose-dependently lowers systolic blood pressure in 2K1C dogs, with effects maintained for over 12 h and without causing reflex tachycardia^[3].
MT-1207 (5 mg/kg/day; p.o.; once daily; for 7 consecutive days) free base significantly lowers systolic blood pressure and slightly slows heart rate without affecting ECG^[3].
MT-1207 (2 mg/kg/day; p.o.; once daily; for 7 consecutive days) free base significantly lowers systolic blood pressure and slightly slows heart rate, accompanied by minor ECG changes that recover after drug withdrawal^[3].