MT-1207 is an orally active and selective adrenergic α 1 and 5-HT 2A receptor antagonist. MT-1207 shows IC 50 <0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α 1A , α 1B , α 1D and 5-HT 2A , respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research.