Hypertension is a serious public health problem worldwide. MT-1207 is a chemical entity that has entered into clinical trial as antihypertensive agent. MT-1207 potently inhibits adrenergic α1A, α1B, α1D, and 5-HT2A receptors with K_i<1 nM in a panel of enzyme activity or radioligand binding assays. The binding inhibition activities of MT-1207 were evaluated by Medicilon.