Tilisolol (, 4-[3-(tert-butylamino)- 2-hydroxyproxy]-N-methylisoeabostyril hydrochloride/N-696 ) is a non-selective beta-adrenergic blocking agent, and has a long-lasting and stable action in the clinical treatment of hypertension and angina pectoris. This antihypertensive effect of tilisolol might be largely attributable to its potent beta-adrenergic antagonistic effects. The measurement of the I-V relationship with or without tilisolol excluded the activation of ATP-sensitive K+ current (at least in cardiac muscle) under physiological conditions. However, several investigators suggested that tilisolol has a direct action on smooth muscle cells through ATP-sensitive K+ channels. The possibility that tilisolol has additional effects on the membrane ionic channels of cardiac myocytes under ischemic conditions remains to be tested. It was synthesized by Nisshin Hour Milling Co., Ltd. (Tokyo, Japan)