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)

Etafenone is an antiarrhythmic and coronary vasodilator drug. Etafenone exerts negative inotropic action on myocardium. It is able to block calcium channels. As a coronary vasodilator which produces a decrease in the heart rate and myocardial oxygen consumption, etafenone has been used in the therapy of ischemic heart disease.

Efonidipine is a 1,4-dihydropyridine derivative for the treatment of hypertension and angina. Efonidipine exerts its antihypertensive and antianginal effects through blocking L- and T-type calcium channels.

Efloxate is a coronary vasodilator developed in 1959 in Italy by Recordati and used for the treatment of angina pectoris. The drug is no longer marketed.

Esatenolol is the (S) enantiomer of atenolol, a beta1-adrenergic receptor antagonist. Only (S)-atenolol, but not (R)-atenolol, contributes to the beta-blocking effect of currently used racemic atenolol since the same effect can be elicited with the (S)-enantiomer alone. Pure (S)-atenolol has been launched in India for the treatment of hypertension and angina pectoris.

Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.

Riodipine is the blocker of calcium channels of L-type. Riodipine is indicated for the treatment of arterial hypertension, prevention of attacks of angina pectoris. Antiepileptic effect of riodipine was manifested by a decreased frequency and amplitude of interictal discharges and a less frequent appearance of ictal discharges. Riodipine increased latency to first convulsive episodes and delayed the development of generalized tonic-clonic seizures. Detected side effects are: arterial hypotension, tachycardia, hypostasis of shins, increase of a daily urine. Allergic reactions to the drug are possible. Nitrates, tricyclic antidepressants, and other anti-hypertensive drugs are able to potentiate of riodipine effects.

Bucumolol is a beta-adrenergic antagonist. It can be used in the treatment of myocardial ischemia and hypertension.

Aranidipine (INN, trade name Sapresta) is a calcium channel blocker. Calcium channel antagonists have become popular medications for the management of hypertension. These agents belong to the diphenylalkylamine, benzothiazepine, dihydropyridine, or tetralol chemical classes. Although the medications share a common pharmacological mechanism in reducing peripheral vascular resistance, clinical differences between the sub-classes can be linked to structural profiles. This heterogeneity is manifested by differences in vascular selectivity, effects on cardiac conduction and adverse events. The lack of differentiation between calcium channel antagonists in clinical trials has contributed to uncertainty associated with their impact on morbidity and mortality. Administartion of aranidipine once daily had a high potent antihypertensive effect and clinical utility in all the clinical trials conducted in Japan. Aranidipine is now under registration.

Gallopamil is a L-type calcium channel blocker designed for the treatment of coronary heart diseases: angina pectoris, prinzmetal angina and hypertonia.