Cicloprolol hydrochloride is a new potent and selective beta 1-adrenoceptor antagonist with partial agonist activity for the study of coronary heart disease.

Cicloprolol, a partial β1-adrenoceptor agonist, is being considered for the treatment of patients with coronary artery disease and impaired left ventricular function[1]. This new β-adrenoceptor partial agonist, Cicloprolol, functions as a β-agonist at normal levels and as a β-antagonist at high levels of adrenergic discharge. The treatment with Cicloprolol is designed to protect the heart against excessive stimulation while maintaining a baseline level of sympathetic drive. Specifically, Cicloprolol exhibits a weak β1-agonistic effect at normal levels of adrenergic discharge and acts as an antagonist at high levels of discharge[2].