Pharmacological Characteristics and Clinical Applications of K201

Title: Pharmacological Characteristics and Clinical Applications of K201

Volume: 4 Issue: 2

Author(s): Noboru Kaneko, Ryuko Matsuda, Yoshihito Hata and Ken Shimamoto

Affiliation:

Keywords: K201, cardiac ryanodine receptor (RyR2), annexin V, diastolic heart failure, multiple-channel blocker

Abstract: K201 is a 1,4-benzothiazepine derivative that is a promising new drug with a strong cardioprotective effect. We initially discovered K201 as an effective suppressant of sudden cardiac cell death due to calcium overload. K201 is a nonspecific blocker of sodium, potassium and calcium channels, and its cardioprotective effect is more marked than those of nicorandil, prazosine, propranolol, verapamil and diltiazem. Recently, K201 has also been shown to have activities indicated for treatment of atrial fibrillation, ventricular fibrillation, heart failure and ischemic heart disease, including action as a multiple-channel blocker, inhibition of diastolic Ca2+ release from the sarcoplasmic reticulum, suppression of spontaneous Ca2+ sparks and Ca2+ waves, blockage of annexin V and provision of myocardial protection, and improvement of norepinephrine-induced diastolic dysfunction. Here, we describe the pharmacological characteristics and clinical applications of K201.

Cite this article as:

Kaneko Noboru, Matsuda Ryuko, Hata Yoshihito and Shimamoto Ken, Pharmacological Characteristics and Clinical Applications of K201, Current Clinical Pharmacology 2009; 4 (2) . https://dx.doi.org/10.2174/157488409788184972