Pharmacological Modulation and (Patho)Physiological Roles of TRPM4 Channel—Part 1: Modulation of TRPM4

Pharmaceuticals

Csaba Dienes¹  Norbert Szentandrássy¹  Balázs Horváth¹  Zsigmond Máté Kovács¹  János Magyar¹  Tamás Hézső¹  Tamás Bányász¹  János Almássy¹  Péter P. Nánási¹ 

[1] Department of Physiology, Faculty of Medicine, University of Debrecen, 4032 Debrecen, Hungary;

关键词: TRPM4;    SUR1;    CBA;    flufenamic acid;    9-phenanthrol;    siRNA;   

DOI  :  10.3390/ph15010081

来源: DOAJ

【 摘 要 】

Transient receptor potential melastatin 4 is a unique member of the TRPM protein family and, similarly to TRPM5, is Ca²⁺-sensitive and permeable to monovalent but not divalent cations. It is widely expressed in many organs and is involved in several functions by regulating the membrane potential and Ca²⁺ homeostasis in both excitable and non-excitable cells. This part of the review discusses the pharmacological modulation of TRPM4 by listing, comparing, and describing both endogenous and exogenous activators and inhibitors of the ion channel. Moreover, other strategies used to study TRPM4 functions are listed and described. These strategies include siRNA-mediated silencing of TRPM4, dominant-negative TRPM4 variants, and anti-TRPM4 antibodies. TRPM4 is receiving more and more attention and is likely to be the topic of research in the future.

【 授权许可】

Unknown