Connexin channel modulators and their mechanisms of action

• Published in: Neuropharmacology Vol. 75; pp. 517 - 524
• Main Authors: Verselis, Vytas K., Srinivas, Miduturu
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.12.2013
• Subjects: Animals; Connexin; Connexins - antagonists & inhibitors; Connexins - chemistry; Connexins - metabolism; Gap junctions; Gap Junctions - drug effects; Gap Junctions - physiology; Hemichannels; Humans; Ion Channel Gating - drug effects; Ion Channels - drug effects; Ion Channels - physiology; Membrane Transport Modulators - pharmacology; Pharmacology; Connexin; Hemichannels; Pharmacology; Gap junctions
• ISSN: 0028-3908; 1873-7064
• DOI: 10.1016/j.neuropharm.2013.03.020

Gap junction channels and hemichannels formed by the connexin family of proteins play important roles in many aspects of tissue homeostasis in the brain and in other organs. In addition, connexin channels have been proposed as pharmacological targets in the treatment of a number of human disorders. In this review, we describe the connexin-subtype selectivity and specificity of pharmacological agents that are commonly used to modulate connexin channels. We also highlight recent progress made toward identifying new agents for connexin channels that act in a selective and specific manner. Finally, we discuss developing insights into possible mechanisms by which these agents modulate connexin channel function. This article is part of the Special Issue Section entitled ‘Current Pharmacology of Gap Junction Channels and Hemichannels’. •We provide an overview of the pharmacology of connexin channels.•We discuss the selectivity and specificity of commonly used inhibitors.•New methods to discover new modulators are highlighted.•The mechanisms and sites of action of drugs are discussed.