Pharmacology of pannexin channels

Pannexin channels play fundamental roles in regulating inflammation and have been implicated in many diseases including hypertension, stroke, and neuropathic pain. Thus, the ability to pharmacologically block these channels is a vital component of several therapeutic approaches. Pharmacologic interrogation of model systems also provides a means to discover new roles for pannexins in cell physiology. Here, we review the state of the art for agents that can be used to block pannexin channels, with a focus on chemical pharmaceuticals and peptide mimetics that act on pannexin 1. Guidance on interpreting results obtained with pannexin pharmacologics in experimental systems is discussed, as well as strengths and caveats of different agents, including specificity and feasibility of clinical application.

Automated summary

Pannexin channels have important roles in regulating inflammation and are associated with various diseases. Blocking these channels pharmacologically is crucial for therapeutic approaches. This review discusses the current state of agents that can block pannexin channels, focusing on pharmaceuticals and peptide mimetics targeting pannexin 1. It also provides guidance on interpreting results obtained with pannexin pharmacologics and evaluates the strengths and limitations of different agents in terms of specificity and clinical application.