receptor and channel heteromers as pain targets受体和通道heteromers痛苦的目标.pdfVIP

Pharmaceuticals 2012, 5, 249-278; doi:10.3390/ph5030249 OPEN ACCESS Pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals Review Receptor and Channel Heteromers as Pain Targets Kelly A. Berg 1, Amol M. Patwardhan 2 and Armen N. Akopian 1,3,* 1 Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, TX 78229, USA; E-Mail: berg@ (K.A.B.) 2 Department of Anesthesiology, Arizona Health Sciences Center, Tucson, AZ 85724, USA; E-Mail: amol.arizona@ (A.M.P.) 3 Department of Endodontics, University of Texas Health Science Center at San Antonio, San Antonio, TX 78229, USA * Author to whom correspondence should be addressed; E-Mail: akopian@; Tel.: +1-210-567-6668. Received: 4 January 2012; in revised form: 4 February 2012 / Accepted: 15 February 2012 / Published: 23 February 2012 Abstract: Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on such unique properties to augment therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting heteromers may have greater tissue specificity and analgesic efficacy. This review will focus on current progress in our understanding of rol