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Pharmaceuticals 2012, 5(3), 249-278; doi:10.3390/ph5030249

Receptor and Channel Heteromers as Pain Targets

, 2
 and 1,3,*
Received: 4 January 2012 / Revised: 4 February 2012 / Accepted: 15 February 2012 / Published: 23 February 2012
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
View Full-Text   |   Download PDF [287 KB, uploaded 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 roles of heteromeric GPCRs and channels in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric receptors and channels. This approach may be instrumental in the discovery of novel classes of drugs and expand our repertoire of targets for pain pharmacotherapy.
Keywords: pain; receptors; channels; sensory neurons; heteromers pain; receptors; channels; sensory neurons; heteromers
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Berg, K.A.; Patwardhan, A.M.; Akopian, A.N. Receptor and Channel Heteromers as Pain Targets. Pharmaceuticals 2012, 5, 249-278.

AMA Style

Berg KA, Patwardhan AM, Akopian AN. Receptor and Channel Heteromers as Pain Targets. Pharmaceuticals. 2012; 5(3):249-278.

Chicago/Turabian Style

Berg, Kelly A.; Patwardhan, Amol M.; Akopian, Armen N. 2012. "Receptor and Channel Heteromers as Pain Targets." Pharmaceuticals 5, no. 3: 249-278.

Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert