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G Protein-Coupled Receptor Genetics pp 347–364Cite as

Novel Mechanisms of G Protein-Coupled Receptor Oligomer and Ion Channel Interactions in Nociception

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Part of the book series: Methods in Pharmacology and Toxicology ((MIPT))

Abstract

G protein-coupled receptors (GPCRs) represent the largest family of cell surface receptors that are involved in regulating several physiological and behavioral responses in organisms. Indeed, over half of all the approved drugs on the market target GPCRs. Over the past 20 years, several lines of evidence have suggested that GPCRs associate to form oligomeric structures that substantially expand the complexity of signaling processes in vivo. In addition, GPCRs have also been shown to functionally regulate ion channels and help fine-tune neurotransmission. In this review, we will discuss recent advances in both mechanisms, with specific focus on opioid receptors, cannabinoid receptors, and transient receptor potential (TRP) calcium channels in nociception. A better understanding of such mechanisms will be imperative in designing analgesics devoid of deleterious side effects and mitigating drug abuse.

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Acknowledgments

I thank Drs. Philip Portoghese and Sonia Das and Mr. Jared Sprague for their constructive comments. The expert assistance of Mr. David Roberson in designing figures is also most appreciated.

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Authors and Affiliations

  1. F.M. Kirby Neurobiology Center, Children’s Hospital Boston and Harvard Medical School, Boston, MA, USA

    Ajay S. Yekkirala

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  1. Ajay S. Yekkirala
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  1. Oklahoma State University, Tulsa, Oklahoma, USA

    Craig W. Stevens

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Yekkirala, A.S. (2014). Novel Mechanisms of G Protein-Coupled Receptor Oligomer and Ion Channel Interactions in Nociception. In: Stevens, C. (eds) G Protein-Coupled Receptor Genetics. Methods in Pharmacology and Toxicology. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-779-2_19

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  • DOI: https://doi.org/10.1007/978-1-62703-779-2_19

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  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-62703-778-5

  • Online ISBN: 978-1-62703-779-2

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