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Behavioral Pharmacology of Drugs Acting at Mu Opioid Receptors

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Substance Use Disorders

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 258))

Abstract

Despite the therapeutic utility of opioids for relieving pain, other behavioral effects, including their potential for abuse and overdose, can be quite detrimental to individuals as well as society and have contributed to the ongoing opioid crisis. The dramatic escalation in overdose deaths over the last 15 years was initially driven by abuse of prescription opioids, although abuse of heroin, fentanyl, and fentanyl analogs has been increasing, largely due to increased availability and lower cost compared with prescription opioids. All of these opioids share pharmacological properties, acting as agonists at mu opioid receptors, and produce similar behavioral effects, including abuse-related, pain-relieving, dependence-producing, and respiratory-depressant effects. Despite their similarities, opioids are not pharmacologically identical. In fact, drugs that act at mu opioid receptors, including abused opioids, can vary on a number of dimensions, including pharmacological efficacy, drug-receptor interactions, receptor selectivity, and pharmacokinetics. Overall, these differences impact behavioral effects of drugs acting at mu opioid receptors, and this chapter describes variations in those behavioral effects and how these differences continue to provide new strategies that can be developed to address the ongoing opioid epidemic.

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Acknowledgments

This work was supported by the National Institutes of Health, National Institute on Drug Abuse [Grants R01 DA005018, R01 DA048417, and R21 DA 046805], and the Welch Foundation [Grant AQ-0039]. The authors have no conflict of interest. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health or the National Institute on Drug Abuse.

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Authors and Affiliations

  1. Department of Pharmacology, University of Texas Health Science Center at San Antonio, San Antonio, TX, USA

    Lisa R. Gerak, David R. Maguire & Charles P. France

  2. Addiction Research, Treatment and Training Center of Excellence, University of Texas Health Science Center at San Antonio, San Antonio, TX, USA

    Lisa R. Gerak, David R. Maguire & Charles P. France

  3. Department of Psychiatry, University of Texas Health Science Center at San Antonio, San Antonio, TX, USA

    Charles P. France

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  1. Lisa R. Gerak
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  2. David R. Maguire
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  3. Charles P. France
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Correspondence to Charles P. France .

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Editors and Affiliations

  1. Wake Forest School of Medicine, Winston-Salem, NC, USA

    Michael A. Nader

  2. Addiction Institute of Mount Sinai, Icahn School of Medicine at Mount Sinai, New York, NY, USA

    Yasmin L. Hurd

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Gerak, L.R., Maguire, D.R., France, C.P. (2019). Behavioral Pharmacology of Drugs Acting at Mu Opioid Receptors. In: Nader, M., Hurd, Y. (eds) Substance Use Disorders. Handbook of Experimental Pharmacology, vol 258. Springer, Cham. https://doi.org/10.1007/164_2019_265

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