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Drug Development pp 203–238Cite as

Opioid Receptors

Targets for New Gastrointestinal Drug Development

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Abstract

For centuries, opium and its derivatives have been used for both therapeutic and recreational purposes. One such derivative, morphine, is still one of the most used analgesics. Besides a predominant role in pain control (both somatic and visceral pain), opioids and opioid receptors have a broad spectrum of actions, including modulations of reinforcement and reward pathways, neurotransmitter release, neuroendocrine functions, as well as gastrointestinal (GI) motility, transit, and secretion. The opioid drugs made available, or clinically tested as analgesics, have essentially targeted µ- and κ-receptors in the central nervous system (CNS). The development and use of such compounds have been limited or even discontinued because of their side effects (constipation, respiratory depression, addiction potential, and/or aversion). Only peripherally acting µ-agonists have been approved for therapeutic use in gastroenterology.

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Authors
  1. Pierre J. M. Rivière
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  2. Jean-Louis Junien
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Editors and Affiliations

  1. School of Pharmacy, University of Wisconsin, Madison, WI, USA

    Timothy S. Gaginella

  2. Parke-Davis Pharmaceutical Research Division, Ann Arbor, MI, USA

    Antonio Guglietta

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Rivière, P.J.M., Junien, JL. (2000). Opioid Receptors. In: Gaginella, T.S., Guglietta, A. (eds) Drug Development. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-202-9_8

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  • DOI: https://doi.org/10.1007/978-1-59259-202-9_8

  • Publisher Name: Humana Press, Totowa, NJ

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