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Nicotinic Receptors as Targets for Novel Analgesics and Anti-inflammatory Drugs

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Nicotinic Receptors

Part of the book series: The Receptors ((REC,volume 26))

Abstract

Nicotine and nicotinic receptors have been explored for the past three decades as a strategy for pain control. These receptors are widely expressed throughout the central and peripheral nervous system as well as immune cells. Despite encouraging results with many selective α4β2* agonists in animal models of pain, human studies showed a narrow therapeutic window between analgesic efficacy and toxicity is associated with the use of these agonists as analgesics. α4β2 positive allosteric modulators are being developed with the aim to increase the potency or therapeutic window of these agonists. However, several recent developments have potentially opened new windows of opportunity in the use of nicotinic agents for analgesia. Accumulating evidences suggest that α7 agonists and positive allosteric modulators hold a lot of promise in the treatment of chronic inflammatory pain conditions. In addition, recent animal studies suggest the therapeutic potential of ligands acting at other subtypes of nicotinic receptors. The current review will attempt to highlight these recent developments and outline some important findings that demonstrate further potential for the development of nicotinic ligands as novel analgesics.

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Abbreviations

nAChRs:

Nicotinic acetylcholine receptors

CNS:

Central nervous system

PAM:

Positive allosteric modulator

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Acknowledgements

Participants in this research review are supported by the National Institutes of Health (NIH) and The Scientific and Technological Research Council of Turkey (TUBITAK).

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Authors and Affiliations

  1. Department of Pharmacology & Toxicology, Virginia Commonwealth University School of Medicine, 1220 East Broad Street, Molecular Medical Research Building, Richmond, VA, 23298, USA

    M. Imad Damaj Ph.D. & Kelen Freitas

  2. Experimental Animals Breeding and Research Center, Faculty of Medicine, Uludag University, Bursa, Turkey

    Deniz Bagdas Ph.D.

  3. Department of Anesthesia and Perioperative Care, University of California at San Francisco, San Francisco, CA, USA

    Pamela Flood M.D.

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  1. M. Imad Damaj Ph.D.
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  2. Kelen Freitas
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  3. Deniz Bagdas Ph.D.
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  4. Pamela Flood M.D.
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Corresponding author

Correspondence to M. Imad Damaj Ph.D. .

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Editors and Affiliations

  1. Department of Neurobiology SHEL 1006, University of Alabama at Birmingham, Birmingham, Alabama, USA

    Robin A.J. Lester

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Damaj, M.I., Freitas, K., Bagdas, D., Flood, P. (2014). Nicotinic Receptors as Targets for Novel Analgesics and Anti-inflammatory Drugs. In: Lester, R. (eds) Nicotinic Receptors. The Receptors, vol 26. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-1167-7_12

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