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Frontiers in Pharmacology of Neurotransmitters pp 381–414Cite as

Pharmacology of Endogenous Opioids, Opiates and Their Receptors

Abstract

The search for analgesia is the main drive for the discovery of opioid receptors and their endogenous ligand peptides. Although opioid peptides are very similar in their N-terminal sequence, they are classified into different types according to their precursor proteins. The peptides activate opioid receptors by binding to orthosteric-binding sites to mediate intracellular second messengers. Biased signaling and allosteric modulation is a new approach to obtain receptor subtype selectivity and separates the desirable from a myriad of unwanted pharmacological effects. This chapter describes endogenous opioids and opiates with an emphasis on structure, origin and processing, receptors, physiological roles, and potential involvement in therapeutic interventions. Further, it also provides a brief discussion on the effect of opioids on various ion channels and recent developments of established and investigational opioid molecules.

Keywords

  • Opioids receptors
  • Endorphin
  • Enkephalin
  • Dynorphin
  • GPCR
  • Neurological disorders
  • Ion channels

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Fig. 12.1
Fig. 12.2
Fig. 12.3

Abbreviations

ACTH:

Adrenocorticotropin

BACE1:

Beta-site APP cleaving enzyme 1

CLIP:

Corticotropin-like intermediate peptide

DOR:

Delta opioid receptor

GPCR:

G protein-coupled receptor

KOR:

Kappa opioid receptor

MOR:

Mu opioid receptor

MSH:

Melanotropins or melanocyte-stimulating hormone

N/OFQ:

Nociceptin/orphanin FQ

OP:

Opioid peptide

OR:

Opioid receptor

ORL-1:

Opioid receptor-like-1

POMC:

Proopiomelanocortin

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Authors and Affiliations

  1. Department of Pharmacy, Al–Noor University College, Mosul, Iraq

    Mohammed Noorladeen Al–Qattan

  2. Department of Pharmaceutical Science, Sushruta School of Medical and Paramedical Sciences, Assam University, Silchar, Assam, India

    Nirupam Das & Rati Kailash Prasad Tripathi

Authors
  1. Mohammed Noorladeen Al–Qattan
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  2. Nirupam Das
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  3. Rati Kailash Prasad Tripathi
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Editor information

Editors and Affiliations

  1. Department of Pharmacology, Central University of Punjab, Bathinda, Punjab, India

    Dr. Puneet Kumar

  2. Department of Pharmaceutical Sciences Faculty of Pharmacy, Philadelphia University, Amman, Jordan

    Dr. Pran Kishore Deb

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Al–Qattan, M.N., Das, N., Tripathi, R.K.P. (2020). Pharmacology of Endogenous Opioids, Opiates and Their Receptors. In: Kumar, P., Deb, P.K. (eds) Frontiers in Pharmacology of Neurotransmitters. Springer, Singapore. https://doi.org/10.1007/978-981-15-3556-7_12

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