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Related Concept Videos

Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+. Activation...
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...

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Constitutively active μ-opioid receptors.

Mark Connor1, John Traynor

  • 1Australian School of Advanced Medicine, Macquarie University, New South Wales, Australia.

Methods in Enzymology
|November 2, 2010
PubMed
Summary

Understanding constitutive activity of the mu-opioid receptor (MOR) is key. New methods reveal distinct active states, aiding the development of safer opioid therapies with fine-tuned effects.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Neuroscience

Background:

  • The mu-opioid receptor (MOR) is a G protein-coupled receptor (GPCR) mediating morphine's effects.
  • Constitutive activity, spontaneous receptor activation, is common in GPCRs.
  • MOR exhibits basal constitutive activity and activity in mutants, with a unique agonist-induced μ*-state.

Purpose of the Study:

  • To outline methods for measuring constitutively active MOR.
  • To explore the pharmacology of different active MOR states.
  • To identify knowledge gaps for improved opioid pharmacotherapy.

Main Methods:

  • Measurement of constitutive MOR activity, including methods utilizing direct coupling to ion channels.
  • Pharmacological characterization of basal, mutant, and μ*-state MOR activity.

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  • Review of existing literature on MOR constitutive activity.

    • Main Results:

    • Established methods for quantifying MOR constitutive activity.
    • Differentiated the pharmacological profiles of basal, mutant, and μ*-state MOR.
    • Highlighted the distinct ligand sensitivity of the μ*-state.

    Conclusions:

    • Constitutive activity at MOR, particularly the μ*-state, plays a role in opioid adaptation and withdrawal.
    • Understanding these states is crucial for developing selective ligands.
    • Fine-tuning opioid pharmacotherapy by targeting specific MOR conformations is a potential future direction.