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Related Experiment Video

Updated: May 18, 2026

The Muscle Cuff Regenerative Peripheral Nerve Interface for the Amplification of Intact Peripheral Nerve Signals
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The Muscle Cuff Regenerative Peripheral Nerve Interface for the Amplification of Intact Peripheral Nerve Signals

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Orphan GPCRs and neuromodulation.

Olivier Civelli1

  • 1Department of Pharmacology, University of California, Irvine, Irvine, CA 92697-4625, USA. ocivelli@uci.edu

Neuron
|October 9, 2012
PubMed
Summary

Discovering novel neuromodulators from orphan G protein-coupled receptors (GPCRs) has significantly advanced our understanding of brain functions, including sleep, obesity, and feeding behaviors. These findings offer new therapeutic targets for higher brain functions and psychiatric disorders.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Many G protein-coupled receptors (GPCRs) were initially identified as 'orphan' receptors without known ligands.
  • The identification of ligands for orphan GPCRs has revealed diverse neuroreceptor families and functions.
  • Orphan GPCRs serve as crucial targets for discovering novel neuromodulators.

Purpose of the Study:

  • To provide an overview of how novel neuropeptides, discovered through orphan GPCR research, have expanded our understanding of brain function.
  • To discuss the impact of these discoveries on key physiological processes such as sleep/wakefulness, obesity, and feeding.
  • To explore broader implications of orphan GPCR studies, including neuromodulator specificity and receptor sensing mechanisms.

Main Methods:

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  • Review of existing literature on orphan GPCRs and their cognate ligands.
  • Analysis of the impact of newly identified neuropeptides on physiological responses.
  • Discussion of conceptual advances in neuromodulation derived from orphan GPCR research.

    • Main Results:

    • Novel neuropeptides have elucidated complex regulatory roles in sleep/wakefulness, obesity, and feeding behaviors.
    • Orphan GPCR studies have advanced concepts like neuromodulator specificity and the role of receptors as sensors.
    • These discoveries have significantly broadened the understanding of brain function and neuroreceptor families.

    Conclusions:

    • The study of orphan GPCRs has been pivotal in uncovering the diversity of neuromodulation.
    • Newly discovered neuromodulators offer profound insights into fundamental brain processes.
    • Future research on these modulators may unlock understanding of higher brain functions and psychiatric disorders.