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Updated: Jul 9, 2026
09:49
Brain Membrane Fractionation: An Ex Vivo Approach to Assess Subsynaptic Protein Localization
Published on: May 12, 2017
Presynaptic neuropeptide receptors.
1Institut für Pharmakologie und Toxikologie, Rheinische Friedrich-Wilhelms-Universität, Reuterstrasse 2b, 53113 Bonn, Germany. e.schlicker@uni-bonn.de
Handbook of Experimental Pharmacology
|December 8, 2007
Summary
This study explores presynaptic neuropeptide receptors, including opioids, neuropeptide Y, ACTH, and orexins, detailing their roles in neurotransmitter release and therapeutic potential.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Presynaptic receptors modulate neurotransmitter release in the central and peripheral nervous systems.
- Four key neuropeptide families—opioids, neuropeptide Y, adrenocorticotropic hormone (ACTH), and orexins—interact with presynaptic receptors.
Purpose of the Study:
- To review the function and signaling mechanisms of presynaptic receptors for opioids, neuropeptide Y, ACTH, and orexins.
- To discuss the therapeutic implications of targeting these presynaptic receptors.
Main Methods:
- Literature review of studies on presynaptic neuropeptide receptors.
- Analysis of receptor coupling, downstream signaling pathways, and effects on neurotransmitter release.
Main Results:
- Opioid and neuropeptide Y receptors inhibit neurotransmitter release via G(i/o) proteins, affecting Ca(2+) and K(+) channels.
- ACTH receptors (MC(2)) in cardiovascular tissues facilitate noradrenaline release via G(s) and adenylyl cyclase.
- Orexin receptors (OX(2)) in the brain facilitate glutamate and GABA release, likely involving G(q) and vesicle machinery.
Conclusions:
- Presynaptic opioid receptors contribute to therapeutic effects of related drugs.
- Targeting presynaptic neuropeptide Y, ACTH, and orexin receptors represents potential therapeutic avenues, though drugs are not yet available.
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