Presynaptic receptors

Richard J. Miller*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

269 Scopus citations


Activation of different types of G-protein-linked and ionotropic presynaptic receptors has been shown to regulate neurotransmitter release throughout the central and peripheral nervous systems. In the case of G- protein-linked receptors, three major mechanisms have been suggested: (a) inhibition of Ca channels in the nerve terminal; (b) the activation of presynaptic K channels, resulting in a reduction in the effectiveness of the action potential; and (c) direct modulation of one or more components of the neurotransmitter vesicle release apparatus. In the case of ionotropic presynaptic receptors, inhibition of release may be achieved through depolarization of the terminal and inactivation of Na and Ca channels. Activation of presynaptic ionotropic receptors that are appreciably Ca permeable can also enhance the release of transmitters as a result of their ability to raise [Ca], in the terminal directly. Many transmitters employ several of these mechanisms, thus allowing considerable flexibility in the presynaptic regulation of transmitter release.

Original languageEnglish (US)
Pages (from-to)201-227
Number of pages27
JournalAnnual Review of Pharmacology and Toxicology
StatePublished - 1998


  • Ca channels
  • G proteins
  • Ionotropic receptors
  • Potassium channels
  • Transmitter release

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology


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