Nociceptor Signalling through ion Channel Regulation via GPCRs

• Main Authors: Isabella Salzer, Sutirtha Ray, Klaus Schicker, Stefan Boehm
• Format: Article
• Language: English
• Published: MDPI AG 2019-05-01
• Series: International Journal of Molecular Sciences
• Subjects: nociceptor; inflammatory pain; G protein-coupled receptor; voltage-gated ion channel; TRP channel; K_2<i>P</i> channel; Ca²⁺-activated Cl⁻ channel
• Online Access: https://www.mdpi.com/1422-0067/20/10/2488

The prime task of nociceptors is the transformation of noxious stimuli into action potentials that are propagated along the neurites of nociceptive neurons from the periphery to the spinal cord. This function of nociceptors relies on the coordinated operation of a variety of ion channels. In this review, we summarize how members of nine different families of ion channels expressed in sensory neurons contribute to nociception. Furthermore, data on 35 different types of G protein coupled receptors are presented, activation of which controls the gating of the aforementioned ion channels. These receptors are not only targeted by more than 20 separate endogenous modulators, but can also be affected by pharmacotherapeutic agents. Thereby, this review provides information on how ion channel modulation via G protein coupled receptors in nociceptors can be exploited to provide improved analgesic therapy.