Referenced in: none

Automatically associated channels: Kv1.4 , Slo1

Title: G protein-coupled receptor kinase mediates desensitization of norepinephrine-induced Ca2+ channel inhibition.

Authors: M Diversé-Pierluissi, J Inglese, R H Stoffel, R J Lefkowitz, K Dunlap

Journal, date & volume: Neuron, 1996 Mar , 16, 579-85

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/8785055

Abstract
G protein-coupled receptors are essential signaling molecules at sites of synaptic transmission. Here, we explore the mechanisms responsible for the use-dependent termination of metabotropic receptor signaling in embryonic sensory neurons. We report that the inhibition of voltage-dependent Ca2+ channels mediated by alpha2-adrenergic receptors desensitizes slowly with prolonged exposure to the transmitter and that the desensitization is mediated by a G protein-coupled receptor kinase (GRK). Intracellular introduction of recombinant, purified kinases or synthetic blocking peptides into individual neurons demonstrates the specific involvement of a GRK3-like protein. These results suggest that GRK-mediated termination of receptor-G protein coupling is likely to regulate synaptic strength and, as such, may provide one effective mechanism for depression of synaptic transmission.