Article
The small molecule GAT1508 activates brain-specific GIRK1/2 channel heteromers and facilitates conditioned fear extinction in rodents.
The Journal of biological chemistry - 13 Mar 2020
Xu Yu, Cantwell Lucas, Molosh Andrei I, Plant Leigh D, Gazgalis Dimitris, Fitz Stephanie D, Dustrude Erik T, Yang Yuchen, Kawano Takeharu, Garai Sumanta, Noujaim Sami F, Shekhar Anantha, Logothetis Diomedes E, Thakur Ganesh A
Abstract excerpt
G-protein-gated inwardly-rectifying K+ (GIRK) channels are targets of Gi/o-protein-signaling systems that inhibit cell excitability. GIRK channels exist as homotetramers (GIRK2 and GIRK4) or heterotetramers with nonfunctional homomeric subunits (GIRK1 and GIRK3). Although they have been implicated in multiple conditions, the lack of selective GIRK drugs that discriminate among the different GIRK channel subtypes...
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