biostudies-literatureZhou YNIAAA NIH HHS136092https://www.ebi.ac.uk/biostudies/studies/S-EPMC8355176biostudies-literatureUnknown760Though it is well known that G protein-coupled receptor kinase 2 [GRK2] is involved in regulation of mu opioid receptor [MOR] desensitization and morphine-related behaviors, the potential role of GRK2 in regulation of kappa opioid receptor [KOR] functions in vivo has not been established yet. A couple of recent studies have found that GRK2 activity desensitizes KOR functions via decreasing G protein-coupled signaling with sensitizing arrestin-coupled signaling. Nalfurafine, a G protein-biased KOR full agonist, produces an inhibitory effect on alcohol intake in mice, with fewer side effects (sedation, aversion, or anxiety/depression-like behaviors). Using RNA sequencing (RNA-seq) analysis, we first identified that nuclear transcript level of grk2 [adrbk1] (but not other grks) was significanNeuroscience lettersInvolvement of GRK2 in modulating nalfurafine-induced reduction of excessive alcohol drinking in mice.PMC8355176R03 AA021970Liang YZhou YfalseInvolvement of GRK2 in modulating nalfurafine-induced reduction of excessive alcohol drinking in mice.Though it is well known that G protein-coupled receptor kinase 2 [GRK2] is involved in regulation of mu opioid receptor [MOR] desensitization and morphine-related behaviors, the potential role of GRK2 in regulation of kappa opioid receptor [KOR] functions in vivo has not been established yet. A couple of recent studies have found that GRK2 activity desensitizes KOR functions via decreasing G protein-coupled signaling with sensitizing arrestin-coupled signaling. Nalfurafine, a G protein-biased KOR full agonist, produces an inhibitory effect on alcohol intake in mice, with fewer side effects (sedation, aversion, or anxiety/depression-like behaviors). Using RNA sequencing (RNA-seq) analysis, we first identified that nuclear transcript level of grk2 [adrbk1] (but not other grks) was significan2021-01-01T00:00:00Z2021 Aug2025-04-27T01:47:55.119Z2025-04-06T18:20:44.389ZS-EPMC83551763419790510.1016/j.neulet.2021.136092