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• W1863094966 abstract "Abstract Opioid receptors can display spontaneous agonist‐independent G‐protein signaling (basal signaling/constitutive activity). While constitutive κ‐opioid receptor ( KOR ) activity has been documented in vitro , it remains unknown if KOR s are constitutively active in native systems. Using [ 35 S] guanosine 5′‐O‐[gamma‐thio] triphosphate coupling assay that measures receptor functional state, we identified the presence of medial prefrontal cortex KOR constitutive activity in young rats that declined with age. Furthermore, basal signaling showed an age‐related decline and was insensitive to neutral opioid antagonist challenge. Collectively, the present data are first to demonstrate age‐dependent alterations in the medial prefrontal cortex KOR constitutive activity in rats and changes in the constitutive activity of KOR s can differentially impact KOR ligand efficacy. These data provide novel insights into the functional properties of the KOR system and warrant further consideration of KOR constitutive activity in normal and pathophysiological behavior. image Opioid receptors exhibit agonist‐independent constitutive activity; however, kappa‐opioid receptor (KOR) constitutive activity has not been demonstrated in native systems. Our results confirm KOR constitutive activity in the medial prefrontal cortex (mPFC) that declines with age. With the ability to presynaptically inhibit multiple neurotransmitter systems in the mPFC, maturational or patho‐logical alterations in constitutive activity could disrupt corticofugal glutamatergic pyramidal projection neurons mediating executive function. Regulation of KOR constitutive activity could serve as a therapeutic target to treat compromised executive function." @default.
• W1863094966 created "2016-06-24" @default.
• W1863094966 creator A5070108106 @default.
• W1863094966 creator A5082244326 @default.
• W1863094966 date "2015-09-11" @default.
• W1863094966 modified "2023-10-03" @default.
• W1863094966 title "Maturational alterations in constitutive activity of medial prefrontal cortex kappa-opioid receptors in Wistar rats" @default.
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• W1863094966 doi "https://doi.org/10.1111/jnc.13279" @default.
• W1863094966 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4636924" @default.
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