The kappa opioid receptor (KOR) has numerous important roles in the nervous system including the modulation of mood, reward, pain, and itch. In addition, KOR is expressed in many non-neuronal tissues. However, the specific cell types that express KOR are poorly characterized. Here, we report the development of a KOR-Cre knockin allele, which provides genetic access to cells that express KOR. In this mouse, Cre recombinase (Cre) replaces the initial coding sequence of the Opkr1 gene (encoding the kappa opioid receptor). We demonstrate that the KOR-Cre allele mediates recombination by embryonic day 14.5 (E14.5). Within the brain, KOR-Cre shows expression in numerous areas including the cerebral cortex, nucleus accumbens and striatum. In addition, this allele is expressed in epithelium and throughout many regions of the body including the heart, lung, and liver. Finally, we reveal that KOR-Cre mediates recombination of a subset of bipolar and amacrine cells in the retina. Thus, the KOR-Cre mouse line is a valuable new tool for conditional gene manipulation to enable the study of KOR.
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http://dx.doi.org/10.1002/dvg.22910 | DOI Listing |
Neuropharmacology
January 2025
Center for Substance Abuse Research, Lewis Katz School of Medicine, Temple University, Philadelphia, PA, USA. Electronic address:
Akuammicine (AKC), an indole alkaloid, is a kappa opioid receptor (KOR) full agonist with a moderate affinity. 10-Iodo-akuammicine (I-AKC) and 10-Bromo-akuammicine (Br-AKC) showed higher affinities for the KOR with K values of 2.4 and 5.
View Article and Find Full Text PDFNeurosci Biobehav Rev
January 2025
Department of Nutrition and Health, Beijing Advanced Innovation Center for Food Nutrition and Human Health, China Agricultural University, Beijing, China; Beijing Life Science Academy, Beijing, China. Electronic address:
Nicotine, a neuroactive substance in tobacco products, has been widely studied for its effects on feeding and body weight, mostly focusing on the involvement of nervous system, metabolism, hormones, and gut microbiota. To elucidate the action mechanism of nicotine on feeding and body weight, especially the underlying neurobiological mechanisms, we reviewed the studies on nicotine's effects on feeding and body weight by the regulation of various nerve systems, energy expenditure, peripheral hormones, gut microbiota, etc. The role of neuronal signaling molecules such as AMP-activated protein kinase (AMPK) and kappa opioid receptor (κOR) were specialized in the nicotine-regulating energy expenditure.
View Article and Find Full Text PDFExpert Rev Clin Pharmacol
January 2025
Department of Medical Cosmetology, Hunan Provincial Hospital of Maternal and Child Health Care, Changsha, China.
Background: Anrikefon (HSK21542), a potent and selective peripheral kappa opioid receptor (KOR) agonist developed by Haisco, effectively blocks pain and itch signals.
Aim: To develop a population pharmacokinetic (PK) model for anrikefon and conduct exposure-response (E-R) analysis for safety and efficacy in postoperative pain patients.
Method: The Population PK analysis uses NONMEM software with data from six trials.
Br J Anaesth
January 2025
Department of Anesthesiology and Critical Care Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA; Department of Anesthesiology, Weill Cornell Medicine, New York, NY, USA. Electronic address:
The publisher regrets that this article has been temporarily removed. A replacement will appear as soon as possible in which the reason for the removal of the article will be specified, or the article will be reinstated. The full Elsevier Policy on Article Withdrawal can be found at https://www.
View Article and Find Full Text PDFNat Chem Biol
January 2025
The Bridge Institute, Michelson Center for Convergent Biosciences, University of Southern California, Los Angeles, CA, USA.
Opioid receptors, a subfamily of G protein-coupled receptors (GPCRs), are key therapeutic targets. In the canonical GPCR activation model, agonist binding is required for receptor-G protein complex formation, while antagonists prevent G protein coupling. However, many GPCRs exhibit basal activity, allowing G protein association without an agonist.
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