Morphine activates the excitatory cingulate cortex–intermediate rostrocaudal division of zona incerta (Cg‐ZIm) pathway to drive hyperlocomotion in mice. Inhibiting the Cg‐ZIm pathway attenuates both acute and chronic morphine‐induced hyperlocomotion, while its activation mimics morphine's motor effects.
Chun‐Yue Li +13 more
wiley +1 more source
PET imaging reveals lower kappa opioid receptor availability in alcoholics but no effect of age
Opioid receptors are implicated in alcoholism, other addictions, withdrawal, and depression, and are considered potential pharmacological targets for treatment. Our goal in the present study was to compare the availability of kappa opioid receptors (KOR)
A. Vijay +7 more
semanticscholar +1 more source
Scalable Production of Highly-Sensitive Nanosensors Based on Graphene Functionalized with a Designed G Protein-Coupled Receptor [PDF]
We have developed a novel, all-electronic biosensor for opioids that consists of an engineered mu opioid receptor protein, with high binding affinity for opioids, chemically bonded to a graphene field-effect transistor to read out ligand binding.
Crook, Alexander +10 more
core +4 more sources
Chronic morphine suppresses Trpc5 in spinal GABAergic interneurons via EZH2‐mediated histone modification, reducing Ca2+ influx and GABA release. TRPC5 activation enhances morphine analgesia, while EZH2 inhibition restores efficacy and reverses tolerance.
Li Wan +9 more
wiley +1 more source
Differential stability of the crystallographic interfaces of mu- and kappa-opioid receptors. [PDF]
The recent mu-opioid receptor (MOPr) and kappa-opioid receptor (KOPr) crystal structures have inspired hypotheses of physiologically relevant dimerization contacts, specifically: a closely packed interface involving transmembrane (TM) helices TM5 and TM6,
Jennifer M Johnston, Marta Filizola
doaj +1 more source
Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors*
Background: Kappa opioid receptor (KOR) signaling may produce antinociception through G protein or dysphoria through βarrestin pathways. Results: Two highly selective, brain penetrant agonist scaffolds bias KOR signaling toward G protein coupling and ...
Lei Zhou +13 more
semanticscholar +1 more source
Placenta ingestion by rats enhances d- and k-opioid antinociception, but suppresses m-opioid antinociception [PDF]
Ingestion of placenta or amniotic fluid produces a dramatic enhancement of centrally mediated opioid antinociception in the rat. The present experiments investigated the role of each opioid receptor type (m, d, k) in the antinociception-modulating ...
DiPirro, Jean M., Kristal, Dr. Mark B.
core
Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
Internalisation of the mu opioid receptor from the surface of cells is generally achieved by receptor occupancy with agonist ligands of high efficacy. However, in many situations the potent analgesic morphine fails to promote internalisation effectively ...
Lopez-Gimenez, J.F., Milligan, G.
core +2 more sources
Characterization and visualization of rat and guinea pig brain kappa opioid receptors: evidence for kappa 1 and kappa 2 opioid receptors. [PDF]
kappa opioid receptors (kappa receptors) have been characterized in homogenates of guinea pig and rat brain under in vitro binding conditions. kappa receptors were labeled by using the tritiated prototypic kappa opioid ethylketocyclazocine under conditions in which mu and delta opioid binding was suppressed. In the case of guinea pig brain membranes, a
R S, Zukin +4 more
openaire +2 more sources
Esketamine and ketamine are widely used for perioperative analgesia and anesthesia. Despite their established roles in analgesia, sedation, and anesthesia, as well as emerging antidepressant, anti‐tumor, and anti‐inflammatory effects, their clinical use is limited due to side effects and addiction potential.
Yinxin Wang +7 more
wiley +1 more source

