Characterization of opioid receptors in the Mongolian gerbil cerebellum. 1994

M Niwa, and T Iwai, and A E Luay, and M Nozaki, and K Tsurumi
Department of Pharmacology, Gifu University School of Medicine, Japan.

Characteristics of opioid receptors binding in the Mongolian gerbil cerebellum were determined by in vitro radioligand binding technique. Homogenate of cerebellar membranes possessed a binding capacity for 3H-DAMGO, a mu-agonist, and for 3H-diprenorphine, an antagonist of mu, delta and kappa-receptors. These bindings were saturable, and characterized by high affinity (Kd values: 1.55 +/- 0.43 nM for 3H-DAMGO and 0.56 +/- 0.20 nM for 3H-diprenorphine) and high density (Bmax: 127.8 +/- 23.8 fmoles/mg protein for 3H-DAMGO and 135.8 +/- 9.03 fmoles/mg protein for 3H-diprenorphine). Autoradiographically, the binding sites were predominantly located in the molecular layer of the cerebellum. 3H-DPDPE, a delta-agonist, showed only very small binding capacity to the cerebellar membranes. The kappa-agonist, 3H-U-69593, also showed very small binding capacity to the cerebellar membranes except in the early postnatal period. Thus, the gerbil cerebellum can be considered as a tissue containing a homogeneous population of mu-opioid receptors.

UI MeSH Term Description Entries
D009294 Narcotics Agents that induce NARCOSIS. Narcotics include agents that cause somnolence or induced sleep (STUPOR); natural or synthetic derivatives of OPIUM or MORPHINE or any substance that has such effects. They are potent inducers of ANALGESIA and OPIOID-RELATED DISORDERS. Analgesics, Narcotic,Narcotic Analgesics,Narcotic,Narcotic Effect,Narcotic Effects,Effect, Narcotic,Effects, Narcotic
D011759 Pyrrolidines Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH. Tetrahydropyridine,Tetrahydropyridines
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011957 Receptors, Opioid Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known. Endorphin Receptors,Enkephalin Receptors,Narcotic Receptors,Opioid Receptors,Receptors, Endorphin,Receptors, Enkephalin,Receptors, Narcotic,Receptors, Opiate,Endorphin Receptor,Enkephalin Receptor,Normorphine Receptors,Opiate Receptor,Opiate Receptors,Opioid Receptor,Receptors, Normorphine,Receptors, beta-Endorphin,beta-Endorphin Receptor,Receptor, Endorphin,Receptor, Enkephalin,Receptor, Opiate,Receptor, Opioid,Receptor, beta-Endorphin,Receptors, beta Endorphin,beta Endorphin Receptor,beta-Endorphin Receptors
D002531 Cerebellum The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills. Cerebella,Corpus Cerebelli,Parencephalon,Cerebellums,Parencephalons
D004174 Diprenorphine A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine. Diprenorphine Hydrochloride,Revivon,Hydrochloride, Diprenorphine
D004745 Enkephalins One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla. Enkephalin
D005849 Gerbillinae A subfamily of the Muridae consisting of several genera including Gerbillus, Rhombomys, Tatera, Meriones, and Psammomys. Gerbils,Jird,Meriones,Psammomys,Rats, Sand,Gerbil,Jirds,Merione,Rat, Sand,Sand Rat,Sand Rats
D006165 Guanylyl Imidodiphosphate A non-hydrolyzable analog of GTP, in which the oxygen atom bridging the beta to the gamma phosphate is replaced by a nitrogen atom. It binds tightly to G-protein in the presence of Mg2+. The nucleotide is a potent stimulator of ADENYLYL CYCLASES. GMP-PNP,GMP-P(NH)P,Gpp(NH)p,Guanosine 5'-(Beta,Gamma-Imido)Triphosphate,Guanyl-5'-Imidodiphosphate,P(NH)PPG,Guanyl 5' Imidodiphosphate,Imidodiphosphate, Guanylyl
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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