Human μ opiate receptor
FEBS LettersPublished 31 January 1994Open access
Jia-Bei Wang, Peter S. Johnson, Antonio M. Persico, Anita L. Hawkins, Constance A. Griffin, George R. Uhl
Citations290
SJR quartileQ1
SJR score1.22
SNIP0.77
Generate an AI Snapshot to get a quick, structured summary of this paper.
Study Snapshot
ObjectiveStudy objective
MethodsResearch methodology
PopulationPopulation studied
Sample sizeSample sizes
OutcomesStudy outcomes here
ResultsStudy results comes here
LimitationsResearch study limitations comes here
A concise AI-generated summary of the paper will appear here once you click Generate AI Snapshot.
TL;DR
Analysis of hybridization to DNA prepared from human rodent hybrid cell lines and chromosomal in situ hybridization studies indicate localization to 6q24-25, which may prove useful in assessing this gene's involvement in neuropsychiatric disorders involving opiatergic systems.
Abstract
A human mu opiate receptor cDNA has been identified from a cerebral cortical cDNA library using sequences from the rat mu opiate receptor cDNA. The human mu opiate receptor (h mu OR1) shares 95% amino acid identity with the rat sequence. The expressed mu OR1 recognized tested opiate drugs and opioid peptides in a sodium- and GTP-sensitive fashion with affinities virtually identical to those displayed by the rat mu opiate receptor. Effects on cyclic AMP are similar to those noted for the rat mu opiate receptor. An 18 kb genomic clone hybridizing with the h mu OR1 cDNA contains 63 and 489 bp exonic sequences flanked by splice donor/acceptor sequences. Analysis of hybridization to DNA prepared from human rodent hybrid cell lines and chromosomal in situ hybridization studies indicate localization to 6q24-25. An MspI polymorphism, producing a 3.7 kb band, may prove useful in assessing this gene's involvement in neuropsychiatric disorders involving opiatergic systems.
Keywords
NeuroscienceBiochemistry, Genetics and Molecular Biology
Nucleic Acids ResearchA comprehensive set of sequence analysis programs for the VAX
14,423 Citations1984John Devereux, Paul Haeberli +1 more
A group of programs that will interact with each other has been developed for the Digital Equipment Corporation VAX computer using the VMS operating system.
Medical Entomology and ZoologyPsychopharmacology: The Fourth Generation of Progress
2,988 Citations1995Floyd E. Bloom, David J. Kupfer
Journal of Pharmacology and Experimental TherapeuticsThe effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.
2,976 Citations1976W R Martin, C. G. Eades +3 more
It has been shown that buprenorphine is a partial agonist of the mu type which both suppressed and precipitated abstinence in the morphine-dependent dog while morphine and propoxyphene are stronger agonists.
NatureEndogenous opioid peptides: multiple agonists and receptors
2,482 Citations1977John A.H. Lord, Angela A. Waterfield +2 more
It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.
ScienceHigh-Resolution Mapping of Human Chromosome 11 by in Situ Hybridization with Cosmid Clones
1,344 Citations1990Peter Lichter, Chieh-Ju C. Tang +5 more
The results demonstrate the feasibility of rapidly producing high-resolution maps of human chromosomes by in situ hybridization and show that by hybridizing three or more cosmids simultaneously, gene order on the chromosome could be established unequivocally.
ScienceCloning of a Delta Opioid Receptor by Functional Expression
1,225 Citations1992Christopher J. Evans, Duane E. Keith +3 more
A complementary DNA clone encoding a functional delta opioid receptor has been identified and shows homology to G protein-coupled receptors, in particular the receptors for somatostatin, angiotensin, and interleukin-8.
Proceedings of the National Academy of SciencesThe delta-opioid receptor: isolation of a cDNA by expression cloning and pharmacological characterization.
1,003 Citations1992Brigitte L. Kieffer, Katia Befort +2 more
A random primed expression cDNA library was constructed from the RNA of NG 108-15 cells that encodes a 371-amino acid-residue protein presenting all the structural characteristics of receptors that interact with guanine nucleotide-binding proteins.
PainAutoradiographic differentiation of mu, delta and kappa opioid receptors in the rat forebrain and midbrain
980 Citations1988Alfred Mansour, Henry Khachaturian +3 more
The distributions of the mu, delta, and kappa opioid receptor subtypes in the rat forebrain and midbrain using in vitro autoradiography support the existence of at least 3 distinct opioid receptors with possibly separate functional roles.
Regulatory PeptidesMolecular cloning and functional expression of a mu opioid receptor from rat brain
810 Citations1994Yan Chen, Anton Mestek +3 more
Hydropathy analysis of the deduced protein exhibits seven hydrophobic domains typical of G protein-coupled receptors, which shows high homologies at the amino acid sequence level with the published mouse δ opioid receptor and a rat brain κ opioid receptor.
Proceedings of the National Academy of SciencesCloning and functional comparison of kappa and delta opioid receptors from mouse brain.
619 Citations1993Kazuki Yasuda, K Raynor +5 more
RNA blotting studies and in situ hybridization histochemistry showed that kappa opioid receptor mRNA was expressed at high levels in brain in the neocortex, hippocampus, amygdala, medial habenula, hypothalamus, locus ceruleus, and parabrachial nucleus, suggesting that this receptor may play a role in arousal and regulation of autonomic and neuroendocrine functions.
Archives of General PsychiatryHeterogeneity in the Inheritance of Alcoholism
488 Citations1991Roy W. Pickens
Genetic influence on risk for alcoholism was examined in a US treatment sample of 50 monozygotic (MZ) and 64 dizygotic (DZ) male and 31 MZ and 24 DZ female same-sex twin pairs, suggesting forms of alcoholism that may be moderately to highly heritable.
Proceedings of the National Academy of SciencesDifferentiation of delta and mu opiate receptor localizations by light microscopic autoradiography.
464 Citations1980Robert Goodman, Solomon H. Snyder +2 more
It is proposed that mu and delta receptors are respectively the physiologic receptors for [Met]- and [Leu]enkephalin neurons.
Proceedings of the National Academy of Sciencesmu opiate receptor: cDNA cloning and expression.
409 Citations1993J B Wang, Yasuo Imai +4 more
A 2.1-kb rat brain cDNA whose predicted translation product displays 63% identity with recently described delta and kappa opiate receptor sequences was identified through polymerase chain reaction and cDNA homology approaches.
Proceedings of the National Academy of SciencesNeuroanatomical patterns of the mu, delta, and kappa opioid receptors of rat brain as determined by quantitative in vitro autoradiography.
381 Citations1987Ann Tempel, R. Suzanne Zukin
The present study concludes that delta receptors occur at high density only in the forebrain and in two midbrain structures, whereas mu and kappa receptors exhibit discrete patterns in most major brain regions.
Proceedings of the National Academy of SciencesClassification of multiple morphine and enkephalin binding sites in the central nervous system.
372 Citations1981Benjamin Wolozin, Gavril W. Pasternak
Life SciencesMinireview: Multiple MU opiate receptors
347 Citations1986Gavril W. Pasternak, Paul Wood
This review will address both the biochemical and pharmacological evidence supporting the existence of a common site with very high affinity for both enkephalins and opiates termed the mu 1 site.
Journal of Pharmacology and Experimental TherapeuticsKappa opiate receptor multiplicity: evidence for two U50,488-sensitive kappa 1 subtypes and a novel kappa 3 subtype.
339 Citations1989J A Clark, L Liu +4 more
Competition studies with both alpha-neoendorphin and dynorphin B together suggest that both compounds label the same site with high affinity, whereas Classical kappa opiates and dynoirin A have high affinity for both subtypes whereas dynorphIn B and alpha-Neo endorphin label kappa 1b over 50-fold more potently than kappa 2a sites.
FEBS LettersPrimary structures and expression from cDNAs of rat opioid receptor δ‐and μ‐subtypes
279 Citations1993Kazuhiko Fukuda, Shigehisa Kato +3 more
RNA blot hybridization analysis revealed that cerebrum and brainstem contain both R OR‐A and ROR‐B mRNAs, whereas neither ROR •A nor ROR•B m RNAs can be detected in cerebellum.
FEBS LettersCloning and expression of a cDNA for the rat <i>k</i>‐opioid receptor
233 Citations1993Masabumi Minami, Takashi Toya +6 more
Northern blot analysis demonstrated that k‐opioid receptor mRNA is expressed in a regionally specific manner in rat brain.
Proceedings of the National Academy of SciencesOpiates inhibit adenylate cyclase by stimulating GTP hydrolysis.
231 Citations1981Greg Koski, Werner A. Klee
It is concluded that receptor-mediated stimulation of GTP hydrolysis is the mechanism by which opiates and other inhibitory hormones lower adenylate cyclase activity in NG108-15 cell membranes.
Proceedings of the National Academy of SciencesInteraction of ligands with the opiate receptors of brain membranes: Regulation by ions and nucleotides
216 Citations1978Arthur J. Blume
Archives of General PsychiatryGenetic Vulnerability to Drug Abuse
201 Citations1992Stevens S. Smith
Results are consistent with a role for a D2 dopamine receptor gene variant marked by these restriction fragment length polymorphisms in enhanced substance abuse vulnerability in polysubstance users and controls free of significant substance use.
Journal of Pharmacology and Experimental TherapeuticsRelative involvement of mu, kappa and delta receptor mechanisms in opiate-mediated antinociception in mice.
154 Citations1983Susan J. Ward, A.E. Takemori
It was concluded that an agonist interaction with mu, but not kappa, receptors results in antinociceptive action on the radiant heat tail-flick test, and that a possible combination of mu and delta receptor interaction can result in ant inocICEptive activity in both tests.
PeptidesInteraction of endogenous opioid peptides and other drugs with four kappa opioid binding sites in guinea pig brain
146 Citations1990Richard B. Rothman, Victor Bykov +4 more
Quantitative autoradiographic studies demonstrated that kappa 2a and kapp 2b binding sites are heterogeneously distributed in guinea pig brain, and that the anatomical distribution of kappa 1 binding sites reported in the literature is different from that observed in this study for the kappa2 binding sites.
Journal of Biological ChemistryModulation of sodium-sensitive GTPase by partial opiate agonists. An explanation for the dual requirement for Na+ and GTP in inhibitory regulation of adenylate cyclase.
125 Citations1982Greg Koski, Richard A. Streaty +1 more
The results provide a mechanism for the dual requirement for Na+ and GTP in the inhibitory coupling of opiate receptors to the adenylate cyclase system in these cells and may be of general significance to the action of other inhibitory hormones.
Proceedings of the National Academy of Sciences[D-Ala2]deltorphin I binding and pharmacological evidence for a special subtype of delta opioid receptor on human and invertebrate immune cells.
123 Citations1992George B. Stefano, Pietro Melchiorri +3 more
Nucleic Acids ResearchDirect visualization of single copy genes on banded metaphase chromosomes by nonisotopic<i>in situ</i>hybridization
108 Citations1988Bhupendra Bhatt, John M. Burns +2 more
A rapid method is described for non isotopic in situ mapping of single copy genes directly on G-banded chromosomes by "one-step" regular light microscopy based on hybridizing biotinylated probes to metaphase chromosomes that gives results within 1 day of hybridization and has much better resolution.
Proceedings of the National Academy of SciencesSingle potassium channels opened by opioids in rat locus ceruleus neurons.
104 Citations1989Michihisa Miyake, MacDonald J. Christie +1 more
The results indicate that mu opioid receptors, alpha 2 adrenoceptors, and somatostatin receptors can couple directly to membrane potassium channels through the local intermediary action of a GTP binding protein.
FEBS LetterscDNA cloning and pharmacological characterization of an opioid receptor with high affinities for κ‐subtype‐selective ligands
103 Citations1993Miyuki Nishi, Hiroshi Takeshima +3 more
RNA blot hybridization analysis indicated that ROR‐D mRNA is distributed in cerebrum and brainstem but not in cerebellum, and high affinities for ligands selective for the δ‐ and μ‐subtypes.
Journal of Biological ChemistryCloning and expression of a rat somatostatin receptor enriched in brain.
99 Citations1992X J Li, Michael Forte +3 more
Northern analysis and in situ hybridization indicate that mRNA for cloned rat SRIF receptor is preferentially expressed in rat brain regions such as cerebral cortex and hippocampus with no detectable expression in most peripheral organs.
Annals of NeurologyParkinsonism‐inducing neurotoxin MPP<sup>+</sup>: Uptake and toxicity in nonneuronal COS cells expressing dopamine transporter cDNA
96 Citations1992S. Kitayama, Shoichi Shimada +1 more
By documenting that the dopamine transporter can confer MPP+ sensitivity to nonneural cells, these results highlight the key role that this transporter could play in mechanisms underlying parkinsonism.
Molecular PharmacologyComparative pharmacological properties and functional coupling of mu and delta opioid receptor sites in human neuroblastoma SH-SY5Y cells.
93 Citations1987Syed M.I. Kazmi, Ram K. Mishra
The characteristics of mu and delta opioid receptor sites present in human neuroblastoma SH-SY5Y cells were investigated using D-Ala2-N-methyl-Phe4-Gly-(01)5]enkephalin (DAGO) and DPDPE, which are the most selective radioligands available for mu andDelta sites, respectively, and shown to be functionally coupled to adenylate cyclase.
Proceedings of the National Academy of SciencesVisualization of mu1 opiate receptors in rat brain by using a computerized autoradiographic subtraction technique.
93 Citations1985Robert Goodman, Gavril W. Pasternak
A quantitative computerized subtraction technique is developed to demonstrate in rat brain the regional distribution of mu1 sites, a common very-high-affinity binding site for both morphine and the enkephalins, and the previously described role of mu 1 sites in analgesia.
Brain ResearchPertussis toxin blocks depressant effects of opioid, monoaminergic and muscarinic agonists on dorsal-horn network responses in spinal cord-ganglion cultures
66 Citations1987Stanley M. Crain, Bea Crain +1 more
The present study demonstrates that a remarkably similar degree of tolerance to opioids develops in mouse spinal cord-ganglion explants after exposure to pertussis toxin (PTX), and suggests that the neuromodulatory effects of opioid, monoaminergic and muscarinic agonists on primary afferent networks in the spinal cord may be mediated by binding to neuronal receptor subtypes that are negatively coupled via Gi to a common pool of adenylate cyclase.
Journal of Biological ChemistryPurification and partial amino acid sequence of a mu opioid receptor from rat brain.
66 Citations1993C. Mark Eppler, J D Hulmes +6 more
A rat brain opioid receptor protein was isolated by binding [epsilon-biotinyl-Lys32] beta-endorphin to membranes, solubilizing the receptor-ligand (R.125I-L) complex with deoxycholate-lysophosphatidylcholine and purifying on immobilized streptavidin and wheat germ agglutinin.
Journal of Pharmacology and Experimental TherapeuticsFurther demonstration of kappa opioid binding sites in the brain: evidence for heterogeneity.
64 Citations1985Tsung‐Ping Su
By selectively blocking cross-interferences from other types of binding sites, a binding site which likely represents kappa opioid binding sites was obtained in the guinea-pig brain suspension of the particulate fraction and indicates a possibility of the heterogeneity of kappa opioids binding sites in the brain.
Journal of NeurochemistryDistinct Subtypes of the Opioid Receptor with Allosteric Interactions in Brain Membranes
63 Citations1986Catherine Demoliou-Mason, Eric A. Barnard
The evidence suggests that the formation of heterologous K–δ or μ1–μ2 receptor complexes is required for stabilization of the high‐affinity conformational state of the receptor.
Biological PsychiatryDopamine transporter gene polymorphisms are not associated with polysubstance abuse
62 Citations1993Antonio M. Persico, David J. Vandenbergh +2 more
Cloned human DATI complementary DNAs are identified and a 5' polymorphic restriction fragment length polymorphism (RFLP) and a 3' variable number tandem repeat (VNTR) marker for the human D ATI gene locus are identified, which allow study of possible allelic association of these human DatI gene markers with substance abuse.
NeuroreportExpressed mu opiate receptor couples to adenylate cyclase and phosphatidyl inositol turnover
61 Citations1994P. S. Johnson, Jia Bei Wang +2 more
Results represent the first clear representation of the second messenger system promiscuity possible with a single cloned opiate receptor and could be blocked by naloxone and Gpp(NH)p.
European Journal of PharmacologyNa+ ions and Gpp(NH)p selectively inhibit agonist interactions at μ- and κ-opioid receptor sites in rabbit and guinea-pig cerebellum membranes
57 Citations1985Bernard Francès, Christiane Moisand +1 more
It is reported here that Na+ ions, Gpp(NH)p and most efficiently, the two agents in association selectively inhibited binding of opioid agonists not only in the mu preparation but also in the kappa preparation and a method to rapidly screen newly designed drugs as mu- or kappa-opioid agonists or antagonists is suggested.
Journal of NeurochemistryDifferentiation of Human Neuroblastoma Cells: Marked Potentiation of Prostaglandin E‐Stimulated Accumulation of Cyclic AMP by Retinoic Acid
55 Citations1988Victor C. Yu, Günther Hochhaus +4 more
The ability of neuroblastoma cells to elevate cyclic AMP levels upon prostaglandin stimulation could modulate differentiation therapy with retinoic acid in vivo.
Nucleic Acids ResearchPrimary structure of the rat beta-2 adrenergic receptor gene
46 Citations1990Paul R. Buckland, Rhiannon M. Hill +2 more
Life SciencesOpioid agonists binding and responses in SH-SY5Y cells
22 Citations1992Elizabeth M. Costa, Brian B. Hoffman +1 more
Results provide further evidence that mu-receptors are coupled to inhibition of adenylate cyclase and that the SH-SY5Y cell line is a good system for assessment of mu-agonists functional responses.
Molecular Brain ResearchOrganization and expression of the gene encoding chick kainate binding protein, a member of the glutamate receptor family
18 Citations1992Paul Gregor, Xiaodong Yang +4 more
Transfection of 293 kidney cell cultures with chKBP cDNA orchKBP gene expression constructs confers CNQX-sensitive kainate binding with the pharmacological specificity displayed by both chK BP and kainates receptors, however, expression of the same constructs in Xenopus oocytes fails to yield detectable agonist-activated currents.
European Journal of Pharmacologyμ-Opioid receptor binding in intact SH-SY5Y neuroblastoma cells
14 Citations1990Lawrence Toll
These studies indicate the usefulness of [3H]CTOP for the determination of affinities at the μ receptor under physiological conditions.