Human Mu-type opioid receptor(OPRM1) ELISA kit

Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors. The agonist- and cell type-specific activity is predominantly coupled to pertussis toxin-sensitive G(i) and G(o) G alpha proteins, GNAI1, GNAI2, GNAI3 and GNAO1 isoforms Alpha-1 and Alpha-2, and to a lesser extent to pertussis toxin-insensitive G alpha proteins GNAZ and GNA15. They mediate an array of downstream cellular responses, including inhibition of adenylate cyclase activity and both N-type and L-type calcium channels, activation of inward rectifying potassium channels, mitogen-activated protein kinase (MAPK), phospholipase C (PLC), phosphoinositide/protein kinase (PKC), phosphoinositide 3-kinase (PI3K) and regulation of NF-kappa-B. Also couples to adenylate cyclase stimulatory G alpha proteins. The selective temporal coupling to G-proteins and subsequent signaling can be regulated by RGSZ proteins, such as RGS9, RGS17 and RGS4. Phosphorylation by members of the GPRK subfamily of Ser/Thr protein kinases and association with beta-arrestins is involved in short-term receptor desensitization. Beta-arrestins associate with the GPRK-phosphorylated receptor and uncouple it from the G-protein thus terminating signal transduction. The phosphorylated receptor is internalized through endocytosis via clathrin-coated pits which involves beta-arrestins. The activation of the ERK pathway occurs either in a G-protein-dependent or a beta-arrestin-dependent manner and is regulated by agonist-specific receptor phosphorylation. Acts as a class A G-protein coupled receptor (GPCR) which dissociates from beta-arrestin at or near the plasma membrane and undergoes rapid recycling. Receptor down-regulation pathways are varying with the agonist and occur dependent or independent of G-protein coupling. Endogenous ligands induce rapid desensitization, endocytosis and recycling whereas morphine induces only low desensitization and endocytosis. Heterooligomerization with other GPCRs can modulate agonist binding, signaling and trafficking properties. Involved in neurogenesis. Isoform 12 couples to GNAS and is proposed to be involved in excitatory effects. Isoform 16 and isoform 17 do not bind agonists but may act through oligomerization with binding-competent OPRM1 isoforms and reduce their ligand binding activity.

1. Cyclopeptide Dmt-[D-Lys-p-CF3-Phe-Phe-Asp]NH2, a novel G protein-biased agonist of the mu opioid receptor. PMID: 29196181
2. Higher methylation levels within the infants at the -18 (11.4% vs 4.4%, P = .0001), -14 (46.1% vs 24.0%, P = .002) and +23 (26.3% vs 12.9%, P = .008) CpG sites were associated with higher rates of infant pharmacologic treatment. Higher levels of methylation within the mothers at the -169 (R = 0.43, P = .008), -152 (R = 0.40, P = .002) and +84 (R = 0.44, P = .006) sites were associated with longer infant length of stay. PMID: 29575474
3. selection of a medication for opioid dependence based on OPRM1 rs10485058 genotype might improve outcomes in this ethnic group. PMID: 27958381
4. A118G (N40D) polymorphism is significantly associated with opioid addiction in Pakistani population. PMID: 30033503
5. Ligation of the identical phosphopeptide onto the beta2AR, the muscarinic acetylcholine receptor 2 and the mu-opioid receptor reveals that the ability of beta-arrestin1 to enhance agonist binding relative to G protein differs substantially among receptors. PMID: 29581292
6. DNA methylation analysis in the promoter region of OPRM1 identified twenty-two CpG sites in the OPRM1 promoter region significantly associated with opioid exposure in a Chinese Han population. PMID: 29564682
7. OPRM1 A118G polymorphism is associated with pain experience in young women with primary dysmenorrhea. PMID: 28057931
8. findings demonstrated DNA hypermethylation of the R2 region of the OPRM1 promoter in leukocytes of opium use disorder. PMID: 28121474
9. Genetic variations in the mu-opioid receptor (OPRM1) gene have been related to high sensitivity to rewarding effects of alcohol. PMID: 27594419
10. Findings suggest no OPRM1-based susceptibility to the number of heavy-drinking peers, adding to the existing mixed findings from correlational studies. Future research on OPRM1-related susceptibility to alcohol-promoting peer environments through meta-analytic synthesis and both experimental and prospective, multiwave designs is needed to resolve these mixed findings. PMID: 28992386
11. The MDR1/CYP3A4/OPRM1 gene polymorphisms influenced the fentanyl consumption and the physiological effects of intravenous analgesia in the Chinese women who received lower segment caesarean section surgeries. PMID: 29601950
12. Participants with the OPRM1 118G allele evidenced steeper breath alcohol concentration (BrAC) trajectories and greater peak BrAC relative to 118A homozygous participants. Significant indirect associations of OPRM1 with follow-up heavy drinking were observed. PMID: 27046326
13. Study demonstrated in a cohort of 84 cancer patients that high-dose opioid use correlates with OPRM1 hypermethylation in peripheral leukocytes; and showed that targeted re-expression of mu-opioid receptor on cancer cells inhibits mechanical and thermal hypersensitivity, and prevents opioid tolerance, in a mouse cancer pain model. Epigenetic regulation of OPRM1 contributes to opioid tolerance in cancer patients. PMID: 28456745
14. In summary, our results suggest that, by genetic association, the mu-opioid receptor interacts with serotonin transporter and serotonin 1A receptor to modulate exercise-induced hypoalgesia in fibromyalgia. PMID: 28282362
15. Significant epistatic interactions were determined between OPRM1 and DAT1 genotypes on alcohol consumption and subjective effects in social drinkers. PMID: 28376280
16. OPRM1/mu-opioid receptor system was uniformly expressed by epidermal keratinocytes from psoriasis patients and controls. PMID: 27958613
17. Morphine-induced MOP receptor endocytosis is facilitated by concurrent M3 activation.M3 and MOP assemble in receptor heterocomplexes mainly located at the plasma membrane.M3-MOP receptor pharmacological interaction is independent of heterocomplex formation.M3 and MOP receptor heteromers disrupt upon both receptor endocytosis. PMID: 28411124
18. A quantitative trait loci in OPRM1 is associated with alcohol use phenotypes and the subjective response to alcohol. PMID: 28273335
19. ADRB2 gene expressed in HIV-associated neurocognitive impairment and encephalitis chaperones OPRM1, normally located intracellularly in astrocytes, to the cell surface. PMID: 27400929
20. These results are in line with previous studies suggesting that mu-opioid receptor signalling has been elaborated beyond its basic function of pain modulation to play an important role in managing our social encounters. PMID: 27121297
21. Significant interaction of OPRM1 genotype, binding potential for [(11)C]carfentanil in the ventral striatum, and relapse risk in alcoholics. PMID: 27510425
22. In utero exposure to opioids is associated with increased DNA methylation of ABCB1, CYP2D6, and OPRM1 opioid-related genes in the newborn infant. PMID: 28867064
23. This study demonstrates that OPRM1 118A>G and the combined OPRM1/COMT genotype are associated with experimental thermal pain sensitivity in a paediatric population. PMID: 27541715
24. The 118G allele appears to confer greater sensitivity to nicotine reinforcement in males, but not females. PMID: 27459726
25. This study found significant effects for rs563649, but not rs1799971 of OPRM1, the so far most frequently analyzed opioidergic SNP in pain research. PMID: 28092323
26. DRD2 A2/A1, DRD3 Ser9Gly, DbetaH -1021C>T, OPRM1 A118G and GRIK1 rs2832407C>A are not associated with alcoholism alone or in interaction. PMID: 27447243
27. The OPRM1 rs1799971 A > G polymorphism is not strongly associated with alcohol-dependence. (Meta-analysis) PMID: 29070014
28. Low OPRM1 expression is associated with L-asparaginase resistance in pediatric acute lymphoblastic leukemia. PMID: 28650467
29. PET imaging with [11C]carfentanil tested the hypotheses that acute cigarette smoking increases release of endogenous opioids in the human brain and that smokers have an upregulation of mu opioid receptors (MORs) when compared to nonsmokers. No significant changes found in binding potential of [11C]carfentanil between the placebo and active cigarette sessions; no differences in MOR binding between smokers and nonsmokers. PMID: 25493427
30. These results do not support strong modulatory effects of OPRM1 genetic variation on opioid receptor antagonist attenuation of alcohol- and food-related behaviors. PMID: 27109624
31. AG and GG genotypes of OPRM1 rs1799971 were associated with a decreased risk of CVS ( P <0.05). In addition, AG and GG genotypes of OPRM1 rs1799971 were correlated with migraine episodes and a family history of migraines. PMID: 28349993
32. Subjects with schizophrenia who had the OPRM1 *G genotype smoked more cigarettes per day than the AA allele carriers with schizophrenia. In bipolar patients, there were no OPRM1 genotype differences in smoking status. PMID: 28548579
33. The MOR-Gal1R heteromer can explain previous results showing antagonistic galanin-opioid interactions and offers a new therapeutic target for the treatment of opioid use disorder PMID: 28007761
34. This study examined associations of the mu opioid receptor gene with several self-report measures relating to personality. These analyses revealed a pattern of Gene x Environment interactions that are consistent with the view that the G allele confers greater vulnerability than the A allele to adverse effects of childhood social adversity on adult personality qualities related to social connection. PMID: 26527429
35. MOR is present in human endometrium and levels change during the menstrual cycle. PMID: 28256208
36. Data show the multimicrosecond, all-atom molecular dynamics (MD) simulations of the binding of oliceridine (TRV-130) to the activated mu-opioid receptor (MOR) crystal structure. PMID: 27778501
37. These results establish the role of hnRNP K and PCPB1 in the translational control of morphine-induced MOR expression in human neuroblastoma (NMB) cells as well as cells stably expressing MOR (NMB1). PMID: 27292014
38. distinct ligands can leverage specific sequence elements on microR to regulate receptor endocytic lifetimes and the magnitude of arrestin-mediated signaling. PMID: 28153854
39. the single nucleotide polymorphism (SNP) of A118G and its interaction with smoking and drinking on oesophageal squamous cell carcinoma (ESCC) risk, was investigated. PMID: 27373278
40. AA patients for opioid receptor mu 1 single nucleotide polymorphism had significantly lower cognitive function than AG patients. PMID: 28346387
41. Study shows that overnight-abstinent smokers have decreased mu-opioid receptor (MOR) nondisplaceable binding potential (BPND) compared to nonsmoking controls, and that those individuals with the lowest MOR BPND in the basal ganglia also had higher nicotine dependence scores and greater craving after overnight nicotine abstinence; also suggests that A118G genotype may differentially affect MOR BPND in smokers vs. nonsmo... PMID: 27095017
42. OPRM1 minor variant of A118G (G-allele) predicts greater speed-dating success for women. PMID: 27193909
43. The OPRM1 G118 allele was significantly associated with more severe alcohol dependence in the Turkish population. Similar to other European populations, the frequency of the OPRM1 T17 allele was very low. PMID: 27370058
44. no significant associations were found between the 4 polymorphisms screened and the dose of morphine needed for pain relief. This result can be explained by the genetic heterogeneity and cosmopolitan areas of our Tunisian patients compared to the others homogenous population. PMID: 27288213
45. Arg181Cys mutation occurs at clinically relevant frequencies and produces a signaling dead hMOR which may abolish or significantly reduce opioid effects in affected individuals PMID: 27113810
46. We found a C-rich element (CRE) in mu-opioid receptor (MOR) 3'-untranslated region (UTR) to which poly (rC) binding protein 1 (PCBP1) binds, resulting in MOR mRNA stabilization. AUF1 phosphorylation also led to an increased interaction with PCBP1. PMID: 27836661
47. rs1799971 of OPRM1 contributes to mechanisms of addiction liability that are shared across different addictive substances. PMID: 26392368
48. Initial studies in neonates with in utero opiate exposure demonstrated that single-nucleotide polymorphisms in OPRM1 gene were associated with improved outcomes in infants with Neonatal abstinence syndrome. PMID: 26791055
49. OPRM1 might be used in near future to customize the opioid therapy, avoiding not only opioid side effects PMID: 25300626
50. The two patients homozygous for the G allele in this study of postoperative pain after knee arthroplasty had more pain than the other patients and required larger amounts of opioids, however, the sample size did not allow for statistical significance. PMID: 26517014

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Cell membrane; Multi-pass membrane protein. Cell projection, axon. Perikaryon. Cell projection, dendrite. Endosome.; [Isoform 12]: Cytoplasm.

G-protein coupled receptor 1 family

Expressed in brain. Isoform 16 and isoform 17 are detected in brain.

HGNC: 8156

OMIM: 600018

KEGG: hsa:4988

STRING: 9606.ENSP00000394624

UniGene: Hs.2353