μ Opioid receptor-mediated G-protein activation by heroin metabolites: Evidence for greater efficacy of 6-monoacetylmorphine compared with morphine

Biochemical Pharmacology

Volumn 62, Issue 4, 2001, Pages 447-455

  Selley, Dana E ^a   Cao, Cheng Chun ^b   Sexton, Tammy ^b   Schwegel, Jennifer A ^a   Martin, Thomas J ^b   Childers, Steven R ^b  

^a VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

^b WAKE FOREST SCHOOL OF MEDICINE   (United States)

Author keywords

6 Monoacetylmorphine; Agonist efficacy; G protein; Heroin; Mu opioid receptor; Signal transduction

Indexed keywords

DELTA OPIATE RECEPTOR; DIAMORPHINE; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); GUANOSINE DIPHOSPHATE; LEVALLORPHAN; METHADONE; MORPHINE; MORPHINE 6 ACETATE; MORPHINE 6 GLUCURONIDE; MU OPIATE RECEPTOR; NALOXONE; NALTRINDOLE;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BRAIN MEMBRANE; BRAIN REGION; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DEACETYLATION; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; ENZYME ACTIVATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; MALE; METABOLITE; NONHUMAN; PRIORITY JOURNAL; RAT; THALAMUS;

ANALGESICS, OPIOID; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HEROIN; MALE; MORPHINE; MORPHINE DERIVATIVES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID, MU; SULFUR RADIOISOTOPES; TUMOR CELLS, CULTURED;

EID: 0035882744     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-2952(01)00689-X     Document Type: Article

References (41)

1. The therapeutic use of heroin: A review of the pharmacological literature
2. Anti-allodynic actions of intravenous opioids in the nerve injured rat: Potential utility of heroin and dihydroetorphine against neuropathic pain
3. The pharmacologic effects of heroin in relationship to its rate of biotransformation
4. Metabolism of heroin and its pharmacologic implications
5. The pharmacokinetics of heroin in patients with chronic pain
6. Loss of morphine-induced analgesia, reward effect and withdrawal symptoms in mice lacking the μ-opioid receptor gene
7. Opiate receptor knockout mice define μ receptor roles in endogenous nociceptive responses and morphine-induced analgesia
8. μ Opioid receptor knockout in mice: Effects on ligand-induced analgesia, and morphine lethality
9. μ-Opioid receptor-knockout mice: The role of μ-opioid receptor in gastrointestinal transit
10. Selectivity of ligands for opioid receptors
11. Antisense mapping of MOR-1 in rats: Distinguishing between morphine and morphine-6β-glucuronide antinociception
12. Retention of heroin and morphine-6β-glucuronide analgesia in a new line of mice lacking exon 1 of MOR-1
13. 35S]thio)triphosphate binding to membranes from human neuroblastoma SH-SY5Y cells
14. Characterization of opioid agonist efficacy in a C6 glioma cell line expressing the μ opioid receptor
15. μ Opioid receptor-stimulated guanosine-5′-O-(γ-thio)-triphosphate binding in rat thalamus, and cultured cell lines: Signal transduction mechanisms underlying agonist efficacy
16. Catecholamine-stimulated guanosine 5′-O-(3-thiotriphosphate) binding to the stimulatory GTP-binding protein of adenylyl cyclase: Kinetic analysis in reconstituted phospholipid vesicles
17. Functional interaction of purified muscarinic receptors with purified inhibitory guanine nucleotide regulatory proteins reconstituted in phospholipid vesicles
18. Muscarinic acetylcholine receptor-stimulated binding of guanosine 5′-O-(3-thiotriphosphate) to guanine-nucleotide-binding proteins in cardiac membranes
19. 35S]GTPγS binding in mMOR-CHO cells and rat thalamus
20. 35S]GTPγS binding in rat brain: Evidence for partial agonist activity at μ-opioid receptors
21. Light microscopic localization of brain opiate receptors: A general autoradiographic method which preserves tissue quality
22. 35S]thio]-triphosphate binding
23. Heroin, morphine, and hydromorphone determination in postmortem material by high performance liquid chromatography
24. Acute and chronic effects of opioids on δ and μ receptor activation of G proteins in NG108-15 and SK-N-SH cell membranes
25. 3H-Morphine-6β-glucuronide binding in brain membranes, and an MOR-1-transfected cell line
26. 35S]GTPγS binding to rat cerebellar membranes correlates with agonist-induced decreases in GDP affinity
27. 1A receptor agonists in recombinant cell lines: Modulation of apparent efficacy by G-protein activation state
28. 1 adenosine receptor with receptor/G protein complexes in rat brain membranes
29. Characterization of the murine μ opioid receptor gene
30. The heroin metabolite, 6-monoacetylmorphine, activates delta opioid receptors to produce antinociception in Swiss-Webster mice
31. Opioid receptor selectivity of heroin given intracerebroventricularly differs in six strains of inbred mice
32. Heroin acts on different opioid receptors than morphine in Swiss Webster and ICR mice to produce antinociception
33. Evidence for κ- and μ-opioid receptor expression in C6 glioma cells
34. Evidence from opiate binding studies that heroin acts through its metabolites
35. The effect of temperature and pH on the deacetylation of diamorphine in aqueous solution and in human plasma
36. Diamorphine stability in aqueous solution for subcutaneous infusion
37. Metabolism of cocaine and heroin is catalyzed by the same human liver carboxylesterases
38. Heroin: Analgesia, toxicity, and disposition in the mouse
39. Heroin, 6-acetylmorphine, and morphine effects on threshold for rewarding, and aversive brain stimulation
40. 3H]DAMGO binding to rat brain sections
41. Disposition of heroin and its metabolites in heroin-related deaths