Inverse agonistic effect of ICI-174,864 on the cloned δ-opioid receptor: Role of G protein and adenylyl cyclase activation

Molecular Pharmacology

Volumn 50, Issue 6, 1996, Pages 1651-1657

  Chiu, Tillie T ^a,b   Yung, Lisa Y ^a   Wong, Yung H ^a  

^a HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (Hong Kong)

^b UNIVERSITY OF WESTERN ONTARIO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE; ADENYLATE CYCLASE; DELTA OPIATE RECEPTOR; ENKEPHALIN DERIVATIVE; ENKEPHALIN[2,5 DEXTRO PENICILLAMINE]; FORSKOLIN; GUANINE NUCLEOTIDE BINDING PROTEIN; N,N DIALLYLTYROSYL 2 METHYLALANYL 2 METHYLALANYLPHENYLALANYLLEUCINE; N,N DIALLYLTYROSYLGLYCYL ALPHA (2 AMINOETHYLTHIO)HYDROCINNAMOYLLEUCINE; NALOXONE; NALTRINDOLE; NORBINALTORPHIMINE; PERTUSSIS TOXIN;

ADENOSINE DIPHOSPHATE RIBOSYLATION; ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; ENZYME ACTIVATION; HUMAN; HUMAN CELL; PRIORITY JOURNAL; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION; THERMODYNAMICS;

CELL LINE; CYCLIC AMP; DRUG INTERACTIONS; ENKEPHALIN, LEUCINE; FORSKOLIN; HUMANS; NARCOTIC ANTAGONISTS; RECEPTORS, OPIOID, DELTA;

EID: 0030448770     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (27)

1. Leff, P. The two-state model of receptor activation. Trends Pharmacol. Sci. 16:89-97 (1995).
2. 2-adrenergic receptor. Mol. Pharmacol. 46:390-394 (1994).
3. 1B-adrenergic receptor by all amino acid substitutions at a single site: evidence for a region which constrains receptor activation. J. Biol. Chem. 267:1430-1433 (1992).
4. 2-adrenergic receptor: extending the ternary complex model. J. Biol. Chem. 288:4625-4636 (1993).
5. Chidiac, P., T. E. Hebert, M. Valiquette, M. Dennis, and M. Bouvier. Inverse agonist activity of β-adrenergic antagonists. Mol. Pharmacol. 45: 490-499 (1994).
6. Kenakin, T. Agonist-receptor efficacy. I. Mechanisms of efficacy and receptor promiscuity. Trends Pharmacol. Sci. 16:188-192 (1995).
7. Wong, Y. H., C. D. Demoliou-Mason, and E. A. Barnard. The opioid receptor(s) in magnesium-digitonin solubilized rat brain membranes are tightly coupled to a pertussis toxin sensitive guanine nucleotide binding protein. J. Neurochem. 52:999-1009 (1989).
8. Costa, T., and A. Herz. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc. Natl. Acad. Sci. USA 86:7321-7325 (1989).
9. Costa, T., Y. Ogino, P. J. Munson, H. O. Onaran, and D. Rodbard. Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: thermodynamic interpretation of negative antagonism and of receptor activity in the absence of ligand. Mol. Pharmacol. 41:549-560 (1992).
10. Mullaney, I., I. C. Carr, and G. Milligan. Analysis of inverse agonism at the δ opioid receptor after expression in Rat 1 fibroblasts. Biochem. J. 315: 227-234 (1996).
11. 2-adrenoceptor. Nature (Lond.) 374:272-276 (1995).
12. Tsu, R. C., J. S. C. Chan, and Y. H. Wong. Regulation of multiple effectors by the cloned δ-opioid receptor: stimulation of phospholipase C and type II adenylyl cyclase. J. Neurochem. 64:2700-2707 (1995).
13. Evans, C. J., D. E. Keith, H. Morrison, K Magendzo, and R. H. Edwards. Cloning of a delta opioid receptor by functional expression. Science (Washington D. C.) 258:1952-1955 (1992).
14. i assays in transfected cells. Methods Enzymol. 238:81-94 (1994).
15. i2 inhibit cyclic AMP accumulation. Nature (Lond.) 351:63-65 (1991).
16. Raynor, K., H. Kong, Y. Chen, K. Yasuda, L. Yu, G. I. Bell, and T. Reisine. Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptors. Mol. Pharmacol. 45:330-334 (1994).
17. 5α alter stimulations of adenylyl cyclase. J. Biol. Chem. 264:15467-15474 (1989).
18. Taussig, R., W.-J. Tang, J. R. Hepler, and A. G. Gilman. Distinct patterns of bidirectional regulation of mammalian adenylyl cyclases. J. Biol. Chem. 269:6093-6100 (1994).
19. Tsai, S. C., R. Adamik, Y. Kanoho, E. L. Hewlett, and J. Moss. Effects of guanyl nucleotides and rhodopsin on ADP-ribosylation of the inhibitory GTP-binding component of adenylate cyclase by pertussis toxin. J. Biol. Chem. 259:15320-15323 (1984).
20. Sindt, K. A., E. L. Hewlett, G. T. Redpath, R. Rappuoli, L. S. Gray, and S. R. Vandenberg. Pertussis toxin activates platelets through an interaction with platelet glycoprotein 1b. Infect. Immunol. 62:3108-3114 (1994).
21. Kindt, R. M., and A. D. Lander. Pertussis toxin specifically inhibits growth cone guidance by a mechanism independent of direct G protein inactivation. Neuron 15:79-88 (1995).
22. Rosoff, P. M., R. Walker, and L. Winberry. Pertussis toxin triggers rapid second messenger production in human T lymphocytes. J. Immunol. 139: 2419-2423 (1987).
23. De Lean, A., J. M. Stadel, and J. R. Lefkowitz. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled β-adrenergic receptor. J. Biol. Chem. 255:5108-5117 (1980).
24. 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state. Mol. Pharmacol. 48:524-531 (1994).
25. Richardson, A., C. Demoliou-Mason, and E. A. Barnard. Guanine nucleotide-binding protein-coupled and -uncoupled states of opioid receptors and their relevance to the determination of subtypes. Proc. Natl. Acad. Sci. USA 89:10198-10202 (1992).
26. 2c receptors reveal novel inverse agonist activity of receptor ligands. J. Biol. Chem. 269:11687-11690 (1994).
27. Westphal, R. S., and E. Sanders-Bush. Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol. Pharmacol. 46:937-942 (1994).