Agonist potency at the cloned human beta-3 adrenoceptor depends on receptor expression level and nature of assay

Journal of Pharmacology and Experimental Therapeutics

Volumn 279, Issue 1, 1996, Pages 214-221

  Wilson, Shelagh ^a   Chambers, Jon K ^a   Park, Janet E ^a   Ladurner, Andreas ^a   Cronk, David W ^a   Chapman, Conrad G ^a   Kallender, Howard ^a   Browne, Michael J ^a   Murphy, Gregory J ^a   Young, Paul W ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; 4 [2 [[2 (3 CHLOROPHENYL) 2 HYDROXYETHYL]AMINO]PROPYL]PHENOXYACETIC ACID; ADENYLATE CYCLASE; BETA 3 ADRENERGIC RECEPTOR; CYCLIC AMP; ISOPRENALINE; NORADRENALIN;

AGONIST; ANIMAL CELL; ARTICLE; CHO CELL; DRUG POTENCY; DRUG RECEPTOR BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR DENSITY;

ADENYLATE CYCLASE; ADRENERGIC BETA-AGONISTS; ANIMALS; CHO CELLS; CRICETINAE; CYCLIC AMP; HUMANS; PROPANOLAMINES; RECEPTORS, ADRENERGIC, BETA; RECEPTORS, ADRENERGIC, BETA-3;

EID: 12644296023     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (40)

1. 1E receptor couples to inhibition and activation of adenylyl cyclase via two distinct pathways in transfectad BS-C-1 cells. Neuropharmacology 33: 403-410, 1994.
2. ARCH, J. R. S., AINSWORTH, A. T., CAWTHORNE, M. A., PIERCY, V., SENNITT, M. V., THODY, V. E., WILSON, C. AND WILSON, S.:, Atypical β-adrenoceptor on brown adipocytes as target for anti-obesity drugs. Nature 309: 163-165, 1984.
3. BLACK, J. W. AND LEFF, P.: Operational models cf pharmacological agonism. Proc. R. Soc. Lond. B 220: 141-162, 1983.
4. 3-adrenoceptor. Br. J. Pharmacol. 112: 911-919, 1994.
5. 1A receptors: variations in intrinsic activity studied in tranefected HeLa cells. Naunyn-Schmiedeberg's Arch. Pharmacol. 346: 257-263, 1992.
6. BOJANIC, D., JANSEN, J. D., NAHORSKI, S. R. AND ZAAGSMA, J.: Atypical characteristics of the β-adrenoceptor mediating cyclic AMP generation and lipolysis in the rat adipocyte. Br. J. Pharmacol. 84: 131-137, 1985.
7. 2-adrenergic receptor in Chinese hamster fibro blasts (CHW): Functionality and regulation of the expressed receptors. Mol. Pharmacol. 33: 133-139, 1988.
8. BOWEN, W. P., JERMAN, J. C. AND BAXTER, G. S.: Optima: Simultaneous fitting of response curves to the operational model of agonism with microsoft excel. Br. J. Pharmacol. 112: 659P, 1994.
9. 3-adrenoceptor refractory to down-regulation. Biochem J. 303: 973-978, 1994.
10. i in rat adipocytes. Cell. Signal. 6: 457-465, 1994.
11. 50) of an enzymatic reaction. Biochem. Pharmacol. 22: 3099-3108, 1973.
12. CHIDIAC, P., HEBERT, T. E., VALIQUETTE, M., DENNIS, M. AND BOUVIER, M.: Inverse agonist activity of β-adrenergic antagonists. Mol. Pharmacol. 45: 490-499, 1994.
13. 3-adrenergic receptor. Science 245: 1118-1121, 1989.
14. 3-adrenergic receptor. J. Biol. Chem. 266: 20329-20336, 1991.
15. FURCHGOTT, R. F.: The use of β-haloaklylamines in the differentiation of receptors and in the determination of dissociation constants of receptor-agonist complexes. Adv. Drug Res. 3: 21-55, 1966.
16. 3-adrenergic receptor. Mol. Pharmacol. 40: 895-899, 1991.
17. 3-adrenergic receptor gene. Mol. Pharmacol. 44: 264-270, 1993.
18. S-adrenergic receptor? Cell. Signal. 7: 9-15, 1995.
19. HARMS, H. H., ZAAGSMA, J. AND VAN DER WAL, B.: β-adrenoceptor studies III: on the β-adrenoceptors in rat adipose tissue. Eur. J. Pharmacol. 26: 87-91, 1974.
20. 3-adrenoceptor mediated lipolysis in human fat cells. Obesity Res. 3: 447-457, 1995.
21. HOLLENGA, CH., BROUWER, F. AND ZAAGSMA, J.: Relationship between lipolysis and cyclic AMP generation mediated by atypical β-adrenoceptors in rat adipocytes. Br. J. Pharmacol. 102: 577-580, 1991.
22. KAUFMAN, R. J. AND SHARP, P. A.: Amplification and expression of sequences cotransfected with a modular dihydrofolate reductase complementary DNA gene. J. Mol. Biol. 159: 601-621, 1982.
23. KENAKIN, T. P. AND MORGAN, P. H.: Theoretical effects of single and multiple transducer receptor coupling proteins on estimates of the relative potency of agonists. Mol. Pharmacol. 35: 214-222, 1989.
24. LAFONTAN, M.: Differential recruitment and differential regulation by physiological amines of fat cell β-1, β-2 and β-3 adrenergic receptors expressed in native fat cells and in transfected cell lines. Cell. Signal. 6: 363-392, 1994.
25. LANGIN, D., PORTILLO, M. P., SAULNIER-BLACHE, J. AND LAFONTAN, M.: Coexistence of three β-adrenoceptor subtypes in white fat cells of various mammalian species. Eur. J. Pharmacol., 199: 291-301, 1991.
26. 3-adrenergic receptors: differential agonist activation of recombinant receptors in Chinese hamster ovary cells. Mol. Pharmacol. 42: 634-637, 1992.
27. LOHSE, M. J., VENOVIC, J. L., CARON, M. G. AND LEFKOWITZ, R. J.: Multiple pathways of rapid β2-adrenergic receptor desensitization: Delineation with specific inhibitors. J. Biol. Chem. 265: 3202-3209, 1990.
28. 3-adrenoceptor in man. Br. J. Pharmacol. 110: 929-936, 1993.
29. 1 Muscarinic receptor and the hydrolysis of inositol lipids in transfected murine fibroblast cells (B82) expressing different receptor densities. J. Pharmacol. Exp. Ther. 251: 90-97, 1989.
30. 2-adrenoceptor. Mol. Pharmacol. 48: 316-325, 1995.
31. 3-adrenoceptor-induced activation of cyclic AMP-dependent protein kinase with activation of lipolysis in rat white adipocytes. Biochem. Pharmacol. 46: 575-581, 1993.
32. MUZZIN, P., REVELL, J., KUHNE, F., GOCAYNE, J. D., MCCOMBIE, W. R., VENTER, J. C., GIACOBINO, J. AND FRASER, C. M.: An adipose tissue-specific β-adrenergic receptor: Molecular cloning and down-regulation in obesity. J. Biol. Chem. 266: 24053-24058, 1991.
33. 3-adrenergic receptor: Relationship with the atypical receptor of adipocytes. EMBO J. 10: 3721-3727, 1991.
34. SALOMON, Y., LONDOS, C. AND RODBELL, M.: A highly sensitive adenylate cyclase assay. Anal. Biochem. 58: 541-548, 1974.
35. 2-adrenergic receptor: Extending the ternary complex model. J. Biol. Chem. 268: 4625-4636, 1993.
36. VAN LIEFDE, I., VAN ERMEN, A. AND VAUQUELIN, G.: No functional atypical β-adrenergic receptors in human omental adipocytes. Life Sci. 64: 209-214, 1994.
37. 1A receptors to adenylyl cyclase. Mol. Pharmacol. 41: 999-1007, 1992.
38. VILARDAGA, J. P., CICCARELLI, E., DUBEAUX, C., DE NEEF, P., BOLLEN, A. AND ROBBERECHT, P.: Properties and regulation of the coupling to adenylate cyclase of secretin receptors stably transfected in Chinese hamster ovary cells. Mol. Pharmacol. 45: 1022-1028, 1994.
39. WHALEY, B. S., YUAN, N., BIRNBAUMER, L., CLARK, R. B. AND BARBER, R.: Differential expression of the β-adrenergic receptor modifies agonist stimulation of adenylyl cyclase: A quantitative evaluation. Mol. Pharmacol. 45: 481-489, 1994.
40. WILSON, C., WILSON, S., PIERCY, V., SENNIT, M. V. AND ARCH, J. R. S.: The rat lipolytic β-adrenoceptor; studies using novel β-adrenoceptor agonists. Eur. J. Pharmacol. 100: 309-319, 1984.