Prospects for β3-adrenoceptor agonists in the treatment of obesity and diabetes

International Journal of Obesity

Volumn 20, Issue 3, 1996, Pages 191-199

  Arch, J R S ^a   Wilson, S ^b  

^a GLAXOSMITHKLINE   (United Kingdom)

^b NONE   (United Kingdom)

Author keywords

3 adrenoceptor; Diabetes (type II); Lipolysis; Obesity; Pharmacotherapy; Thermogenesis

Indexed keywords

4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; 4 [2 [[2 (3 CHLOROPHENYL) 2 HYDROXYETHYL]AMINO]PROPYL]PHENOXYACETIC ACID; ADENYLATE CYCLASE; BETA 1 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; BETA 3 ADRENERGIC RECEPTOR; BETA ADRENERGIC RECEPTOR STIMULATING AGENT; ISOPRENALINE; BETA ADRENERGIC RECEPTOR;

ADIPOSE TISSUE; CHO CELL; DIABETES MELLITUS; DRUG EFFICACY; DRUG SELECTIVITY; DRUG STRUCTURE; ENZYME ACTIVATION; HUMAN; LIPOLYSIS; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PRIORITY JOURNAL; RAT; RECEPTOR DENSITY; REVIEW; SPECIES DIFFERENCE; THERMOGENESIS; ANIMAL; COMPARATIVE STUDY; PHYSIOLOGY; THERMOREGULATION;

ADRENERGIC BETA-AGONISTS; ANIMALS; BODY TEMPERATURE REGULATION; DIABETES MELLITUS, TYPE 2; HUMANS; LIPOLYSIS; OBESITY; RECEPTORS, ADRENERGIC, BETA;

EID: 0029865228     PISSN: 03070565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (90)

1. Arch JRS. The brown adipocyte β-adrenoceptor. Proc Nutr Soc 1989; 48: 215-223.
2. 3-adrenergic receptor. Science 1989; 245: 1118-1121.
3. Arch JRS, Ainsworth AT. Thermogenic and antiobesity activity of a novel β-adrenoceptor agonist (BRL 26830A) in mice and rats. Am J Clin Nutr 1983; 38: 549-558.
4. 3-Adrenoceptor agonists. Drugs of the Future 1993; 18: 529-549.
5. 3-adrenergic agonism. Futura: New York, 1995.
6. Arch JRS, Ainsworth AT, Ellis RDM, Piercy V, Thody VE, Thurlby PL, Wilson C, Wilson S, Young P. Treatment of obesity with thermogenic β-adrenoceptor agonists: studies on BRL 26830A in rodents. Int J Obesity 1984; 8(1): 1-11.
7. Meier MK, Alig L, Burgi-Saville ME, Muller M. Phenethanolamine derivatives with calorigenic and antidiabetic qualities. Int J Obesity 8(1): 215-225.
8. Yen TT, McKee MM, Stamm NB. Thermogenesis and weight control. Int J Obesity 1984; 8(1): 65-78.
9. Cawthorne MA, Carroll MJ, Levy AL, Lister CL, Sennitt MV, Smith SA, Young P. Effects of novel β-adrenoceptor agonists on carbohydrate metabolism: relevance for the treatment of non-insulin-dependent diabetes. Int J Obesity 1984: 8(1): 93-102.
10. Croci T, Guidice A, Bianchetti A, Manara L. Colonic and cardiovascular actions of the atypical β-adrenergic agonist SR 58611A in rats. J Gastrointest Motility 1991; 3: 273-279.
11. Simiand J, Keane PE, Guitard J, Langlois X, Gonalons N, Martin P, Bianchetti A, Le Fur G, Soubrie P. Antidepressant profile in rodents of SR 58611A, a new selective agonist for atypical β-adrenoceptors. Eur J Pharmacol 1992; 219: 193-201.
12. Arch JRS, Bywater RJ, Coney KA, Ellis RDM, Thurlby PL, Smith SA, Zed C. Influences on body composition and mechanism of action of the β-adrenoceptor agonist BRL 26803A. In: Proceedings of the Eighteenth Steenbeck Symposium, Hormones, thermogenesis and obesity, HA Lardy, F Stratman (eds). Elsevier: New York, 1989, pp 465-476.
13. Arch JRS, Cawthorne MA, Coney KA, Gusterson BA, Piercy V, Sennitt MV, Smith SA, Wallace J, Wilson S. β-adrenoceptor-mediated control of thermogenesis, body composition and glucose homeostasis. In: Obesity and cachexia, NJ Rothwell, MJ Stock (eds). Wiley: Chichester, 1990, pp 241-268.
14. Meier MK, Blum-Kaelin D, Gerold M, Isler D, Meuller M. Ro 40-2148: a novel thermogenic β-agnoist with antiobesity activity. In: Obesity in Europe 88: Proceedings of the First European Congress on Obesity, P Bjorntorp, J Rossner (eds). Libbey: London, 1989, pp 329-338.
15. Yen TT. The antiobesity and metabolic activities of LY79771 in obese and normal mice. Int J Obesity 1984; 8: 69-78.
16. Yen TT, Fuller RW, Hemrick-Leuckce SK, Dininger NB. Effects of LY104119, a thermogenic weight-reducing compound, on norephinephrine concentrations and turnover in obese and lean mice. Int J Obesity 1988; 12: 59-67.
17. Holloway BR. Selective β-agonists of brown fat and thermogenesis. In: Proceedings of the Eighteenth Steenbeck Symposium, Hormones, thermogenesis and obesity, HA Lardy, FW Stratman (eds). Elsevier: New York, 1989, pp 477-484.
18. Holloway BR, Howe R, Rao BS, Stribling D. ICI D7114: a novel selective adrenoceptor agonist of brown fat and thermogenesis. Am J Clin Nutr 1992; 55: 262S-264S.
19. 3-adrenoceptor agonist, in mice with monosodium L-glutamate-induced obesity. Eur J Endocrinol 1994; 131: 97-102.
20. 3-adrenoceptor agonist, in yellow KK. mice. Life Sci 1994; 54: 491-498.
21. 3-adrenoceptor agonist (CL 316243). Drug Dev Res 1994; 32: 69-76.
22. 3-agonist, on energy balance and brown and white adipose tissue in rats. Am J Physiol 1994; 266: R1371-R1382.
23. Lowell BB, Susulic VC, Hamann A, Lawitts JA, Himms-Hagan, Boyer BB, Kozak LP, Flier JS. Development of obesity in transgenic mice after ablation of brown adipose tissue. Nature 1993; 366: 740-742.
24. Thurlby PL, Ellis RDM. Differences between the effects of noradrenaline and the β-adrenoceptor agonist BRL 28410 in brown adipose tissue and hind limb of the anaesthetized rat. Can J Physiol Pharmacol 1985; 64: 1111-1114.
25. Challis RAJ, Leighton B, Wilson S, Thurlby PL, Arch JRS. An investigation of the β-adrenoceptor that mediates metabolic responses to the novel agonist BRL 28410 in rat soleus muscle. Biochem Pharmacol 1988; 37: 947-950.
26. Wilson S, Thurlby PL, Arch JRS. Substrate supply for thermogenesis induced by the β-adrenoceptor agonist BRL 26830A. Can J Physiol Pharmacol 1987; 65: 113-119.
27. Moinat M, Deng C, Muzzin P, Assimacopoulos-Jeannet F, Seydoux J, Dullo AG, Giacobino J-P. Modulation of obese gene in rat brown and white adipose tissues. FEBS Lett 1995; 373: 131-134.
28. Pelleymounter MA, Cullen MJ, Baker MB, Hecht R, Winters D, Boone T, Collins F. Effects of the obese gene product on body weight in ob/ob mice. Science 1995; 269: 540-543.
29. Young PW, King L, Cawthorne MA. Increased insulin binding and glucose transport in white adipocytes isolated from C57B1/6 ob/ob mice treated with the thermogenic β-adrenoceptor agonist BRL 26830. Biochem Biophys Res Commun 1985; 133: 457-461.
30. Smith SA, Sennitt MV, Cawthorne MA. BRL 35135: an orally active antihyperglycaemic agent with weight reducing effects. In: New antidiabetic drugs, CJ Bailey, PR Flatt (eds). Smith-Gordon: London, 1990, pp 177-189.
31. 3-adrenoceptor agonist, Zeneca ZD2079, improves glucose homeostasis in insulin resistant rodents [Abstract]. Diabetologia 1994; 37(1): A212.
32. 3-adrenergic receptor agonist in obese mice. Am J Physiol 1995; 268: E678-E684.
33. McGarry JD. What if Minkowski had been ageusic? An alternative angle on diabetes. Science 1992; 258: 766-770.
34. 3-adrenergic agonist, BRL 35135A, on glucose uptake in rat skeletal in vivo and in vitro. J Endocrinol 1993; 139: 479-486.
35. Young PW, Cawthorne MA, Smith SA. Brown adipose tissue is a major site of glucose utilisation in C57B1/6 ob/ob mice treated with a thermogenic β-adrenoceptor agonist. Biochem Biophys Res Commun 1985; 130: 241-248.
36. 3-adrenceptor agonist, BRL 35135, on tissue glucose utilisation. Br J Pharmacol 1995; 114: 888-894.
37. Liu Y-L, Cawthorne MA, Stock MJ. Biphasic effect of the β-adrenoceptor agonist BRL 37344 on glucose utilisation in isolated rat skeletal muscle. Br J Pharmacol; in press.
38. Zed CA, Harris GS, Harrison PJ, Robb GH. Anti-obesity activity of a novel β-adrenoceptor agonist (BRL 26830A) in diet-restricted obese subjects [Abstract]. Int J Obesity 1985; 9: 231.
39. Connacher AA, Lakie M, Powers N, Elton RA, Walsh EG, Jung RT. Tremor and the anti-obesity drug BRL 26830A. Br J Clin Pharmacol 1990; 30: 613-615.
40. 3-adrenoceptor agonist BRL 35135 in man. Br J Clin Pharm 1994; 37: 363-369.
41. Connacher AA, Jung RT, Mitchell PEG. Weight loss in obese subjects on a restricted diet given BRL 26830A, a new atypical β adrenoceptor agonist. Br Med J 1988; 296: 1217-1220.
42. Abraham R, Zed C, Mitchell T, Parr J, Wynn V. The effect of a novel β-agonist BRL 26830A on weight and protein loss in obese patients [Abstract]. Int J Obesity 1987; 11: 306A.
43. Munro JF, Chapman BJ, Robb GH, Zed C. Clinical studies with thermogenic drugs. In: Recent advances in obesity research: V, EM Berry, SH Eliahou, E Shafrir (eds). Libbey: London, 1987, pp 155-159.
44. Connacher AA, Bennet WM, Jung RT, Rennie MJ. Metabolic effects of three weeks administration of the β-adrenoceptor agonist BRL 26830A. Int J Obesity 1992; 16: 685-692.
45. Smith SA, Cawthorne MA, Fay LC, McCullough DA, Mitchell TH. Effect of a novel β-adrenoceptor agonist on insulin sensitivity in lean healthy male volunteers [Abstract]. Diabetes 1987; 36(1): 15A.
46. Henny C, Schutz Y, Buckert A, Meylan M, Jequier E, Felber J. Thermogenic effect of the new β-adrenoceptor agonist Ro 16-8714 in healthy male volunteers. Int J Obesity 1987; 11: 473-483.
47. Henny C, Buckert A, Schutz Y, Jequier E, Felber J. Comparison of thermogenic activity induced by the new sympathomimetic Ro 16-8714 between normal and obese subjects. Int J Obesity 1988; 12: 227-236.
48. Haesler E, Golay A, Guzelhan C, Schutz Y, Hartmann D, Jequier E, Felber J. Effect of a novel β-adrenoceptor agonist (Ro 40-2148) on resting energy expenditure in obese women. Int J Obesity 1994; 18: 313-322.
49. 3 agonist (ICI D7114) in healthy lean men. Int J Obesity 1995; 19: 625-631.
50. 3-agonist on 25 h energy expenditure and lipid oxidation in obese patients [Abstract]. Int J Obesity 1992; 17(2): 73.
51. 3 agonist Zeneca ZD2079 in healthy male volunteers [Abstract]. Can J Physiol Pharmacol 1994; 72(1): 182.
52. Holloway BR, Howe R, Rao BS, Stribling D. ICI 198157: a novel selective agonist of brown fat and thermogenesis. In: Obesity in Europe, 88, P Bjorntorp, S Rossner (eds). John Libbey: London, 1989, pp 323-328.
53. 3 and atypical β-adrenoceptors. Med Res Rev 1993; 13: 663-729.
54. 2-adrenergic receptor binding and mediated accumulation of cAMP in transfected Chinese hamster ovary cells. Biochem Pharmacol 1991; 42: 1683-1689.
55. Tate T, Briend-Sutren M, Emorine LJ, Delavier-Klutchko C, Marullo S, Strosberg AD. Expression and three human β-adrenergic-receptor subtypes in transfected Chinese hamster ovary cells. Eur J Biochem 1991; 196: 357-361.
56. 3-adrenoceptors and the regulation of metabolism in adipose tissues. Biochem Soc Trans 1996; in press.
57. Muzzin P, Revelli J, Kuhne F, Gocayne JD, McCombie WR, Venter JC, Giacobino J, Fraser CM. An adipose tissue-specific β-adrenergic receptor: molecular cloning and down-regulation in obesity. J Biol Chem 1991; 266: 24053-24058.
58. 3-adrenergic receptor. J Biol Chem 1991; 266: 20329-20336.
59. Harms HH. Stereochemical aspects of β-adrenoceptor agonist-receptor interaction in adipocytes. Differentiation of β-adrenoceptors in human and rat adipocytes. Life Sci 1976; 19: 1447-1452.
60. Harms HH, Zaagsma J, de Vente J. Differentiation of β-adrenoceptors in right atrium, diaphragm and adipose tissue of the rat, using stereoisomers of propranolol, alprenolol, nifenalol and practolol. Life Sci 1977; 21: 123-128.
61. 3-adrenergic receptor: relationship with the atypical receptor of adipocytes. EMBO J 1991; 10: 3721-3727.
62. Dolan JA, Muenkel HA, Burns MG, Pellegrino SM, Fraser CM, Peitri F, Strosberg AD, Largis EE, Dutia MD, Bloom JD, Bass AS, Tanikella TK, Cobuzzi A, Lai FM, Claus TH. Beta-3 adrenoceptor selectivity of the dioxolane dicarboxylate phenethanolamines. J Pharm Exp Ther 1994; 269: 1000-1006.
63. Black JW, Leff P. Operational models of pharmacological agonism. Proc R Soc Lond 1983; B220: 141-162.
64. 3-adrenceptor: the search for a physiological function. Trends Pharmacol Sci 1994; 15: 3-7.
65. 3-adrenergic receptor gene. New Engl J Med 1995; 333: 343-347.
66. 3-adrenergic-receptor gene with features of the insulin resistance syndrome in Finns. New Engl J Med 1995; 333: 348-351.
67. 3-adrenergic receptor and increased capacity to gain weight in patients with morbid obesity. New Engl J Med 1995; 333: 352-354.
68. 3-adrenergic receptor gene is associated with obesity and hyperinsulinemia in Japanese subjects. Biochem Biophys Res Commun 1995; 215: 555-560.
69. 3-adrenoceptors mediate metabolic responses to isoprenaline? Q J Med 1993; 86: 595-600.
70. Wheeldon NM, McDevitt DG, McFarlane LC, Lipworth BJ. β-adrenoceptor subtypes mediating the metabolic effects of BRL 35135 in man. Clin Sci 1994; 86: 331-337.
71. 3-adrenoceptor activation to ephedrin-induced thermogenesis in humans. Int J Obesity 1995; 19: 678-685.
72. Astrup A, Lundsgaard C, Madsen J, Christensen NJ. Enhanced thermogenic responsiveness during chronic ephedrine treatment in man. Am J Clin Nutr 1985; 42: 83-94.
73. 3-adrenoceptors in obesity. J Clin Invest 1995; 95: 1109-1116.
74. 3-adrenergic receptor mRNA in man. J Clin Invest 1993; 91: 344-349.
75. 3-adrenergic receptor in human white adipose tissue. J Mol Endocr 1993; 10: 193-197.
76. 3-adrenergic receptor gene. Molec Pharm 1993; 44: 264-270.
77. 3-adrenoceptor in man. Br J Pharmacol 1993; 110: 929-936.
78. 3-adrenergic receptor mRNA in human tissues. Eur J Pharm 1995; 289: 223-228.
79. 3-adrenoceptor expression in white fat cells. Fundam Clin Pharmacol 1995; 9: 97-106.
80. Langin D, Portillo MP, Saulnier-Blache J-S, Lafontan M. Coexistence of three β-adrenoceptor subtypes in white fat cells of various mammalian species. Eur J Pharmacol 1991; 199: 291-301.
81. Van Liefde I, Van Ermen A, Vauquelin G. No functional atypical β-adrenergic receptors in human omental adipocytes. Life SCI 1994; 54: 209-214.
82. 3-adrenergic effect on lipolysis in human subcutaneous adipose tissue. J Clin Endocr Metab 1993; 77: 352-355.
83. 3-adrenoceptors. In: Adrenoceptors: structure, mechanism, function. Advances in pharmacological science, E Szabadi, CM Bradshaw (eds). Birkhauser: Basel, 1991, pp 47-58.
84. 3-adrenoceptor mediated lipolysis in human fat cells. Obesity Res 1995; 3: 447-457.
85. 3-adrenoceptor in man. J Clin Invest 1995; 95: 2239-2245.
86. Del Barrio AS, Rocandio A, Diaz E, Errasti J, Mtz-Blazquez C, Portillo MP. β-atypical adrenergic response from different human adipose tissues [Abstract]. Int J Obesity 1994; 18(2): 18.
87. Sennitt MV, Young PW, Kirkham D, Smith SA, Cawthorne MA. Pharmacological evidence for the existence of multiple β-adrenoceptor subtypes mediating the lipolytic response in human adipose tissue [Abstract]. Int J Obesity 1994; 18(2): 19.
88. 3-adrenoceptors in tissues. Pharmacol Commun 1995; 6: 223-228.
89. 3-AR. In: Genomes, molecular biology and drug discovery, MJ Browne, PL Thurlby (eds). Academic Press: London, 1995, in press.
90. 3-adrenoceptor in human isolated taenia coli [Abstract]. Pharmacology of Adrenoceptors abstracts, Official Satellite of XIIth IUPHAR Congress, King of Prussia, PA, 21-23 July, 1994.