Clinical pharmacology of β3-adrenoceptors

British Journal of Clinical Pharmacology

Volumn 42, Issue 3, 1996, Pages 291-300

  Lipworth, Brian J ^a  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

Author keywords

Lipolysis; Thermogenesis; 3 adrenoceptors

Indexed keywords

4 [2 [(2 HYDROXY 2 PHENYLETHYL)AMINO]PROPYL]BENZOIC ACID METHYL ESTER HYDROGEN MALEATE; 4 [2 [[2 (3 CHLOROPHENYL) 2 HYDROXYETHYL]AMINO]PROPYL]PHENOXYACETIC ACID METHYL ESTER; ATENOLOL; BETA 3 ADRENERGIC RECEPTOR; BISOPROLOL; ISOPRENALINE; NADOLOL; RECEPTOR SUBTYPE; SALBUTAMOL;

ADIPOSE TISSUE; GENETIC POLYMORPHISM; GLUCOSE METABOLISM; HISTOCHEMISTRY; HUMAN; LIPID METABOLISM; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; OBESITY; PRIORITY JOURNAL; RECEPTOR BINDING; REVIEW; THERMOGENESIS;

EID: 0029793561     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1996.04222.x     Document Type: Review

References (70)

1. Lands AM, Arnold AA, McAuliff JP, Luduena FP, Brown TG. Differentiation of receptor systems activated by sympathomimetic amines. Nature 1967; 214: 597-598.
2. Tan S, Curtis-Prior PB. Characterization of the beta-adrenoceptor of the adipose cell of the rat. Int J Obesity 1983; 7: 409-414.
3. Emorine LJ, Marullo S, Briend-Sutren M-M, Patey G, Tate K, Dalavier-Klutchko C, Strosberg AD. Molecular characterization of the human beta 3-adrenergic receptor. Science 1989; 245: 1118-1121.
4. Granneman JG, Lahners KN, Chaudhry A. Molecular cloning and expression of the rat beta 3-adrenergic receptor. Mol Pharmacol 1991; 40: 895-899.
5. Granneman JG, Lahners KN, Chaudhry A. Characterisation of the human beta 3-adrenergic receptor gene. Mol Pharmacol 1993; 44: 264-270.
6. Arch JR, Ainsworth AT, Cawthorne MA, et al. Atypical beta-adrenoceptor on brown adipocytes as target for anti-obesity drugs. Nature 1984; 309: 163-165.
7. Wilson C, Wilson S, Piercy V, Sennitt MV, Arch, JRS. The rat lipolytic beta-adrenoceptor: Studies using novel beta-adrenoceptor agonists. Eur J Pharmacol 1984; 100: 309-319.
8. Hollenga, CH, Zaagsma J. Direct evidence for the atypical nature of functional beta-adrenoceptors in rat adipocytes. Br J Pharmacol 1989; 98: 1420-1424.
9. Hollenga C, Hass M, Deinum JT, Zaagsma J. Discrepancies in lipolytic activities induced by β-adrenoceptor agonists in human and rat adipocyles. Horm Metabol Res 1990; 22: 17-21.
10. 1-receptor down-regulation in heart failure. Circ Res 1986; 59: 297-309.
11. 2-adrenoceptor responses after regular twice-daily treatment with eformoterol dry powder in asthmatic patients. Thorax 1995; 50: 497-504.
12. Granneman JG, Lahners KN. Differential adrenergic regulation of beta-1 and beta 3-adrenoceptor messenger ribonucleic acids in adipose tissues. Endocrinology 1992; 130: 109-114.
13. Granneman JG. Effects of agonist exposure on the coupling of beta 1- and beta 3-adrenergic receptors to adenyl cyclase in isolated adipocytes. J Pharmacol Exp Ther 1992; 261: 638-642.
14. Carpene C, Galitzky J, Collon P, Esclapez F, Dauzats M, La -fontan M. Desensitization of beta 1- and beta 2- but not beta 3-adrenoceptor-mediated lipolytic responses of adipocytes after long-term norepinephrine infusion. J Pharmacol Exp Ther 1993; 265: 237-247.
15. Thomas RF, Holt BD, Schwinn DA, Liggett SB. Long-term agonist exposure induces upregulation of beta 3-adrenergic receptor expression via multiple cAMP response elements. Proc Natl Acad Sci 1992; 89: 4490-4494.
16. Liggett SB, Freedman NJ, Schwinn DA, Lefkowitz, RJ. Structural basis for receptor subtype-specific regulation revealed by a chimeric beta 3/beta 2-adrenergic receptor. Proc Natl Acad Sci 1993, 90: 3665-3669.
17. Bond RA, Clarke DE. A response to isoprenaline unrelated to alpha- and beta-adrenoceptor agonism. Br J Pharmacol 1987; 91: 683-686.
18. Bond RA, Blue DR, Clarke DE. An adrenoceptor with distinct characteristics from the alpha- and beta-subtypes. Br J Pharmacol 1988; 93: 21P.
19. Norman BJ, Leathard HL. Evidence that an atypical beta-adrenoceptor mediates the inhibition of spontaneous rhythmical contractions of rabbit isolated jejunum induced by ritodrine and salbutamol. Br J Pharmacol 1990; 101: 27-30.
20. Ford APDW, Taneja DT, Clarke DE. Atypical beta-adrenoceptor-mediated relaxation and cyclic AMP formation in tunica muscularis mucosae (TMM) of the rat oesophagus. Br J Pharmacol 1992; 105: 235P.
21. de Boer RE, Brouwer F, Zaagsma J. The beta-adrenoceptors mediating relaxation of rat oesophageal muscularis mucosae are predominantly of the beta 3-, but also of the beta 2-subtype. Br J Pharmacol 1993; 110: 442-446.
22. Nials AT, Barker RC, Coleman RA, Vardey CJ. Further characterisation of the atypical beta-adrenoceptors in guinea-pig gastric fundus. Br J Pharmacol 1992; 106: 66P.
23. Croci T, Cecchi R, Tarantino A, et al. Inhibition of rat colon motility by stimulation of atypical beta-adrenoceptors with new gut-specific agents. Pharmacol Res Commun 1988; 20: 147-151.
24. Bianchetti A, Manara L. In vitro inhibition of intestinal motility by phenylethanolaminotetralines: evidence of atypical beta-adrenoceptors in rat colon. Br J Pharmacol 1990; 100: 831-839.
25. Bianchetti A, Manara L, Codegoni AM, Bizzi A. Atypical beta-adrenoceptors account for inhibition of rat colon motility and lipolytic action of phenylethanolaminotetralines. Eur J Pharmacol 1990; 183: 2196-2197.
26. Challiss RA, Leighton B, Wilson S, Thurlby PL, Arch JRS. An investigation of the beta-adrenoceptor that mediates metabolic responses to the novel agonist BRL 28410 in rat soleus muscle. Biochem Pharmacol 1988; 37: 947-950.
27. 125I]-cyanopindolol binding sites in rat soleus muscle. Br J Pharmacol 1993; 109: 344-352.
28. Webber SE, Stock MJ. Evidence for an atypical, or beta 3-adrenoceptor in ferret tracheal epithelium. Br J Pharmacol 1992; 205: 857-862.
29. Tamaoki J, Kondo M, Chiyotani A, Yamauchi F, Takeuchi S, Konno K. Airway epithelial beta 3-adrenergic receptor: effect on bio-electric properties and its mechanism of action. Nippon Kyobu Shikkan Gakkai Zasshi-Jap J Thorac Dis 1992; 30: 310-316.
30. Tamaoki J, Yamauchi F, Chiyotani A, Yamawaki I, Takeuchi S, Konno K. Atypical beta-adrenoceptor- (beta 3-adrenoceptor) mediated relaxation of canine isolated bronchial smooth muscle. J Appl Physiol 1993; 74: 297-302.
31. Itabashi S, Aikawa T, Sekizaswa K, Sasaki H, Takishima T. Evidence that an atypical beta-adrenoceptor mediates the prejunctional inhibition of non-adrenergic non-cholinergic contraction in guinea-pig bronchi. Eur J Pharmacol 1992; 218: 187-190.
32. 3-adrenoceptor agonist, BRL37344 and SR58611A, do not induce relaxation in human, sheep and guinea-pig airway smooth muscle in vitro. Eur Respir J 1994; 7: 1610-1615.
33. Takeyama K, Tamaoki J, Chiyuotani A, Sakai N, Konno K. Stimulation of ciliary motility by beta 3-adrenoceptor agonist in rabbit tracheal epithelium. Kokyu to Junkan-Resp & Circ 1993; 41: 993-997.
34. Tamaoki J, Chiyotani A, Sakai N, Konno K. Stimulation of ciliary motility mediated by atypical beta-adrenoceptor in canine bronchial epithelium. Life Sci 1993; 53: 1509-1515.
35. 4-induced guinea pig eosinophil chemotaxis. Agents Actions 1992; 37: 232-237.
36. Kaumann AJ. Is there a third heart beta-adrenoceptor? Trends Pharmacol Sci 1989; 10: 316-320.
37. Tavernier G, Galitzky J, Bousquet-Melou A, Montastruc JL, Berlan M. The positive chronotropic effect induced by BRL 37344 and CGP 12177, two beta-3 adrenergic agonists, does not involve cardiac beta adrenoceptors but baroreflex mechanisms. J Pharmacol Exp Ther 1992; 263: 1083-1090.
38. Takeyama S, Furukawa Y, Ren LM, Inove Y, Sawaki S, Chiba S. Positive chrontropic and inotropic responses to BRL 37344, a beta-3 adrenoceptor agonist in isolated blood perfused dog atria. Eur J Pharmacol 1993; 231: 315-321.
39. 3-adrenergic receptor mRNA in man. J Clin Invest 1993; 91: 344-349.
40. 3-adrenoceptor receptor and an increased capacity to gain weight in patients with morbid obesity. N Engl J Med 1995; 333: 352-354.
41. 3-adrenoceptor gene. N Engl J Med 1995; 333: 343-347.
42. 3-adrenoceptor gene with features of the insulin resistance syndrome in Finns. N Engl J Med 1995; 333: 348-351.
43. Arch JR, Piercy V, Wilson C, Wilson S. Characterization of the rat lipolytic beta-adrenoceptor using novel beta-adrenoceptor agonists. Br J Pharmacol 1983; 77: 481P (abstr).
44. Zed CA, Harris GS, Harrison PJ, Robb GH. Anti-obesity activity of a novel beta-adrenoceptor agonist (BRL 26830A) in diet-restricted obese subjects. Int J Obesity 1985; 9: 231.
45. Connacher AA, Jung RT, Mitchell PEG. Weight loss in obese subjects on a restricted dies given BRL 26830A, a new atypical beta-adrenoceptor agonist. Br Med J 1988; 296: 1217-1220.
46. Connacher AA, Lakie M, Powers N, Elton RA, Walsh EG, Jung RT. Tremor and anti-obesity drug BRL 26830A. Br J Clin Pharmacol 1990; 30: 613-615.
47. 3-adrenoceptors mediate metabolic responses to isoprenaline? Quart J Med 1993; 86: 595-600.
48. Wheeldon NM, McDevitt DG, McFarlane LC, Lipworth, BJ. β-adrenoceptor subtypes mediating the metabolic effects of BRL35135 in man. Clin Sci 1994; 86: 331-337.
49. Henny C, Schutz Y, Buckert A, Meylan M, Jequier E, Felber J-P. Thermogenic effect of the new beta-adrenoceptor agonist Ro 16-8714 in healthy male volunteers. Int J Obesity 1987; 11: 473-483.
50. Henny C, Buckert A, Schutz Y, Jequier E, Felber JP. Comparison of thermogenic activity induced by the new sympathomimetic Ro 16-8714 between normal and obese subjects. Int J Obesity 1988; 12: 227-236.
51. Munger R, Buckert A, Jequier E, Felber J.-P. Thermogenic effect of the new beta-adrenoceptor agonist Ro 40-2148 in healthy male volunteers. Diabetes 1990; 39 (Suppl. 1): Abstract 1100.
52. Holloway BR, Howe R, Rao BS, et al. ICI D7114a novel selective beta-adrenoceptor agonist selectively stimulates brown fat and increases whole-body oxygen consumption. Br J Pharmacol 1991; 104: 97-104.
53. Goldberg GR, Prentice AM, Haines W, Murgatroyd, PR. Effect of a specific beta 3-agonist (ICI D7114) on energy expenditure in healthy volunteers. Int J Obesity 1992; 16: 151.
54. Toubro S, Astrup A, Hardman M. The effect of a beta 3-agonist on 24 hour energy expenditure and lipid oxidation in obese patients. Int J Obesity 1993; 17 (Suppl. 2): 73.
55. Bloom JD, Dutia MD, Johnson BD, et al. Disodium (R,R)-5-[2[[2-(3-Chlorophenyl)-2-hydroxyethyl] amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent. J Med Chem 1992; 35: 3081-3084.
56. Cawthorne MA, Carroll MJ, Levy AL, et al. Effects of novel beta-adrenoceptor agonists on carbohydrate metabolism: relevance for the treatment of non-insulin-dependent diabetes. Int J Obesity 1984; 8 (Suppl. 1): 93-102.
57. Smith SA, Levy AL, Sennitt MV, Simson DL, Cawthorne MA. Effects of BRL 26830, a novel beta-adrenoceptor agonist, on glucose tolerance, insulin sensitivity and glucose turnover in Zucker (fa/fa) rats. Biochem Pharmacol 1985; 34: 2425-2429.
58. Sennitt MV, Arch JR, Levy AL, Simon DL, Smith SA, Cawthorne MA. Anti-hyperglycaemic action of BRL 26830, a novel beta-adrenoceptor agonist, in mice and rats. Biochem Pharmacol 1985; 34: 1279-1285.
59. Smith SA, Cawthorne MA, Fay LC, McCullough DA, Mitchell TH. Effect of a novel beta-adrenoceptor agonist on insulin sensitivity in lean healthy male volunteers. Diabetes 1987; 36 (Suppl 1): 58.
60. Connacher AA, Bennet WM, Jung RT. Rennie MJ. Metabolic effects of three weeks administration of the beta-adrenoceptor agonist BRL 26830A. Int J Obesity 1992; 16: 685-694.
61. Sennitt MV, Smith SA, Cawthorne MA. Anti-hyperglycaemic activity in rats and mice of BRL 35135, a novel beta-adrenoceptor agonist. Diabetes 1986; 35 (Suppl. 1): 262.
62. Cawthorne MA, Young P, Smith SA. Effects of BRL 35135, a novel type of beta-adrenoceptor agonist, on glucose tolerance and insulin sensitivity in obese Zucker rats. Diabetes 1986; 35 (Suppl. 1): 263.
63. Mitchell TH, Ellis RD, Smith SA, Robb G, Cawthorne MA. Effects of BRL 35135, a beta-adrenoceptor agonist with novel selectivity, on glucose tolerance and insulin sensitivity in obese subjects. Int J Obesity 1989; 13: 757-766.
64. Cawthorne MA, Sennitt MV, Arch JR, Smith SA. BRL 35135, a potent and selective atypical beta-adrenoceptor agonist. Am J Clin Nutr 1992; 55: 252S-257S.
65. 3-adrenoceptor agonist BRL 35135 in man. Br J Clin Pharmacol 1994; 37: 363-369.
66. 3-adrenoceptors in man. Quart J Med 1993; 86: 255-261.
67. 3-adrenoceptor agonist ZD 2079 in the cardiac response to intravenous isoprenaline in healthy male volunteers. Br J Clin Pharmacol 1995; 319: 581P.
68. 3-adrenoceptor agonist ZD 2079 in the chronotropic and inotropic response to exercise in healthy male volunteers. Br J Clin Pharmacol 1995; 39: 582P.
69. 3-adrenoceptor agonist. Br J Pharmacol 1994; 112 (Suppl): 213P.
70. Newnham DM, Ingram CG, Mackie A, Lipworth BJ. β-adrenal sub-types mediating the airways response to BRL 35135 in man. Br J Clin Pharmacol 1993; 36: 567-571.