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Research

Section Review: Oncologic, Endocrine and Metabolic Adrenoceptors and imidazoline binding sites in the endocrine pancreas as targets for anti-hyperglycaemic drugs

Pages 561-569 | Published online: 03 Mar 2008

References

  • COORE HG, RANDLE PJ: Regulation of insulin secretion studied with pieces of rabbit pancreas incubated in vitro. Biocbem. J. (1964) 93:66–78.
  • MILLER RE: Pancreatic neuroendocrinokogy: peripheral neural mechanisms in the regulation of the islets of Langerhans. Endocrine Rev. (1981) 2:471–494.
  • ROBERTSON RP, HALTER JB, PORTE D: A role for alpha-adrenergic receptors in abnormal insulin secretion in diabetes mellitus. J. Clin. Invest. (1976) 57:791–795.
  • BROADSTONE VL, PFEIFER MA, BAJAJ V, STAGNER JI, SAMOLS E: a-adrenergic blockade improves glucose-po-tentiated insulin secretion in non-insulin dependent diabetes mellitus. Diabetes (1987) 36:932–937.
  • Evidence for enhanced sympathetic activity in NIDDM and illustrates the potential for use of a-adrenoceptor antagonists in management of NIDDM patients.
  • H1LSTEAD J, RICHTER E, MADSBAD S, TRONIER B, CHRIS-TENSEN NJ, HILDEBRANDT P, DAMJKER M, GALBO H: Metabolic and cardiovascular responses to epinephrine in diabetic autonomic neuropathy. N. Eng. J. Med. (1987) 317:421–426.
  • ONO S, TOMIKAWA M: a-Adrenergic hyper-responsive-ness in diabetic A-KK mice. In: Lessons from Animal Diabetes (1987) p331.
  • LACEY RJ, BERROW NS, LONDON NJM, LAKE SP, JAMES RE,SCARPELLO JHB, MORGAN NG: Differential effects of I3-adrenergic agonists on insulin secretion from pancre-atic islets isolated from rat and man. J. Mol. Endocrinol. (1990) 5:49–54.
  • ARCH JRS, AINSWORTH AT, CAWrHORNE MA, PIERCY V, SENNITT MV, THODY VE, WILSON C, WILSON S: Atypical I3-adrenoceptor on brown adipocytes as target for anti-obesity drugs. Nature (1984) 309:163–165.
  • HOLLOWAY BR, HOWE R, RAO BS, STRIBLING D: ICI 198157: a novel selective agonist of brown fat and thermogenesis. In: Obesity in Europe Libbey, London (1988) pp 323–328.
  • YOSHIDA T, H1ROAKA N, YOSHIOKA K, HASEGAWA G, KONDO M: Anti-obesity and anti-diabetic actions of 33-adrenoceptor agonist BRL 26830A in yellow ICK mice. Endocrinol. Japon (1991) 38:397–403.
  • YOSHIDA T: The anti-diabetic 133-adrenoceptor agonist BRL 26830A works by release of endogenous insulin. Am. J. Gun. Nutr. (1992) 55:237S–241S.
  • LACEY RJ, CABLE HC, JAMES RFL, LONDON NJM, SCAR-PELLO JHB, MORGAN NG: Concentration-dependent ef-fects of adrenaline on the profile of insulin secretion from isolated human islets of Langerhans. J. Endocrinol (1993) 138:555–563.
  • BUSE MG, JOHNSON AH, KUPERMINC D, BUSE J: Effect ofa-adrenergk blockade on insulin secretion in man. Metabolism (1970) 19:219–225.
  • MORGAN NG: Regulation of insulin secretion by arad-renergic agonists. Trends Pharmacol. Sct. (1987) 8:369–370.
  • MORGAN NG, HURST RD, CHAN SLF: Control of insulin secretion by aradrenergic receptor activation. Proc 5th Japan a-Receptor Conf (1989) (Excerpta Medica, Tokyo) pp 79–96.
  • SCHWINN DA: Adrenoceptors as models for G protein-coupled receptors: structure, function and regulation. Br. J. Anaesthesia (1993) 77–85.
  • An up to date review which integrates the pharmacology and molecular biology of a2-adrenoceptors.
  • YOUNG P, BERGE J, CHAPMAN H, CAWTHORNE MA: Novel a2-adrenoceptor antagonists show selectivity for a2A- and a2B-adrenoceptor subtypes. Eur. J. Pharmacol. (1989) 168:381–386.
  • First evidence for the development of antagonists that can differen-tiate between Cu-adrenoceptor subtypes.
  • CHAN SLF, MORGAN NG: Characterisation of the arad-renoceptor subtype responsible for inhibition of insu-lin secretion in isolated rat islets. In: Adrenoceptors: Structure, Mechanisms and Function (1991) Birkhauser-Ver-lag, Basel pp 311–312.
  • MORGAN NG, CHAN SLF, LACEY RJ, BROWN CA: The pharmacology and molecular biology of islet cell ad-renoceptors. In: Frontiers of Pancreatic B-Cell Research (1994) Springer International, In press
  • ANGEL I, NIDDAM R, LANGER SZ: Involvement of alpha-2-adrenergic receptor subtypes in hyperglycemia. J. Pharmacol. Exp. Ther. (1990) 254:877–882.
  • NIDDAM R, ANGEL I, BIDET 5, LANGER SZ: Pharmacologi- cal characterization of alpha-2 adrenergic receptor sub-type involved in the release of insulin from isolated rat pancreatic islets. J. Pharmacol. E. Then (1990) 254:883–887.
  • This describes the first evidence that insulin secretion is controlled by an azA-adrenoceptor in rodent islets.
  • HIEBLE JP, SULPIZIO AC, GOLDSTEIN RS: Determination of the a-adrenoceptor subtype involved in modulation of the response to glucose challenge in the rat. Pharma-col. Commun. (1992) 1:59–69.
  • Provides evidence for the involvement of an atypical a2-adrenocep-tor in regulation of insulin secretion.
  • EASON MG, LIGGEII SB: Human aradrenergic receptorsubtype distribution: widespread and subtype selective expression of cum, oc2c4 and a2c2 =RNA in multiple tissues. Mol. Pharmacol. (1993) 44:70–75.
  • CHAN SLF, MORGAN NG: Expression of mRNA for mul-tiple aradrenoceptor subtypes in insulin secreting cells. Diabetologia (1993) 36\(Supp1.1):A81.
  • ANGEL I, SCHOEMAKER H, DUVAL N, OBLIN A, SEVRIN M, LANGER SZ: SL 84.0418: a new alpha2-antagonist with anti-hyperglycaemic properties. Eur. J. Pharmacol. (1990) 183:990–991.
  • First report of the anti-hyperglycaemic activity of a novel az-antago-nist acting as an insulin secretagogue.
  • ANGEL I, SCHOEMAKER H, ARBILLA S, GALZIN AM, BERRY C, NIDDAM R, PIMOULE C, SEVRIN M, WICK A, LANGER SZ: SL 84.0418: a novel, potent and selective alpha-2 adrenoceptor antagonist:/n vitro pharmacological pro-file. J. Pharmacol. Exp. Ther. (1992) 263:1327–1333.
  • PROUTEAU M, LEVRIER J, ANGEL I: Effects of the anti-dia-betic alpha-2 adrenoceptor antagonist SL 84.0418 on plasma glucose and insulin levels following exercise in normal and type H diabetic rats. Diabetologia (1992) 35\(Supp1.1)A104.
  • GUILLOT E, ANGEL I, COSTE A, PROUTEAU M, PIVEUX B, COMTE G, LANGER SZ: Effect of alpha-2 adrenoceptor blockade by SL 86.0715 on glucose tolerance in obese zucker rats. Diabetologia (1993) 36\(Suppl. 1):A87.
  • CHAN CB, MACPHAIL RM: Functional characterization of a-adrenoceptors on pancreatic islets of fa/fa Zucker rats. Mol. Cell Endocrinol. (1992) 84:33–37.
  • SAPERSTEIN R, CHAPIN EW, BRADY EJ, SLATER EE: Effectsof an a2-adrenoceptor antagonist on glucose tolerance In the genetically obese mouse (C57BL/6J ob/ob). Meta-bolism (1990) 39:445–451.
  • BAILEY CJ, FLATT PR: Adrenoceptor-mediated control ofglucose homeostasis in obese hyperglycaemic (ob/ob) mice. Diabetes Res. (1990) 14:87–91.
  • MEURER LC, TOLMAN RL, CHAPIN EW, SAPERSTEIN R, VICARIO PP, ZRADA M, MACCOSS M: Synthesis and hy-poglycaemic activity of substituted 8-(1-Piperaz-inypimiciazo[1,2-a]pyrazines. J. Med. Chem. (1992) 35:3845–3857.
  • CHAN SLF: Role of aradrenoceptors and imidazoline- binding sites in the control of insulin secretion_ Clin. Sci. (1993) 85:671–677.
  • Timely review of the involvement of imidazoline binding sites in regulation of islet KATP channels, and insulin secretion with empha-sis on the relationship between these sites and a2-adrenoceptors.
  • KAMEDA K, ONO S, KOYAMA I, ABIKO Y: Insulin releas-ing action of 2-[2-(4,5-dihydro-1H-imidazol-2-y1)-1-phenylethyl] pyridine dihydrochloride sesquihydraix (1)6-5128), a new orally effective hypoglycaemic agent. Acta Endocrinol. (1982) 99:410–415.
  • KAWAZU S, SUZUKI M, NEGISHI K, WATANABE T, ISHII J:Studies of mid•glizole (1)6-5128) a new type of oral hypoglycaemic drug in healthy subjects. Diabetes (1987) 36:216–220.
  • KAWAZU S, SUZUKI M, NEGISHI K, ISHII J, SANDO H, KATAGIRI H, KANAZAWA Y, YAMANOUCHI S, AKANUMA Y, KAJINUMA H, SUZUKI K, WATANABE, rrox T, KO-BAYASHI T, KOSAKA K: Initial phase II clinical studies
  • In inkisgitrobe (1)6-5128). Diabetes (1987) 36:221-226. Report of the first clinical trials performed with the hypoglycaemic a2-antagonist midaglizole.
  • SCHULZ A, HASSELBLATT A: Dual action of cionidine on Insulin release: suppression but stimulation when a2-adrenoceptors are blocked. NS Archly. Pharmacol. (1989) 340:712–714.
  • DUNNE MJ: Block of ATP-regulated potassium channels by phentolamine and other alpha-adrenoceptor an-tagonists. Br. J. Pbarmacol. (1991) 103:1847–1850.
  • CHAN SLF, DUNNE MJ, STILLINGS MR, MORGAN NG: The a2-adrenoceptor antagonist efaroxan modulates KATP channels in insulin secreting cells. Eur. J. Pharmacol. (1991) 204:41–48.
  • PLANT TD, JONAS JC, HENQUIN JC: Clonidine inhibits ATP-sensitive potassium channels in mouse pancreatic O-ce1ls. Br. J. Pharmacol. (1991) 104:385–390.
  • Direct demonstration that clonidine has actions on islet cell KATP channels that are not due to a2-agonism.
  • JONAS JC, PLANT TD, HENQUIN JC: Imidazoline antago-nists of a2-adrenoceptors increase insulin release in vitro by inhibiting ATP-sensitive IC-channels in pancre-atic O-cells. Br. J. Pharmacol. (1992) 107:8–14.
  • ASHCROFT FM, ASHCROFT SJH: Properties and functions of ATP-sensitive potassium channels. Cell Signalling (1990) 2:197–214.
  • OHNEDA K, OHNEDA A, KOIZUMI F: Mechanism of Insulin secretion by midaglizole. Diabetes Res. Clin. Prac. (1993) 19:127–132.
  • CHAN SLF, MORGAN NG: Stimulation of insulin secretion by efaroxan may involve interaction with potassium channels. Eur. J. Pharmacol. (1990) 176:97–101.
  • BERRIDGE TL, DOXEY JC, ROACH AG, SMITH CFC: Selec-tivity profile of the a2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat. Eur. J. Pharmacol. (1992) 213:205–212.
  • BERRIDGE TL, DOXEY JC, ROACH AG: Comparison of the effects of efaroxan and glibenclamidP on plasma glu-cose and insulin levels in rats. Eur. J. Pharmacol. (1992) 213:213–218.
  • Provides the first evidence that imidazolines and sulphonylureas can act synergistically to increase insulin secretion.
  • CHAN SLF, BROWN CA, MORGAN NG: Stimulation of insulin secretion by the imidazoline aradrenoceptor antagonist efaroxan is mediated by a novel, stereose-lective, binding site. Eur.J.Pharmacol. (1993) 230:375-378. Direct evidence for involvement of a non-adrenergic imidazoline receptor in control of insulin secretion.
  • RONNER P, CHEONG E, KHALID P, TUMAN RW, MAT-SCHINSKY FM: Effect of linogliride on hormone release from perfused rat pancreas - fuel dependence and desensitization by tolbutamide. Diabetes (1991) 40:878–884.
  • STRUTHERS AD, BROWN DC, BROWN MJ, SCHUMER B,BLOOM SR: Selective az-receptor blockade facilitates the Insulin response to adrenaline but not to glucose in man. Clin. Endocrinol. (1985) 23:539–546.
  • BROWN CA, LOWETH AC, SMITH SA, MORGAN NG: Stimu-lation of insulin secretion by imidazoline compounds Is not due to interaction with non-adrenoceptor ida-zoxan binding sites. Br. J. Pharmacol. (1993) 108:312–317.
  • REMAURY A, PARIS H: The insulin secreting cell line RINm5F expresses an alpha-213 adrenoceptor and nonadrenergic idazoxan binding sites. J. Pharmacol. Exp. Ther. (1992) 260:417–426.
  • ERNSBERGER PR, WESTBROOKS KL, CHRISTEN MO, SCHAFER SG: A second generation of centrally acting antihypertensive agents act on putative Il-imidazoline receptors. J. Cardiovasc. Pharmacol. (1992) 20\(Suppl. 4):S1–S10 .
  • HENQUIN JC, GARRINO MG, NENQUIN M: Stimulation ofInsulin release by benzoic acid derivatives related to the non-sulphonylurea moiety of glibenclamkir- structural requirements and cellular mechanisms. Eur. J. Pharma-col. (1987) 141:243–251.
  • GARRINO MG, HENQUIN JC: Highly potent and stereose-lective effects of benzoic add derivative AZ-DF 265 on pancreatic O-cells. Br. J. Pharmacol. (1998) 93:61–68.
  • RONNER P, HANG 'a, KRAEBBER MJ, HIGGINS TJ: Effect of the hypoglycaemic drug (-)-AZ-DF-265 on ATP-sensi-tive potassium channels in rat pancreatic O-cells. Br. J. Pharmacol. (1992) 106:250–255.
  • Evidence for interaction of a non-sulphonylurea drug with the sulphonylurea receptor in the pancreatic B-cell.
  • TUTMAN RW, MORRIS DM, BRYAN DJ, WALLACE NH, VOINIA SJ, BOWDEN CR, TUTWILER GF: Comparative effects of linogliride fumarate and tolbutamide sodium on insulin secretion and glucose utilization in rat pan-creatic islets. Drug Develop. Res. (1991) 24:355–363.
  • RONNER P, HIGGINS TJ, KIMMICH GA: Inhibition of ATP-sensitive IC channels in pancreatic I3-cells by non-sulfonylurea drug linogliride. Diabetes (1991) 40:885–892.
  • BRESLIN HJ, KUKLA MJ, TUMAN RW, REBARCHAK MC, BOWDEN CR: A novel series of N-(1-aminoalky-lidene)carboximidamides as potential hypoglycaemic agents. J. Med. Chem. (1993) 36:1597–1603.
  • JONAS JC, PLANT TD, ANGEL I, LANGER SZ, HENQUIN JC: is vitro stimulation of insulin release by SL 84.0418, a new a2-adrenoceptor antagonist. Eur. J. Pharmacol. (1994) 254:27–33.

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