Modulation of sibutramine-induced increases in extracellular noradrenaline concentration in rat frontal cortex and hypothalamus by α2-adrenoceptors

British Journal of Pharmacology

Volumn 128, Issue 3, 1999, Pages 659-666

  Wortley, K E ^a   Heal, D J ^b   Stanford, S C ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

^b ABBOTT LABORATORIES   (United States)

Author keywords

2 adrenoceptors; Frontal cortex; Hypothalamus; In vivo microdialysis; Noradrenaline; RX821002; Sibutramine

Indexed keywords

2 (2 METHOXY 1,4 BENZODIOXAN 2 YL) 2 IMIDAZOLINE; ALPHA 2 ADRENERGIC RECEPTOR; NORADRENALIN; PRESYNAPTIC RECEPTOR; SIBUTRAMINE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; FRONTAL CORTEX; HYPOTHALAMUS; INTRAPERITONEAL DRUG ADMINISTRATION; LATENT PERIOD; MALE; MICRODIALYSIS; NONHUMAN; NORADRENALIN RELEASE; PRIORITY JOURNAL; RAT;

ADRENERGIC ALPHA-ANTAGONISTS; ANIMALS; APPETITE DEPRESSANTS; CYCLOBUTANES; DIALYSIS; FRONTAL LOBE; HYPOTHALAMUS; IDAZOXAN; IMIDAZOLES; MALE; NOREPINEPHRINE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ADRENERGIC, ALPHA-2;

EID: 0032701288     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702859     Document Type: Article

References (41)

1. CEDARBAUM, J.M. & AGHAJANIAN, G.K. (1976). Noradrenergic neurons of the locus coeruleus: inhibition by epinephrine and activation by the α-antagonist piperoxane. Brain Res., 112, 413-419.
2. 3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacol., 35, 63-70.
3. CHEETHAM, S.C., VIGGERS, J.A., SLATER, N.A., HEAL, D.J. & BUCKETT, W.R. (1993). [3H]Paroxetine binding in rat frontal cortex strongly correlates with [3H]5-HT uptake: Effect of administration of various antidepressant treatments. Neuropharmacol., 32, 737-743.
4. 2-adrenoceptor agonists, medetomidine, clonidine and UK 14,304 on extraneuronal levels of noradrenaline in the rat frontal cortex: evaluation using in vivo microdialysis and synaptosomal uptake studies. Br. J. Pharmacol., 114, 1717-1723.
5. 2-adrenoceptors play a major role in the effects of idazoxan on cortical noradrenaline (as measured by in vivo dialysis) in the rat. J. Pharmacol. Exp. Ther., 241, 642-649.
6. 2-Adrenergic receptor blockade markedly potentiates duloxetine-and fluoxetine-induced increases in noradrenaline, dopamine, and serotonin levels in the frontal cortex of freely-moving rats. J. Neurochem., 69, 2616-2619.
7. 2-noradrenergic receptors mediate feeding induced by paraventricular nucleus injection of norepinephrine and clonidine. Eur. J. Pharmacol., 115, 11-19.
8. GROSSMAN, S.P. (1960). Eating and drinking elicited by direct adrenergic or cholinergic stimulation of the hypothalamus. Science, 132, 301-302.
9. GROSSMAN, S.P. (1975). Role of the hypothalamus in the regulation of food and water intake. Psychol. Rev., 82, 200-224.
10. GUNDLAH, C., MARTIN, K.F., HEAL, D.J. & AUERBACH, S.B. (1997). In vivo criteria to differentiate monoamine uptake inhibitors from releasing drugs: Sibutramine is a reuptake inhibitor. J. Pharmacol. Exp. Ther., 283, 581-591.
11. HALFORD, J.C.G., HEAL, D.J. & BLUNDELL, J.E. (1995). Effects in the rat of sibutramine on food intake and the behavioural satiety sequence. Br. J. Pharmacol., 114, 387P.
12. HEAL, D.J., ASPLEY, S., PROW, M.R., JACKSON, H.C., MARTIN, K.F. & CHEETHAM, S.C. (1998). Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int. J. Obesity, 22 (Suppl 1):S18-S28.
13. 2-adrenoceptors in rat brain after short-term DSP-4 lesioning. Eur. J. Pharmacol., 249, 37-41.
14. HEAL, D.J. & CHEETHAM, S.C. (1997). The pharmacology of sibutramine, the first serotonin and noradrenaline reuptake inhibitor to be developed for the treatment of obesity. La lettre du pharmacologue, 11 (Suppl 10): 3-8.
15. HOLETS, V.R. (1990). The anatomy and function of noradrenaline in the mammalian brain. In: Heal, D.J. & Marsdon, C.A. (eds). The pharmacology of noradrenaline in the central nervous system. Oxford Medical Publications: Oxford, pp 1-40.
16. JACKSON, H.C., BEARHAM, M.C., HUTCHINS, L.J., MAZURKIEWICZ, S.E., NEEDHAM, A.M. & HEAL, D.J. (1997a). Investigation of the mechanisms underlying the hypophagic effects of the 5-HT and noradrenaline reuptake inhibitor, sibutramine, in the rat. Br. J. Pharmacol., 121, 1613-1618.
17. JACKSON, H.C., NEEDHAM, A.M., HUTCHINS, L.J., MAZURKIEWICZ, S.E. & HEAL, D.J. (1997b). Comparison of the effects of sibutramine and other monoamine reuptake inhibitors on food intake in the rat. Br. J. Pharmacol., 121, 1758-1762.
18. 2-adrenoceptor antagonists BRL 44408 and ARC 239 also recognize 5-HT1A receptors in the rat brain. Eur. J. Pharmacol., 312, 385-388.
19. JONSSON, G., HALLMAN, H., PONZIO, F. & ROSS, F. (1981). DSP-4 (N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine) - a useful denervation tool for central and peripheral noradrenaline neurons. Eur. J. Pharmacol., 72, 173-188.
20. 2-adrenoceptor antagonist, atipamezole, on hypothalamic histamine and noradrenaline release in vivo. Eur. J. Pharmacol., 285, 255-260.
21. LANGER, S.Z. (1977). Sixth Gaddum memorial lecture, National Institute for Medical Research, Mill Hill, Presynaptic receptors and their role in the regulation of transmitter release. Br. J. Pharmacol., 60, 481-497.
22. LANGIN, D., PARIS, H. & LAFONTAN, M. (1990). Binding of [3H]idazoxan and of ils methoxy derivative [3H]RX821002 in human fat cells: [3H]idazoxan but not [3H]RX821002 labels additional non-alpha2-adrenergic binding sites. Mol. Pharmacol., 37, 876-885.
23. LEIBOWITZ, S.F. (1976). Brain catecholaminergic mechanisms for the control of hunger. In: Novin, D., Wyrwicka, W. & Bray, G. (eds). Hunger: basic mechanisms and clinical implications. Raven Press: New York, pp 1-18.
24. LEIBOWITZ, S.F. (1978). Paraventricular nucleus: a primary site mediating adrenergic stimulation of feeding and drinking. Pharmacol. Biochem. Behav., 8, 163-175.
25. L'HEUREUX, R.L., DENNIS, T., CURET, O. & SCATTON, B. (1986). Measurement of endogenous noradrenaline release in the rat cerebral cortex in vivo by transcortical dialysis: Effects of drugs affecting noradrenergic transmission. J. Neurochem., 46, 1794-1801.
26. LUSCOMBE, G.P., HOPCROFT, R.H., THOMAS, P.C. & BUCKETT, W.R. (1989). The contribution of metabolites to the rapid and potent down-regulation of rat cortical β-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacol., 28, 129-134.
27. 2-adrenoceptors in the locus coeruleus are involved in the in vivo modulation of cortical noradrenaline release by the antidepressant desipramine. J. Neurochem., 71, 790-798.
28. MATTHEWS, J.W., BOOTH, D.A. & STOLERMAN, I.P. (1977). Factors influencing feeding elicited by intracranial noradrenaline in rats. Brain Res. 141, 119-128.
29. NORUSIS, M.J. (1988). SPSS/PC + ™ V2.0 Base Manual for the IBM PC/XT/AT and PS/2. Chicago. U.S.A. SPSS Inc.
30. PAXINOS, G. & WATSON, C. (1986). The rat brain in stereotaxic coordinates. Academic Press, Australia.
31. SANDBERG, M., BUTCHER, S.P. & HAGBERG, H. (1986). Extracellular overflow of neuroactive amino acids during severe insulin-induced hypoglycemia: in vivo dialysis of the rat hippocampus. J. Neurochem., 47, 178-184.
32. 2-adrenoceptor antagonist. Eur. J. Pharmacol., 151, 35-42.
33. 2-and β-adrenoceptors in different regions of rat brain. Neurosci., 8, 161-164.
34. STOCK, M.J. (1997). Sibutramine: a review of the pharmacology of a novel anti-obesity agent. Int. J. Obes., 21 (Suppl 1): S25-S29.
35. U'PRICHARD, D.C., GREENBERG, D.A. & SNYDER, S.H. (1977). Binding characteristics of a radiolabelled agonist and antagonist at central nervous system alpha noradrenergic receptors. Mol. Pharmacol., 13, 454-473.
36. VAN VELDHUIZEN, M.J., FEENSTRA, M.G.P., HEINSBROEK, R.P.W. & BOER, G.J. (1993). In vivo microdialysis of noradrenaline overflow: Effects of α-adrenoceptor agonists and antagonists measured by cumulative concentration-response curves. Br. J. Pharmacol., 109, 655-660.
37. 3H]idazoxan. Neurochem. Int., 17, 537-546.
38. WELLMAN, P.J. (1992). Overview of adrenergic anorectic agents. Am. J. Clin. Nutr., 55, 193S-198S.
39. WINTER, J.C. & RABIN, R.A. (1992). Yohimbine as a serotonergic agent: Evidence from receptor binding and drug discrimination. J. Pharmacol. Exp. Ther., 263, 682-689.
40. 2-adrenoceptors. Br. J. Pharmacol., 127, 1860-1866.
41. ZACZEK, R., FRITSCHY, J.M., CULP, S., DE SOUZA, E.B. & GRZANNA, R. (1990). Differential effects of DSP-4 on noradrenaline axons in cerebral cortex and hypothalamus may reflect heterogeneity of noradrenaline uptake sites. Brain. Res., 522, 308-314.