Leptin potentiates the anti-obesity effects of rimonabant

European Journal of Pharmacology

Volumn 658, Issue 2-3, 2011, Pages 270-276

  Boustany Kari, Carine M ^a   Jackson, V Margaret ^a   Gibbons, Colleen P ^a   Swick, Andrew G ^a,b  

^a PFIZER INC   (United States)

^b IL   (United States)

Author keywords

Cannabinoid receptor; Energy expenditure; Energy intake; Hypothalamus; Leptin; Obesity

Indexed keywords

LEPTIN; RIMONABANT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARCUATE NUCLEUS; ARTICLE; BRAIN SLICE; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; DRUG POTENTIATION; FOOD INTAKE; HYPOTHALAMUS VENTROMEDIAL NUCLEUS; LIPID DIET; LOW DRUG DOSE; MALE; MONOTHERAPY; NEUROMODULATION; NONHUMAN; OBESITY; PRIORITY JOURNAL; RAT; REBOUND; TREATMENT DURATION; WEIGHT CHANGE; WEIGHT REDUCTION;

ANIMALS; ANTI-OBESITY AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SYNERGISM; LEPTIN; MALE; PIPERIDINES; PYRAZOLES; RATS; RATS, SPRAGUE-DAWLEY; RECURRENCE; VENTROMEDIAL HYPOTHALAMIC NUCLEUS; WEIGHT LOSS;

EID: 79953790285     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2011.02.021     Document Type: Article

References (43)

1. Alonso, R., Voutsinos, B., Fournier, M., Labie, C., Steinberg, R., Souilhac, J., Le Fur, G., Soubrié, P., 1999. Blockade of cannabinoid receptors by SR141716 selectively increases Fos expression in rat mesocorticolimbic areas via reduced dopamine D2 function. Neuroscience 91, 607-620. (Pubitemid 29193270)
2. Bingham, N.C., Anderson, K.K., Reuter, A.L., Stallings, N.R., Parker, K.L., 2008. Selective loss of leptin receptors in the ventromedial hypothalamic nucleus results in increased adiposity and a metabolic syndrome. Endocrinology 149, 2138-2148. (Pubitemid 351574486)
3. Boozer, C.N., Leibel, R.L., Love, R.J., Cha, M.C., Aronne, L.J., 2001. Synergy of sibutramine and low-dose leptin in treatment of diet-induced obesity in rats. Metabolism 50, 889-893. (Pubitemid 32755004)
4. Browning, K.N., Travagli, R.A., 2006. Short-term receptor trafficking in the dorsal vagal complex: an overview. Auton. Neurosci. 126-127, 2-8.
5. Choi, S., Dallman, M.F., 1999. Hypothalamic obesity: multiple routes mediated by loss of function in medial cell groups. Endocrinology 140, 4081-4088. (Pubitemid 30647104)
6. Cota, D., Marsicano, G., Tschöp, M., Grübler, Y., Flachskamm, C., Schubert, M., Auer, D., Yassouridis, A., Thöne-Reineke, C., Ortmann, S., Tomassoni, F., Cervino, C., Nisoli, E., Linthorst, A.C., Pasquali, R., Lutz, B., Stalla, G.K., Pagotto, U., 2003. The endogenous cannabinoid system affects energy balance via central orexigenic drive and peripheral lipogenesis. J. Clin. Investig. 112, 423-431.
7. Cowley, M.A., Cone, R.D., Enriori, P., Louiselle, I., Williams, S.M., Evans, A.E., 2003. Electrophysiological actions of peripheral hormones on melanocortin neurons. Ann. NY Acad. Sci. 994, 175-186.
8. Dhillon, H., Zigman, J.M., Ye, C., Lee, C.E., McGovern, R.A., Tang, V., Kenny, C.D., Christiansen, L.M., White, R.D., Edelstein, E.A., Coppari, R., Balthasar, N., Cowley, M.A., Chua, J.S., Elmquist, J.K., Lowell, B.B., 2006. Leptin directly activates SF1 neurons in the VMH, and this action by leptin is required for normal body-weight homeostasis. Neuron 49, 191-203. (Pubitemid 43089637)
9. Di Marzo, V., Despres, J.-P., 2009. CB1 antagonists for obesity - what lessons have we learned from rimonabant? Nat. Rev. Endocrinol. 5, 633-638.
10. Di Marzo, V., Matias, I., 2005. Endocannabinoid control of food intake and energy balance. Nat. Neurosci. 8, 585-589.
11. Di Marzo, V., Goparaju, S.K., Wang, L., Liu, J., Batkai, S., Jarai, Z., Fezza, F., Miura, G.I., Palmiter, R.D., Sugiura, T., Kunos, G., 2001. Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 410, 822-825. (Pubitemid 32303781)
12. Enriori, P.J., Evans, A.E., Sinnayah, P., Cowley, M.A., 2006. Leptin resistance and obesity. Obesity 14, 254S-258S.
13. Flegal, K.M., Carroll, M.D., Ogden, C.L., Johnson, C.L., 2002. Prevalence and trends in obesity among US adults, 1999-2000. J. Am. Med. Assoc. 288, 1723-1727.
14. Herling, A.W., Kilp, S., Elvert, R., Haschke, G., Kramer, W., 2008a. Increased energy expenditure contributes more to the body weight-reducing effect of rimonabant than reduced food intake in candy-fed Wistar rats. Endocrinology 149, 2557-2566. (Pubitemid 351574492)
15. Herling, A.W., Kilp, S., Juretschke, H.P., Neumann-Haefelin, C., Gerl, M., Kramer, W., 2008b. Reversal of visceral adiposity in candy-diet fed female Wistar rats by the CB1 receptor antagonist rimonabant. Int. J. Obes. 32, 1363-1372.
16. Irani, B.G., Le Foll, C., Dunn-Meynell, A., Levin, B.E., 2008. Effects of leptin on rat ventromedial hypothalamic neurons. Endocrinology 149, 5146-5154.
17. Jacob, R.J., Dziura, J., Medwick, M.B., Leone, P., Caprio, S., During, M., Shulman, G.I., Sherwin, R.S., 1997. The effect of leptin is enhanced by microinjection into the ventromedial hypothalamus. Diabetes 46, 150-152. (Pubitemid 27009964)
18. Kim, M.S., Park, J.Y., Namkoong, C., Jang, P.G., Ryu, J.W., Song, H.S., Yun, J.Y., Namgoong, I.S., Ha, J., Park, I.S., Lee, I.K., Viollet, B., Youn, J.H., Lee, H.K., Lee, K.U., 2004. Anti-obesity effects of [alpha]-lipoic acidmediated by suppression of hypothalamicAMP-activated protein kinase. Nat. Med. 10, 727-733.
19. Kim, K.W., Jo, Y.H., Zhao, L., Stallings, N.R., Chua Jr., S.C., Parker, K.L., 2008. Steroidogenic factor 1 regulates expression of the cannabinoid receptor 1 in the ventromedial hypothalamic nucleus. Mol. Endocrinol. 22, 1950-1961.
20. King, B.M., 2006. The rise, fall, and resurrection of the ventromedial hypothalamus in the regulation of feeding behavior and body weight. Physiol. Behav. 87, 221-244.
21. Kiss, J., Csaba, Z., Csáki, A., Halász, B., 2005. Glutamatergic innervation of neuropeptide Y and pro-opiomelanocortin-containing neurons in the hypothalamic arcuate nucleus of the rat. Eur. J. Neurosci. 21, 2111-2119.
22. Kola, B., Hubina, E., Tucci, S.A., Kirkham, T.C., Garcia, E.A., Mitchell, S.E., Williams, L.M., Hawley, S.A., Hardie, D.G., Grossman, A.B., Korbonits, M., 2005. Cannabinoids and ghrelin have both central and peripheral metabolic and cardiac effects via AMPactivated protein kinase. J. Biol. Chem. 280, 25196-25201.
23. Kunz, I., Meier, M.K., Bourson, A., Fisseha, M., Schilling, W., 2008. Effects of rimonabant, a cannabinoid CB1 receptor ligand, on energy expenditure in lean rats. Int. J. Obes. 32, 863-870.
24. Levin, B.E., Dunn-Meynell, A.A., 2002. Reduced central leptin sensitivity in rats with diet-induced obesity. Am. J. Physiol. Regul. Integr. Comp. Physiol. 283, R941-R948.
25. Minokoshi, Y., Alquier, T., Furukawa, N., Kim, Y.-B., Lee, A., Xue, B., Mu, J., Foufelle, F., Ferre, P., Birnbaum, M.J., Stuck, B.J., Kahn, B.B., 2004. AMP-kinase regulates food intake by responding to hormonal and nutrient signals in the hypothalamus. Nature 428, 569-574. (Pubitemid 38480541)
26. Nguyen, Q.H., Wagner, E.J., 2006. Estrogen differentially modulates the cannabinoidinduced presynaptic inhibition of amino acid neurotransmission in proopiomelanocortin neurons of the arcuate nucleus. Neuroendocrinology 84, 123-137. (Pubitemid 46141720)
27. Nogueiras, R., Veyrat-Durebex, C., Suchanek, P.M., Klein, M., Tschop, J., Caldwell, C., Woods, S.C., Wittmann, G., Watanabe, M., Liposits, Z., Fekete, C., Reizes, O., Rohner-Jeanrenaud, F., Tschop, M.H., 2008. Peripheral, but not central, CB1 antagonism provides food intake-independent metabolic benefits in diet-induced obese rats. Diabetes 57, 2977-2991.
28. Ravinet Trillou, C., Delgorge, C., Menet, C., Arnone, M., Soubrie, P., 2004. CB1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity. Int. J. Obes. Relat. Metab. Disord. 28, 640-648.
29. Rinaldi-Carmona, M., Barth, F., Héaulme, M., Alonso, R., Shire, D., Congy, C., Soubrié, P., Brelière, J.C., Le Fur, G., 1995. Biochemical and pharmacological characterisation of SR141716A, the first potent and selective brain cannabinoid receptor antagonist. Life Sci. 56, 1941-1947.
30. Rosenbaum, M., Murphy, E.M., Heymsfield, S.B., Matthews, D.E., Leibel, R.L., 2002. Low dose leptin administration reverses effects of sustained weight-reduction on energy expenditure and circulating concentrations of thyroid hormones. J. Clin. Endocrinol. Metab. 87, 2391-2394.
31. Rosenbaum, M., Goldsmith, R., Bloomfield, D., Magnano, A., Weimer, L., Heymsfield, S., Gallagher, D., Mayer, L., Murphy, E., Leibel, R.L., 2005. Low-dose leptin reverses skeletal muscle, autonomic, and neuroendocrine adaptations to maintenance of reduced weight. J. Clin. Investig. 115, 3579-3586.
32. Roth, J.D., Roland, B.L., Cole, R.L., Trevaskis, J.L.,Weyer, C., Koda, J.E., Anderson, C.M., Parkes, D.G., Baron, A.D., 2008. Leptin responsiveness restored by amylin agonism in dietinduced obesity: evidence from nonclinical and clinical studies. Proc. Natl Acad. Sci. 105, 7257-7262.
33. Scallet, A.C., Olney, J.W., 1986. Components of hypothalamic obesity: bipiperidylmustard lesions add hyperphagia to monosodium glutamate-induced hyperinsulinemia. Brain Res. 374, 380-384. (Pubitemid 16077991)
34. Scheen, A.J., Finer, N., Hollander, P., Jensen, M.D., Van Gaal, L.F., 2006. Efficacy and tolerability of rimonabant in overweight or obese patients with type 2 diabetes: a randomised controlled study. Lancet 368, 1660-1672. (Pubitemid 46048528)
35. Shire, D., Calandra, B., Delpech, M., Dumont, X., Kaghad, M., Le Fur, G., Caput, D., Ferrara, P., 1996. structural features of the central cannabinoid CB1 receptor involved in the binding of the specific CB1 antagonist SR 141716A. J. Biol. Chem. 271, 6941-6946.
36. Spiegelman, B.M., Flier, J.S., 2001. Obesity and the regulation of energy balance. Cell 104, 531-543. (Pubitemid 32201948)
37. Sternson, S.M., Shepherd, G.M.G., Friedman, J.M., 2005. Topographic mapping of VMH arcuate nucleus microcircuits and their reorganization by fasting. Nat. Neurosci. 8, 1356-1363.
38. van den Top, M., Spanswick, D., 2006. Integration of metabolic stimuli in the hypothalamic arcuate nucleus. Prog. Brain Research. Elsevier 141-154.
39. Verty, A.N., Allen, A.M., Oldfield, B.J., 2009. The effects of rimonabant on brown adipose tissue in rat: implications for energy expenditure. Obesity 17, 254-261.
40. Vickers, S.P., Webster, L.J., Wyatt, A., Dourish, C.T., Kennett, G.A., 2003. Preferential effects of the cannabinoid CB1 receptor antagonist, SR141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats. Psychopharmacology 167, 103-111. (Pubitemid 36535298)
41. Wang, J.H., Wang, F., Yang, M.J., Yu, D.F., Wu, W.N., Liu, J., Ma, L.Q., Cai, F., Chen, J.G., 2008. Leptin regulated calcium channels of neuropeptide Y and proopiomelanocortin neurons by activation of different signal pathways. Neuroscience 156, 89-98.
42. Widdowson, P.S., Upton, R., Buckingham, R., Arch, J., Williams, G., 1997. Inhibition of food response to intracerebroventricular injection of leptin is attenuated in rats with diet-induced obesity. Diabetes 46, 1782-1785. (Pubitemid 27456411)
43. Xue, B., Kahn, B.B., 2006. AMPK integrates nutrient and hormonal signals to regulate food intake and energy balance through effects in the hypothalamus and peripheral tissues. J. Physiol. 574, 73-83. (Pubitemid 43905798)