Anti-hypertensive treatment preserves appetite suppression while preventing cardiovascular adverse effects of tesofensine in rats

Obesity

Volumn 21, Issue 5, 2013, Pages 985-992

  Bentzen, Bo Hjorth ^a   Grunnet, Morten ^a   Hyveled Nielsen, Lars ^a   Sundgreen, Claus ^a   Lassen, Jørgen Buus ^a   Hansen, Henrik H ^a,b  

^a NEUROSEARCH A S   (Denmark)

^b Gubra   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

METOPROLOL; TELMISARTAN; TESOFENSINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANOREXIGENIC ACTIVITY; ANTIHYPERTENSIVE THERAPY; ARTICLE; BLOOD PRESSURE; CARDIOTOXICITY; CONTROLLED STUDY; DOPAMINERGIC SYSTEM; DRUG ACTIVITY; FOOD INTAKE; HEART RATE; HYPOPHAGIA; INTRINSIC SYMPATHOMIMETIC ACTIVITY; MALE; NERVE STIMULATION; NEUROTRANSMISSION; NONHUMAN; NORADRENERGIC SYSTEM; OBESITY; RAT; TELEMETRY;

ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS; ANIMALS; ANTI-OBESITY AGENTS; ANTIHYPERTENSIVE AGENTS; APPETITE; APPETITE DEPRESSANTS; BENZIMIDAZOLES; BENZOATES; BICYCLO COMPOUNDS, HETEROCYCLIC; BLOOD PRESSURE; CARDIOVASCULAR DISEASES; DOSE-RESPONSE RELATIONSHIP, DRUG; ENERGY INTAKE; FEEDING BEHAVIOR; HEART RATE; MALE; METOPROLOL; OBESITY; RATS, SPRAGUE-DAWLEY; SYMPATHOMIMETICS;

RATTUS;

EID: 84879326963     PISSN: 19307381     EISSN: 1930739X     Source Type: Journal    
DOI: 10.1002/oby.20122     Document Type: Article

References (31)

1. Lehr T, Staab A, Tillmann C, et al. Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach. Br J Pharmacol 2008; 153: 164-174.
2. Astrup A, Madsbad S, Breum L, Jensen TJ, Kroustrup JP, Larsen TM,. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008; 372: 1906-1913.
3. Bray GA, Ryan DH,. Drug treatment of the overweight patient. Gastroenterology 2007; 132: 2239-2252.
4. Gilbert JA, Gasteyger C, Raben A, Meier DH, Astrup A, Sjödin A,. The effect of tesofensine on appetite sensations. Obesity (Silver Spring) 2012; 20: 553 -561.
5. Sjödin A, Gasteyger C, Nielsen AL, et al. The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men. Int J Obes (Lond) 2010; 34: 1634-1643.
6. Hansen HH, Hansen G, Tang-Christensen M, et al. The novel triple monoamine reuptake inhibitor tesofensine induces sustained weight loss and improves glycemic control in the diet-induced obese rat: comparison to sibutramine and rimonabant. Eur J Pharmacol 2010; 636: 88-95.
7. Axel AMD, Mikkelsen JD, Hansen HH,. Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of alpha1 adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat. Neuropsychopharmacology 2010; 35: 1464-1476.
8. Doggrell SA,. Tesofensine-a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008; 372:1906-1913. Expert Opin Investig Drugs 2009; 18: 1043-1046.
9. Wienen W, Hauel N, Van Meel JC, Narr B, Ries U, Entzeroth M,. Pharmacological characterization of the novel nonpeptide angiotensin II receptor antagonist, BIBR 277. Br J Pharmacol 1993; 110: 245-252.
10. Hao K, Chen YC, Cao YG, Yu D, Liu XQ, Wang GJ,. Pharmacokinetic- pharmacodynamic modeling of telmisartan using an indirect response model in spontaneously hypertensive rats. Acta Pharmacol Sin 2007; 28: 738-743.
11. Belpaire FM, de Smet F, Vynckier LJ, et al. Effect of aging on the pharmcokinetics of atenolol, metoprolol and propranolol in the rat. J Pharmacol Exp Ther 1990; 254: 116-122.
12. Di Verniero CA, Silberman EA, Mayer MA, Opezzo JAW, Taira CA, Höcht C,. In vitro and in vivo pharmacodynamic properties of metoprolol in fructose-fed hypertensive rats. J Cardiovasc Pharmacol 2008; 51: 532-541.
13. Pasman WJ, Saris WH, Westerterp-Plantenga MS,. Predictors of weight maintenance. Obes Res 1999; 7: 43-50.
14. Drapeau V, King N, Hetherington M, Doucet E, Blundell J, Tremblay A,. Appetite sensations and satiety quotient: predictors of energy intake and weight loss. Appetite 2007; 48: 159-166.
15. Doucet E, Imbeault P, St-Pierre S, et al. Appetite after weight loss by energy restriction and a low-fat diet-exercise follow-up. Int J Obes Relat Metab Disord 2000; 24: 906-914.
16. Bello NT, Zahner MR,. Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity. Curr Opin Investig Drugs 2009; 10: 1105-1116.
17. Lehr T, Staab A, Tillmann C, et al. Population pharmacokinetic modelling of NS2330 (tesofensine) and its major metabolite in patients with Alzheimer's disease. Br J Clin Pharmacol 2007; 64: 36-48.
18. Reisine TD, Chesselet MF, Lubetzki C, Chéramy A, Glowinski J,. A role for striatal beta-adrenergic receptors in the regulation of dopamine release. Brain Res 1982; 241: 123-130.
19. Hernández-Hernández R, Sosa-Canache B, Velasco M, Armas-Hernández MJ, Armas-Padilla MC, Cammarata R,. Angiotensin II receptor antagonists role in arterial hypertension. J Hum Hypertens 2002; 16 (Suppl 1): S93-S99.
20. Lehr T, Staab A, Trommeshauser D, Schaefer HG, Kloft C,. Semi-mechanistic population pharmacokinetic drug-drug interaction modelling of a long half-life substrate and itraconazole. Clin Pharmacokinet 2010; 49: 53-66.
21. Stangier J, Schmid J, Türck D, et al. Absorption, metabolism, and excretion of intravenously and orally administered [14C]telmisartan in healthy volunteers. J Clin Pharmacol 2000; 40: 1312-1322.
22. Rau T, Heide R, Bergmann K, et al. Effect of the CYP2D6 genotype on metoprolol metabolism persists during long-term treatment. Pharmacogenetics 2002; 12: 465-472.
23. Jackson HC, Needham AM, Hutchins LJ, Mazurkiewicz SE, Heal DJ,. Comparison of the effects of sibutramine and other monoamine reuptake inhibitors on food intake in the rat. Br J Pharmacol 1997; 121: 1758-1762.
24. Connoley IP, Liu YL, Frost I, Reckless IP, Heal DJ, Stock MJ,. Thermogenic effects of sibutramine and its metabolites. Br J Pharmacol 1999; 126: 1487-1495.
25. James WPT, Caterson ID, Coutinho W, et al. Effect of sibutramine on cardiovascular outcomes in overweight and obese subjects. N Engl J Med 2010; 363: 905-917.
26. Scholze J, Grimm E, Herrmann D, Unger T, Kintscher U,. Optimal treatment of obesity-related hypertension: the hypertension-obesity-sibutramine (HOS) study. Circulation 2007; 115: 1991-1998.
27. Pischon T, Sharma AM,. Use of beta-blockers in obesity hypertension: potential role of weight gain. Obes Rev 2001; 2: 275-280.
28. Ersoz HO, Ukinc K, Baykan M, et al. Effect of low-dose metoprolol in combination with sibutramine therapy in normotensive obese patients: a randomized controlled study. Int J Obes Relat Metab Disord 2004; 28: 378-383.
29. Jackson HC, Bearham MC, Hutchins LJ, Mazurkiewicz SE, Needham AM, Heal DJ,. Investigation of the mechanisms underlying the hypophagic effects of the 5-HT and noradrenaline reuptake inhibitor, sibutramine, in the rat. Br J Pharmacol 1997; 121: 1613-1618.
30. Wellman PJ,. Norepinephrine and the control of food intake. Nutrition 2000; 16: 837-842.
31. Stice E, Spoor S, Bohon C, Small DM,. Relation between obesity and blunted striatal response to food is moderated by TaqIA A1 allele. Science 2008; 322: 449-452.