ArticleBritish journal of pharmacology1999
Thermogenic effects of sibutramine and its metabolites.
Article in British journal of pharmacology, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers, 1 of them a synthesis that pooled it.
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Who cites it
28 citing papers in PubMed, 1 synthesis or guideline pooled it, 140 citations in OpenAlex.
- Interventions associated with brown adipose tissue activation and the impact on energy expenditure and weight loss: A systematic review.Frontiers in endocrinology · 2022Pooled it
- Role of Brown Adipose Tissue in Metabolic Health and Efficacy of Drug Treatment for Obesity.Journal of clinical medicine · 2024Article
- Cardiogenic shock in a 28-year-old woman associated with sibutramine use.International journal of legal medicine · 2024Article
- Assessment of redox state and biochemical parameters of salivary glands in rats treated with anti-obesity drug sibutramine hydrochloride.Clinical oral investigations · 2022Article
- Article
- Role of serotonin in body weight, insulin secretion and glycaemic control.Journal of neuroendocrinology · 2021Review
- Idalopirdine - a small molecule antagonist of 5-HT6 with therapeutic potential against obesity.Metabolic brain disease · 2015Article
- Fluoxetine induces lean phenotype in rat by increasing the brown/white adipose tissue ratio and UCP1 expression.Journal of bioenergetics and biomembranes · 2015Article
- Central serotonergic neurons activate and recruit thermogenic brown and beige fat and regulate glucose and lipid homeostasis.Cell metabolism · 2015Article
- Central nervous system regulation of brown adipose tissue.Comprehensive Physiology · 2014Review
- Phentermine, sibutramine and affective disorders.Clinical psychopharmacology and neuroscience : the official scientific journal of the Korean College of Neuropsychopharmacology · 2013Article
- Detection of thermogenesis in rodents in response to anti-obesity drugs and genetic modification.Frontiers in physiology · 2013Article
- Neuropsychiatric adverse effects of centrally acting antiobesity drugs.CNS neuroscience & therapeutics · 2011Review
- The utility of animal models to evaluate novel anti-obesity agents.British journal of pharmacology · 2011Review
- The use of serotonergic drugs to treat obesity--is there any hope?Drug design, development and therapy · 2011Review
- Assessment of acute and chronic pharmacological effects on energy expenditure and macronutrient oxidation in humans: responses to ephedrine.Journal of obesity · 2011Article
- Pharmacotherapies for obesity: past, current, and future therapies.Journal of obesity · 2011Article
- Combinations of drugs in the Treatment of Obesity.Pharmaceuticals (Basel, Switzerland) · 2010Review
- 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 : official publication of the American College of Neuropsychopharmacology · 2010Article
- Efficacy and tolerability of the association of sibutramine and orlistat for six months in overweight and obese patients.Journal of obesity · 2010Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The thermogenic activity of the serotonin and noradrenaline reuptake inhibitor sibutramine (BTS 54524; Reductil) was investigated by measuring oxygen consumption (VO2) in rats treated with sibutramine or its two pharmacologically-active metabolites. 2. Sibutramine caused a dose-dependent rise in VO2, with a dose of 10 mg kg(-1) of sibutramine or its metabolites producing increases of up to 30% that were sustained for at least 6 h, and accompanied by significant increases (0.5-1.0 degrees C) in body temperature. 3. Based on the accumulation in vivo of radiolabelled 2-deoxy-[3H]-glucose, sibutramine had little or no effect on glucose utilization in most tissues, but caused an 18 fold increase in brown adipose tissue (BAT). 4. Combined high, non-selective doses (20 mg kg(-1)) of the beta-adrenoceptor antagonists, atenolol and ICI 118551, inhibited completely the VO2 response to sibutramine, but the response was unaffected by low, beta1-adrenoceptor-selective (atenolol) or beta2-adrenoceptor-selective (ICI 118551) doses (1 mg kg(-1)). 5. The ganglionic blocking agent, chlorisondamine (15 mg kg(-1)), inhibited completely the VO2 response to the metabolites of sibutramine, but had no effect on the thermogenic response to the beta3-adrenoceptor-selective agonist BRL 35135. 6. Similar thermogenic responses were produced by simultaneous injection of nisoxetine and fluoxetine at doses (30 mg kg(-1)) that had no effect on VO2 when injected individually. 7. It is concluded that stimulation of thermogenesis by sibutramine requires central reuptake inhibition of both serotonin and noradrenaline, resulting in increased efferent sympathetic activation of BAT thermogenesis via beta3-adrenoceptor, and that this contributes to the compound's activity as an anti-obesity agent.
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