Sibutramine : a review of the pharmacology of a novel anti-obesity agent

摘要: Sibutramine is a noradrenaline and 5-hydroxytryptamine reuptake inhibitor which causes weight loss in laboratory rodents via effects on both food intake metabolic rate. Sibutramine's are predominantly mediated by two pharmacologically-active metabolites (its primary secondary amines). its active do not cause the release of monoamine neurotransmitters have affinity for their receptors. dose-dependently inhibits 24 h rats enhancing natural physiological process satiety. also stimulates thermogenesis rats, producing sustained (> 6 h) increases oxygen consumption up to 30%. The thermogenic effect sibutramine results from central activation efferent sympathetic activity which, turn, involves beta 3-adrenoceptors. Sympathetic stimulation brown adipose tissue 3-adrenoceptors thought be large, 18 fold increase glucose utilization induced sibutramine. These dual explain anti-obesity animals.