西布曲明:抗肥胖药物。药理的审查证据d-amphetamine和d-fenfluramine区分开来。

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治愈DJ, Aspley年代,船首先生,杰克逊HC,马丁•KF Cheetham SC

西布曲明:抗肥胖药物。药理的审查证据d-amphetamine和d-fenfluramine区分开来。

Int J ob过热金属底座Disord。1998年8月,22增刊1:S18-28;S29讨论。

PubMed ID
9758240 (在PubMed
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文摘

西布曲明(BTS 54 524;N - (1 - (1 - (4-chlorophenyl)环丁基)3-methylbutyl) - N, N-dimethylamine盐酸盐一水)是一种新型5 -(5 -羟色胺)和去甲肾上腺素再摄取抑制剂抗肥胖药物(去甲肾上腺素重摄取抑制剂)。西布曲明减少食物摄入量的啮齿动物和这一效应是由预处理部分或完全逆转5或去甲肾上腺素拮抗剂,表明神经递质参与西布曲明的hypophagic效果。此外,氟西汀和nisoxetine,选择性5 -和去甲肾上腺素再摄取抑制剂,分别对食物摄入量没有影响时,但他们深刻地抑制食物摄取时结合(相当于SNRI的行动,西布曲明),展示了一个协同交互的控制这两个类的摄食行为。西布曲明减少食物摄入量提高post-ingestive饱腹感的生理反应。减少食物摄入量是CNS-mediated效应引起的,因为它是intracerebroventricular注射西布曲明的强有力地活跃的二级和一级胺代谢物(BTS BTS 54 354和54 505)。西布曲明增加能量消耗(生热作用)的老鼠。再一次,而氟西汀和nisoxetine没有产热的效果时,这两个选择性单胺再摄取抑制剂的结合深刻的提高生热作用,展示5和去甲肾上腺素神经传递的协同交互能量消耗的监管。Sibutramine-induced生热作用是由政府废除无选择性高剂量阿替洛尔或ICI 118551块beta3-adrenoceptors除了beta1 beta2-adrenoceptors,但不是由低剂量阿替洛尔或ICI 118551块beta1 beta2-adrenoceptors,分别。葡萄糖利用率研究证明sibutramine-induced生热作用是通过选择性介导交感神经激活棕色脂肪组织,这是一个集中介导的效果,因为它是通过预处理动物神经节阻滞剂,chlorisondamine。 The SNRI mode of action of sibutramine is clearly differentiated from those of the two major classes of anti-obesity drugs, viz, the 5-HT releasing agents, for example, fenfluramine and dexfenfluramine, and the noradrenaline + dopamine-releasing agents, for example, dexamphetamine. In the case of the 5-HT-releasing agents, this mechanism has been linked in animal studies to profound and prolonged depletion and dysfunction of CNS 5-HT neurons. With noradrenaline + dopamine-releasing agents, it is the enhancement of central dopaminergic function which is believed to be responsible for their stimulant, rewarding and reinforcing properties and it is their releasing mechanism which makes them such powerful psychostimulant drugs of abuse. By utilizing noradrenaline and 5-HT for its anti-obesity effects, sibutramine is differentiated from other weight-reducing drugs which act through either 5-HT alone or noradrenaline + dopamine. In addition, sibutramine is further differentiated because it enhances monoamine function by reuptake inhibition, rather than by monoamine release.

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药物