d-フェンフルラミン·塩酸塩 化学特性,用途語,生産方法
効能
食欲抑制薬 (全身性), セロトニン再取り込み阻害薬
説明
Redux, having been already launched in Europe, was marketed in Canada
and the US for obesity. The (+)-isomer of fenfluramine is obtained by resolution using
d-camphoric acid and ultimate conversion to the HCl salt. The levo-isomer has
significant effects on dopaminerigic neurotransmission, while the dextro-isomer has a
greater anorectic effect because it is more selective on serotonin as a 5-HT agonist
with no dopaminergic or noradenergic activity. Redux inhibits the presynaptic release
of serotonin, is a reuptake inhibitor, a 5-HT
1B, receptor agonist, and a postsynaptic 5-HT
2C receptor agonist . A dietary reduction in fat intake was thought to proceed via a
CCK A-type receptor agonist activity. Due to the side effects of primary pulmonary
hypertension, brain serotonin neurotoxicity and valvular heart disease, Redux was
withdrawn world wide.
化学的特性
White Crystalline Powder
使用
Controlled substance. Anorexic
定義
ChEBI: The hydrochloride salt of (S)-fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike the racemate it does not possess catecholamine agonist activity. It was formerly given by mouth in the tre
tment of obesity, but, like the racemate, was withdrawn wolrdwide following reports of valvular heart defects.
生物活性
Indirectly agonizes serotonin receptors via inhibition of 5-HT re-uptake and stimulation of 5-HT release. Anorectic agent; decreases growth hormone, insulin, leptin, fat mass, lean mass and increases ghrelin in diet-switched diet-induced obese mice.
d-フェンフルラミン·塩酸塩 上流と下流の製品情報
原材料
準備製品