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2. 发明授权

US06207699B1 Pharmaceutical combinations for treating obesity and food craving 失效
标题翻译：用于治疗肥胖和食物渴望的药物组合
公开(公告)号：US06207699B1
公开(公告)日：2001-03-27
申请号：US09335841
申请日：1999-06-18
申请人： Richard Brian Rothman
发明人： Richard Brian Rothman
IPC分类号： A61K3140
CPC分类号： A61K45/06 , A61K31/195 , A61K31/31 , A61K31/40 , A61K2300/00
摘要： Numerous studies have documented that medications which increase brain serotonin (5-HT) are effective anorectic agents which help obese patients lose weight and which also decrease craving for sweets and carbohydrates. Evidence from other studies also indicate that increases in brain 5-HT may help decrease craving for alcohol and cocaine. 5-hydroxy-L-tryptophan, abbreviated 5-HTP, is the immediate precursor of serotonin (5-HT). When administered in combination with an inhibitor of peripheral decarboxylase such as carbidopa, 5-HTP increases brain serotonin. Increases in synaptic 5-HT decreases the firing rate of 5-HT neurons via stimulation of inhibitory 5-HT1a receptors located on the cell bodies in the raphe. This serves as a negative feedback loop. The clinically available beta adreneric receptor antagonist medication pindolol is also a 5-HT1a antagonist, and can be used to increase the ability of 5-HTP to increase brain 5-HT. Previous studies with 5-HTP used doses exceeding 50 mg per day. When 5-HTP was used in combination with carbidopa, the dose of carbidopa was in excess of 50 mg per day. One novel aspect of the invention are the doses of the 5-HTP and carbidopa: much lower daily doses than have been used before are effective in decreasing appetite, decreasing craving for food and for promoting weight loss. The second novel aspect of the invention relates to the concurrent use of pindolol along with the 5-HTP/Carbidopa, which enhances the effectiveness of the 5-HTP/Carbidopa combination.
摘要翻译：许多研究已经证明，增加脑5-羟色胺（5-HT）的药物是有效的厌食症药物，其帮助肥胖患者减肥，并且还减少对糖果和碳水化合物的渴望。来自其他研究的证据也表明，脑5-HT的增加可能有助于减少对酒精和可卡因的渴望。缩写为5-HTP的5-羟基-L-色氨酸是5-羟色胺（5-HT）的直接前体。当与卡比多巴等周边脱羧酶抑制剂组合使用时，5-HTP可增加脑血清素。突触5-HT的增加通过刺激位于鳞片上的细胞体上的抑制性5-HT1a受体来降低5-HT神经元的放电速率。这用作负反馈回路。临床上可用的β-肾上腺素受体拮抗剂药物吲哚洛尔也是5-HT1a拮抗剂，可用于增加5-HTP增加脑5-HT的能力。以前的研究，5-HTP使用剂量超过每天50毫克。当5-HTP与卡比多巴组合使用时，卡比多巴的剂量每天超过50毫克。本发明的一个新颖方面是5-HTP和卡比多巴的剂量：比以前使用的日剂量低得多，有效降低食欲，减少对食物的渴望和促进体重减轻。本发明的第二个新颖方面涉及同时使用吲哚洛尔与5-HTP /卡比多巴，其提高了5-HTP /卡比多巴组合的有效性。

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