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近期,诺华公司宣称中止其“未来的拳头产品”——抗严重抑郁症药agomelatine(AGO178)的进一步的开发计划。Agomelatine具5-HT2c受体拮抗剂和褪黑激素受体激动剂双重活性,即可通过抑制5-HT2c受体,促进中枢神经系统中多巴胺和去甲肾上腺素的释放,并激活大脑皮质额叶区多巴胺能和肾上腺素能通路,且能有效激动褪黑激素受体MT1和MT2。该产品目前已在欧盟以商品名Valdoxan获准上市,成为首个褪黑激素能抗抑郁症药物,并有望于2013年在美国获准上市。
Recently, Novartis announced that it has suspended its “Future Fist Product” - a further development plan for the antidepressant agomelatine (AGO178). Agomelatine dual 5-HT2c receptor antagonist and melatonin receptor agonist dual activity, which can be through the inhibition of 5-HT2c receptor, promote central nervous system dopamine and norepinephrine release, and activate the frontal cortex District dopamine and adrenergic pathways, and can effectively stimulate melatonin receptors MT1 and MT2. The product is currently licensed in the European Union under the Valdoxan brand name, becoming the first melatonin-antidepressant and is expected to be approved in the United States in 2013.