-
1.发明授权Use of .alpha.-conotoxin MII to treat disorders resulting from nicotine-stimulated dopamine release 失效使用α-毒素MII来治疗由尼古丁刺激的多巴胺释放引起的疾病
公开(公告)号：US5929034A
公开(公告)日：1999-07-27
申请号：US45926
申请日：1998-03-23
CPC分类号： A61K38/1767 , Y10S514/813
摘要： Neuronal nicotinic acetylcholine receptors (nAChRs) are believed to mediate nicotine addiction. In addition, stimulation of nAChRs modulates release of neurotransmitters including dopamine, norepinephrine and serotonin. Thus, pharmacological manipulation of nicotinic receptors has implications for a wide variety of disorders including psychotic, mood, movement and cognitive. For most nAChRs, there are no subtype selective ligands. However, .alpha.-conotoxin MII, a small peptide from the carnivorous marine snail Conus magus, was recently isolated. This peptide has been shown to be a specific antagonist for .alpha.3.beta.2 nicotinic receptors. The peptide potently blocks part, but not all, of nicotine-stimulated dopamine release from rat brain striatal synaptosomes. In contrast it has no effect on potassium stimulated dopamine release. Other .alpha.-conotoxins specifically target distinct neuronal nAChR subtypes. .alpha.-Conotoxins thus represent new lead compounds for CNS disorders.
摘要翻译： 神经元烟碱乙酰胆碱受体（nAChRs）被认为是介导尼古丁成瘾。 此外，nAChRs的刺激调节神经递质的释放，包括多巴胺，去甲肾上腺素和5-羟色胺。 因此，烟碱受体的药理学操作对各种各样的疾病，包括精神病，情绪，运动和认知有影响。 对于大多数nAChR，没有亚型选择性配体。 然而，α-毒素MII，一种来自肉食海洋蜗牛Conus magus的小肽，最近被隔离。 已经显示该肽是α3β2烟碱受体的特异性拮抗剂。 该肽有力地阻止了大鼠脑纹状体突触体中尼古丁刺激的多巴胺释放的部分，但并非全部。 相反，它对钾刺激的多巴胺释放没有影响。 其他α-酮毒素特异性靶向不同的神经元nAChR亚型。 因此，α-核酸毒素代表CNS疾病的新型铅化合物。
-
2.发明授权Use of .alpha.-conotoxin MII to treat disorders resulting from nicotine stimulated dopamine release 失效使用α-毒素MII治疗由尼古丁刺激的多巴胺释放引起的疾病
公开(公告)号：US5780433A
公开(公告)日：1998-07-14
申请号：US761674
申请日：1996-12-06
CPC分类号： A61K38/1767 , Y10S514/813
摘要： Neuronal nicotinic acetylcholine receptors (nAChRs) are believed to mediate nicotine addiction. In addition, stimulation of nAChRs modulates release of neurotransmitters including dopamine, norepinephrine and serotonin. Thus, pharmacological manipulation of nicotinic receptors has implications for a wide variety of disorders including psychotic, mood, movement and cognitive. For most nAChRs, there are no subtype selective ligands. However, .alpha.-conotoxin MII, a small peptide from the carnivorous marine snail Conus magus, was recently isolated. This peptide has been shown to be a specific antagonist for .alpha.3.beta.2 nicotinic receptors. The peptide potently blocks part, but not all, of nicotine-stimulated dopamine release from rat brain striatal synaptosomes. In contrast it has no effect on potassium stimulated dopamine release. Other .alpha.-conotoxins specifically target distinct neuronal nAChR subtypes. .alpha.-Conotoxins thus represent new lead compounds for CNS disorders.
摘要翻译： 神经元烟碱乙酰胆碱受体（nAChRs）被认为是介导尼古丁成瘾。 此外，nAChRs的刺激调节神经递质的释放，包括多巴胺，去甲肾上腺素和5-羟色胺。 因此，烟碱受体的药理学操作对各种各样的疾病，包括精神病，情绪，运动和认知有影响。 对于大多数nAChR，没有亚型选择性配体。 然而，α-毒素MII，一种来自肉食海洋蜗牛Conus magus的小肽，最近被隔离。 已经显示该肽是α3β2烟碱受体的特异性拮抗剂。 该肽有力地阻止了大鼠脑纹状体突触体中尼古丁刺激的多巴胺释放的部分，但并非全部。 相反，它对钾刺激的多巴胺释放没有影响。 其他α-酮毒素特异性靶向不同的神经元nAChR亚型。 因此，α-核酸毒素代表CNS疾病的新型铅化合物。
-
3.发明授权
公开(公告)号：US5922679A
公开(公告)日：1999-07-13
申请号：US45925
申请日：1998-03-23
CPC分类号： A61K38/1767 , Y10S514/813
摘要： Neuronal nicotinic acetylcholine receptors (nAChRs) are believed to mediate nicotine addiction. In addition, stimulation of nAChRs modulates release of neurotransmitters including dopamine, norepinephrine and serotonin. Thus, pharmacological manipulation of nicotinic receptors has implications for a wide variety of disorders including psychotic, mood, movement and cognitive. For most nAChRs, there are no subtype selective ligands. However, .alpha.-conotoxin MII, a small peptide from the carnivorous marine snail Conus magus, was recently isolated. This peptide has been shown to be a specific antagonist for .alpha.3.beta.2 nicotinic receptors. The peptide potently blocks part, but not all, of nicotine-stimulated dopamine release from rat brain striatal synaptosomes. In contrast it has no effect on potassium stimulated dopamine release. Other .alpha.-conotoxins specifically target distinct neuronal nAChR subtypes. .alpha.-Conotoxins thus represent new lead compounds for CNS disorders.
-
-
搜索结果
3 条记录 (耗时 0.017 秒)