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Synthesis and Pharmacological Evaluation of Novel 9- and 10- Substituted Cytisine Derivatives - Nicotinic Ligands of Enhanced Subtype Selectivity

机译：新型9和10-取代的胱氨酸衍生物-增强亚型选择性的烟碱配体的合成和药理评价

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We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the α4β2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.

机译：我们报告了几种半胱氨酸衍生物的合成和药理特性。其中，在结合试验中，两个10-取代的衍生物对α4β2nAChR亚型的选择性比对胱氨酸的选择性高得多。发现9-乙烯基衍生物具有与胱氨酸非常相似的激动剂活性曲线。

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期刊名称 other
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Sheela K. Chellappan; Yingxian Xiao; Werner Tueckmantel; Kenneth J. Kellar; Alan P. Kozikowski;
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年(卷),期 -1(49),9
年度 -1
页码 2673–2676
总页数 15
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1. Synthesis and pharmacological evaluation of novel 9-and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity [J] . Chellappan SK, Xiao YX, Tueckmantel W, Journal of Medicinal Chemistry . 2006,第9期

机译：新型9-和10-取代的胱氨酸衍生物的合成和药理评价。增强亚型选择性的烟碱配体
2. Synthesis, Binding, and Modeling Studies of New Cytisine Derivatives, as Ligands for Neuronal Nicotinic Acetylcholine Receptor Subtypes [J] . Tasso B, Boido CC, Terranova E, Journal of Medicinal Chemistry . 2009,第14期

机译：作为神经元烟碱乙酰胆碱受体亚型的配体的新型胱氨酸衍生物的合成，结合和模型研究
3. Molecular basis of the selective binding of MDMA enantiomers to the alpha4beta2 nicotinic receptor subtype: Synthesis, pharmacological evaluation and mechanistic studies [J] . Salome Llabres, Sara Garcia-Rates, Edgar Cristobal-Lecina, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2014,第Null期

机译：MDMA对映异构体与α4beta2烟碱型受体亚型选择性结合的分子基础：合成，药理学评估和机理研究
4. Design, Synthesis, and Pharmacological Evaluation of Novel Tasiamide B Derivatives: Selective Inhibitors of BACE1 [C] . Jian Liu, SimingYang, Wei Zhang, Chinese International Peptide Symposium . 2013

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7. Synthesis and Pharmacological Evaluation of Novel 9- and 10-Substituted Cytisine Derivatives. Nicotinic Ligands of Enhanced Subtype Selectivity [O] . Sheela K. Chellappan, Yingxian Xiao, Werner Tueckmantel, 2006

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8. Equilibrium model for ligand-modified micellar-enhanced ultrafiltration, selective separation of metal ions using iminoacetic substituted polyamines and a theoretical model for the titration behavior of polyamines [R] . Dharmawardana, U. R. 1992

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Synthesis and Pharmacological Evaluation of Novel 9- and 10- Substituted Cytisine Derivatives - Nicotinic Ligands of Enhanced Subtype Selectivity

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