Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs

…, HA Navarro, P Abraham, SA Wolckenhauer…

文献索引：Ivy Carroll; Ma, Wei; Navarro, Hernan A.; Abraham, Philip; Wolckenhauer, Scott A.; Damaj; Martin, Billy R. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 2 p. 678 - 685

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被引用次数: 20

摘要

A series of methyllycaconitine (1a, MLA) analogs was synthesized where the (S)-2- methylsuccinimidobenzoyl group in MLA was replaced with a (R)-2-methyl, 2, 2-dimethyl-, 2, 3-dimethyl, 2-phenyl-, and 2-cyclohexylsuccinimidobenzoyl (1b–f) group. The analogs 1b–f were evaluated for their inhibition of [125I] iodo-MLA binding at rat brain α7 nicotinic acetylcholine receptors (nAChR). In order to determine selectivity, MLA and the analogs ...