Bartyzel P, Misztal S, Tatarczyńska E, Chojnacka-Wójcik E
Institute of Pharmacology, Polish Academy of Sciences, Kraków.
Pol J Pharmacol Pharm. 1989 Sep-Oct;41(5):495-504.
A series of aminoalkylderivatives of 1,2,3,4-tetrahydro-beta-carboline-1-spiro-4'-N'-benzylpiperidine were synthesized by means of chloroacetylation of the title compound and substitution of chlorine atom with various heterocyclic amines in DMSO, followed by LAH reduction of the carbonyl group. Of the ten tested compounds (4a-4e, 5a-5e), compound 5d given ip, but not orally, showed an anxiolytic activity in the four-plate test in mice and in the conflict test in rats. Compound 5d is devoid of an anticonvulsant or neurotoxic action. The activity of compound 5d resembles this of buspirone.
通过对标题化合物进行氯乙酰化反应，并在二甲基亚砜中用各种杂环胺取代氯原子，随后用氢化铝锂还原羰基，合成了一系列1,2,3,4-四氢-β-咔啉-1-螺-4'-N'-苄基哌啶的氨基烷基衍生物。在十种测试化合物（4a - 4e，5a - 5e）中，腹腔注射而非口服给予的化合物5d在小鼠的四板试验和大鼠的冲突试验中显示出抗焦虑活性。化合物5d没有抗惊厥或神经毒性作用。化合物5d的活性与丁螺环酮相似。
