LIGAND-BINDING AND PLATELET UPTAKE STUDIES OF LOXAPINE, AMOXAPINE AND THEIR 8-HYDROXYLATED DERIVATIVES
LIGAND-BINDING AND PLATELET UPTAKE STUDIES OF LOXAPINE, AMOXAPINE AND THEIR 8-HYDROXYLATED DERIVATIVES
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DOI：
10.1016/0165-0327(82)90041-6
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发表时间：
1982-01-01
影响因子：
6.6
通讯作者：
BURROWS, GD
中科院分区：
文献类型：
--
作者：
FULTON, A;NORMAN, T;BURROWS, GD
通过[~ 3 H]丙咪嗪与大鼠皮层膜的结合、[~ 3 H]螺哌隆与大鼠纹状体膜的结合以及对人血小板摄取5-羟色胺的抑制作用，研究了洛沙坦、阿莫沙坦及其8-羟基化衍生物。发现[3 H]丙咪嗪结合抑制剂的顺序如下：阿莫西林>羟阿莫西林>洛沙坦=羟阿莫西林;血小板5-羟色胺摄取抑制剂：羟阿莫西林>阿莫西林>羟洛沙坦>洛沙坦;[3 H]螺哌隆结合抑制剂：洛沙坦>阿莫西林>羟阿莫西林>羟洛沙坦。结合结果支持了洛沙坦和阿莫西林的抗精神病特性，这也表明代谢产物可能具有抗精神病活性。这4个化合物可能具有抗抑郁和抗精神病的双重作用。
Loxapine, amoxapine and their 8-hydroxylated derivatives were studied by means of [3H]imipramine binding to rat cortical membranes, [3H]spiperone binding to rat striatal membranes and the inhibition of serotonin uptake by human platelets. The following order of inhibitors of [3H]imipramine binding was found: amoxapine > hydroxyamoxapine > loxapine = hydroxyloxapine; inhibitors of platelet serotonin uptake: hydroxyamoxapine > amoxapine > hydroxyloxapine > loxapine; and inhibitors of [3H]spiperone binding: loxapine > amoxapine > hydroxyamoxapine > hydroxyloxapine. The antipsychotic properties of loxapine and amoxapine were supported by the binding results, which also indicated the probably antipsychotic activities of the metabolites. All 4 compounds may possess dual action of antidepressant effect as well as antipsychotic effects.