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Summary
Novelty: Novel carbazole compounds are disclosed as α-receptor antagonists. They have specific and strong affinity for the σ-receptor without extrapyramidal tract injury and are potentially useful for the treatment of psychotic disorders.
Biology: Two tests are described: a receptor binding assay in male Wistar rats (IC50 values are significantly lower than rimcazole in vitro) and a methaphetamine-induced hyperlocomotion test in six groups of five male ICR mice (three compounds show inhibition).
Chemistry: The preferred compound is 5,8 -dimethyl-4-(2 -di-n-propylaminoethyl) carbazole hydrochloride. Preparative methods are given for six compounds and their intermediates. Eighteen compounds are mentioned altogether and characterization is by mp.
Structure: