SYNTHESIS AND DOPAMINERGIC ACTIVITY OF 3-(3,4-DIHYDROXYPHENYL)-1-N-PROPYLPYRROLIDINE HYDROBROMIDE

被引:15
作者
CRIDER, AM
HEMDI, TF
HASSAN, MN
FAHN, S
机构
[1] UNIV TOLEDO, COLL PHARM, TOLEDO, OH 43606 USA
[2] COLUMBIA UNIV COLL PHYS & SURG, DEPT NEUROL, NEW YORK, NY 10032 USA
关键词
D O I
10.1002/jps.2600731125
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
3-(3,4-Dihydroxyphenyl)-1-n-propylpyrrolidine hydrobromide was synthesized by a 6-step reaction sequence and was evaluated, and compared with apomorphine, for central dopaminergic agonist activity. The compound produced behavioral and biochemical changes characteristic of central dopaminergic stimulation. Administration of 3-(3,4-dihydroxyphenyl)-1-n-propylpyrrolidine hydrobromide to rats resulted in the reversal of the reserpine syndrome, stereotypic behavior, contralateral turning following 6-hydroxydopamine lesion of the substantia nigra, a decrease in dopamine turnover and inhibition of prolactin release. Evidently, 3-(3,4-dihydroxyphenyl)-1-n-propylpyrrolidine hydrobromide is a dopaminergic agonist. The compound exhibited a lower potency but a slightly longer duration of action than apomorphine.
引用
收藏
页码:1585 / 1587
页数:3
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