Central dopamine agonist activity on the 8-alpha-amino-ergoline CU 32-085.

Abstract:

:The effects of the 8-alpha-amino-ergoline CU 32-085 on central dopamine neuronal systems was investigated. Two h after administration of CU 32-085 a slight increase of dopamine levels was observed in the nucleus caudatus-putamen. Radioligand binding studies in vitro have shown that CU 32-085 has a low affinity for striatal dopamine receptors labeled by [3H]n-propylapomorphine or [3H]spiroperidol. However, CU 32-085 effectively displaces in vivo [3H]n-propylapomorphine and [3H]spiroperidol from their respective binding sites in the mouse striatum. Functional studies have shown that CU 32-085 elicits contralateral rotation in rats with unilateral 6-OH-dopamine induced lesions of the meso-striatal dopamine neurons, and ipsilateral rotation in rats with unilateral intrastriatal ibotenic acid lesions. CU 32-085 relieves tremor in monkeys with ventromedial tegmental lesions and produces only slight abnormal involuntary movements. The biochemical and functional studies suggest that CU 32-085 and/or its metabolite exerts central dopamine agonist activity in vivo. Studies in monkeys with ventromedial tegmental lesions suggest that CU 32-085 might be an effective antiparkinsonian agent which produces less dyskinesias than the other tested dopamine agonists.

journal_name

Brain Res

journal_title

Brain research

authors

Fuxe K,Agnati L,Mascagni F,Kuga S,Helmer-Matyjek E,Goldstein M

doi

10.1016/0006-8993(85)91044-3

subject

Has Abstract

pub_date

1985-03-04 00:00:00

pages

325-32

issue

2

eissn

0006-8993

issn

1872-6240

pii

0006-8993(85)91044-3

journal_volume

328

pub_type

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