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Evaluation of ciladopa hydrochloride as a potential anti-Parkinson drug.

Abstract：

:The effects of the putative dopamine agonist, ciladopa hydrochloride (AY 27,110) a non-ergot compound, were investigated in animal models of dopaminergic activity to evaluate its possible role in the treatment of Parkinson's disease. Ciladopa induced stereotyped behavior in both rats and guinea pigs. Unlike apomorphine, however, ciladopa did not produce a maximum behavioral response, i.e. stereotyped gnawing. Pretreatment with haloperidol and sulpiride blocked the effects induced by ciladopa. Pretreatment with reserpine and alpha-methyl-p-tyrosine did not alter the behavioral effects of ciladopa. Ciladopa caused contralateral rotation in rats with unilateral lesions of the substantia nigra induced by 6-hydroxydopamine. Ciladopa induced vomiting in dogs. Small doses of ciladopa decreased locomotor activity in rats, an effect presumably mediated by presynaptic autoreceptors. The chronic injection of both subthreshold and suprathreshold doses of ciladopa failed to induce behavioral supersensitivity. Ciladopa binds to D-2 dopamine receptors in the mammalian caudate nucleus. These data indicate that ciladopa can cause stimulation of central dopaminergic receptors and that the drug is a partial dopamine agonist with direct-acting properties. Ciladopa differs from other available dopaminergic drugs and may possess therapeutic advantages for the treatment of Parkinson's disease.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Koller WC,Fields JZ,Gordon JH,Perlow MJ

doi

10.1016/0028-3908(86)90190-5

subject

Has Abstract

pub_date

1986-09-01 00:00:00

pages

973-9

issue

9

eissn

0028-3908

issn

1873-7064

journal_volume

25

pub_type

杂志文章

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