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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders.

Abstract：

:Parkinson's Disease (PD) and Extrapyramidal Syndrome (EPS) are movement disorders that result from degeneration of the dopaminergic input to the striatum and chronic inhibition of striatal dopamine D(2) receptors by antipsychotics, respectively. Adenosine A(2A) receptors are selectively localized in the basal ganglia, primarily in the striatopallidal ("indirect") pathway, where they appear to operate in concert with D(2) receptors and have been suggested to drive striatopallidal output balance. In cases of dopaminergic hypofunction, A(2A) receptor activation contributes to the overdrive of the indirect pathway. A(2A) receptor antagonists, therefore, have the potential to restore this inhibitor imbalance. Consequently, A(2A) receptor antagonists have therapeutic potential in diseases of dopaminergic hypofunction such as PD and EPS. Targeting the A(2A) receptor may also be a way to avoid the issues associated with direct dopamine agonists. Recently, preladenant was identified as a potent and highly selective A(2A) receptor antagonist, and has produced a significant improvement in motor function in rodent models of PD. Here we investigate the effects of preladenant in two primate movement disorder models. In MPTP-treated cynomolgus monkeys, preladenant (1 or 3 mg/kg; PO) improved motor ability and did not evoke any dopaminergic-mediated dyskinetic or motor complications. In Cebus apella monkeys with a history of chronic haloperidol treatment, preladenant (0.3-3.0 mg/kg; PO) delayed the onset of EPS symptoms evoked by an acute haloperidol challenge. Collectively, these data support the use of preladenant for the treatment of PD and antipsychotic-induced movement disorders.

journal_name

Exp Neurol

journal_title

Experimental neurology

authors

Hodgson RA,Bedard PJ,Varty GB,Kazdoba TM,Di Paolo T,Grzelak ME,Pond AJ,Hadjtahar A,Belanger N,Gregoire L,Dare A,Neustadt BR,Stamford AW,Hunter JC

doi

10.1016/j.expneurol.2010.07.011

subject

Has Abstract

pub_date

2010-10-01 00:00:00

pages

384-90

issue

2

eissn

0014-4886

issn

1090-2430

pii

S0014-4886(10)00249-9

journal_volume

225

pub_type

杂志文章

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