The novel 5-HT1A receptor agonist, NLX-112 reduces l-DOPA-induced abnormal involuntary movements in rat: A chronic administration study with microdialysis measurements
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- 作者：Andrew C. McCreary1 ; amccrear@its.jnj.com" class="auth_mail" title="E-mail the corresponding author ; Mark A. Varney ; Adrian Newman-Tancredi ; anewmantancredi@neurolixis.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：NLX-112 ; Befiradol ; Parkinson's disease ; l-DOPA-Induced dyskinesia ; 5-HT1A receptor ; 5-HT1A agonist
- 刊名：Neuropharmacology
- 出版年：2016
- 出版时间：June 2016
- 年：2016
- 卷：105
- 期：Complete
- 页码：651-660
- 全文大小：689 K
文摘
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NLX-112 is a selective 5-HT1A receptor agonist which eliminates L-DOPA-induced Abnormal Involuntary Movements in Parkinsonian rats.
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The potent anti-AIMs activity of NLX-112 (0.16 mg/kg i.p.) is maintained over a once-daily 2-week dosing period.
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NLX-112 did not prevent the 'priming' process that causes rats to express AIMs in response to repeated dosing of L-DOPA.
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NLX-112 maintained a robust inhibition of striatal serotonin release and blunting of L-DOPA-induced increases in dopamine levels.
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NLX-112 did not modify striatal glutamate release but reversed L-DOPA-induced increases in striatal GABA release.