eltoprazine

07/01/2013 - "The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models. "
01/01/2019 - "The aims of this study were firstly to investigate oscillations in main BG input and output structures-the dorsolateral striatum (dStr) and substantia nigra pars reticulata (SNr), respectively- including the direction of oscillation information flow, and secondly to investigate the effects of 5-HT1A/B receptor agonism with eltoprazine on oscillatory activities and abnormal involuntary movements (AIMs) characteristic. "
10/01/2023 - "Eltoprazine has potential clinical application for dyskinesia."
10/01/2023 - "Eltoprazine intervention reduced gamma oscillations, theta-gamma PAC in the DLS, and coherence and PLVs in the gamma band to alleviate dyskinesia. "
11/01/2015 - "Eltoprazine attenuated the development and expression of dyskinesias, preserving motor coordination on the rotarod. "

04/01/2015 - "Eltoprazine has a favourable risk-benefit and pharmacokinetic profile in patients with Parkinson's disease. "
04/01/2015 - "Eltoprazine counteracts l-DOPA-induced dyskinesias in Parkinson's disease: a dose-finding study."
10/15/2017 - "Eltoprazine, a serotonergic (5-HT)1A/B receptor agonist, is a potential treatment for L-DOPA-induced dyskinesia (LID) in Parkinson's disease (PD) but notably compromises the anti-parkinsonian effects of L-DOPA, as seen in rodent and monkey models of PD. "
04/01/2015 - "Single oral treatment with placebo or eltoprazine, at 2.5, 5 and 7.5 mg, was tested in combination with a suprathreshold dose of L-DOPA (Sinemet®) in 22 patients with Parkinson's disease (16 male/six female; 66.6 ± 8.8 years old) with L-DOPA-induced dyskinesias. "
04/01/2016 - "The serotonin 5-HT1A/1B receptor agonist eltoprazine suppressed dyskinetic-like behavior in animal models of Parkinson's disease (PD) but simultaneously reduced levodopa (l-dopa)-induced motility. "

01/01/2021 - "The present findings suggest that combination of l-dopa with eltoprazine and preladenant may be promising therapeutic strategy for delaying the onset of dyskinesia, preserving l-dopa efficacy and reducing neuroinflammation markers in nigrostriatal system of 6-OHDA-lesioned rats."
01/01/2021 - "The present study investigated whether early subchronic pretreatment with the serotonin 5-HT1A/1B receptor agonist eltoprazine plus the adenosine A2A receptor antagonist preladenant counteracted l-dopa-induced abnormal involuntary movements (AIMs, index of dyskinesia), and neuroinflammation, in unilateral 6-hydroxydopamine(6-OHDA)-lesioned rat model of PD. "

01/01/2017 - "Regarding adverse effects, eltoprazine was found to produce hypothermia starting from 1 mg/kg. At s imilar doses it also increased locomotion in the open field. "
03/01/1993 - "At postsynaptic 5-HT1A receptors mediating hypothermia, eltoprazine, WY 48,723, MDL 72832 and tandospirone are agonists, zalospirone is a partial agonist and (-)-tertatolol, WAY 100,135, MDL 73005 EF and SDZ 216-525 are antagonists."

10/15/2017 - "Eltoprazine treatment alone produced a near-complete suppression of dyskinesia but consistently increased parkinsonism. "