In vitro characterization of SLV308 (7‐[4‐methyl‐1‐piperazinyl]‐2(3H)‐benzoxazolone, monohydrochloride): A novel partial dopamine D2 and D3 receptor agonist and serotonin 5‐HT1A receptor agonist

@article{Glennon2006InVC,
  title={In vitro characterization of SLV308 (7‐[4‐methyl‐1‐piperazinyl]‐2(3H)‐benzoxazolone, monohydrochloride): A novel partial dopamine D2 and D3 receptor agonist and serotonin 5‐HT1A receptor agonist},
  author={Jeffrey C. Glennon and Guus van Scharrenburg and Eric Ronken and Mayke B. Hesselink and Jan Hendrik Reinders and Martina A W van der Neut and Stephen K. Long and Rolf W. Feenstra and Andrew C McCreary},
  journal={Synapse},
  year={2006},
  volume={60}
}
Present Parkinson's disease treatment strategies are far from ideal for a variety of reasons; it has therefore been suggested that partial dopamine receptor agonism might be a potential therapeutic approach with potentially fewer side effects. In the present study, we describe the in vitro characterization of the nonergot ligand SLV308 (7‐[4‐methyl‐1‐piperazinyl]‐2(3H)‐benzoxazolonemonohydrochloride). SLV308 binds to dopamine D2, D3, and D4 receptors and 5‐HT1A receptors and is a partial… 
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An in vivo pharmacological evaluation of pardoprunox (SLV308) — A novel combined dopamine D2/D3 receptor partial agonist and 5-HT1A receptor agonist with efficacy in experimental models of Parkinson's disease
Multitarget 1,4-Dioxane Compounds Combining Favorable D2-like and 5-HT1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.
The effect of methoxy and hydroxy substitutions in different positions of the phenoxy moiety of the N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-phenoxyethan-1-amine scaffold on the affinity/activity…
In vivo effects of pardoprunox (SLV308), a partial D2/D3 receptor and 5‐HT1A receptor agonist, on rat dopamine and serotonin neuronal activity
TLDR
The present study shows that pardoprunox acts in the VTA as a potent partial D2‐like receptor agonist reducing preferentially the burst activity linked to the phasic activity of DA neurons.
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TLDR
Twenty novel 1-(3-((6-fluoropyridin-3-yl)oxy)propyl)piperazine derivatives were designed and synthesized using a bioisosterism approach, and the results showed that several compounds exhibited a multitarget combination of D2/5-HT1A agonism.
From the cell to the clinic: a comparative review of the partial D₂/D₃receptor agonist and α2-adrenoceptor antagonist, piribedil, in the treatment of Parkinson's disease.
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Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.
TLDR
Results suggest that 5-HT(1A) and D(2) dual-receptor agonist (-)-15 may present a novel candidate drug in the treatment of PD and LID.
Synthesis, Pharmacological Characterization and QSAR Modelling of 4-Phenylpiperidines and 4-Phenylpiperazines Effects on the dopaminergic neurotransmission in vivo
TLDR
It is primarily interactions with these two targets that lead to the in vivo response observed for this class of compounds, and a strong correlation between the affinities to the D2 receptor and to MAO A and the levels of the metabolite DOPAC in striatum has been established.
Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1.
The partial dopamine agonist pardoprunox (SLV308) administered in combination with l-dopa improves efficacy and decreases dyskinesia in MPTP treated common marmosets
Pardoprunox reverses motor deficits but induces only mild dyskinesia in MPTP‐treated common marmosets
TLDR
The results suggest that the partial D2 agonist pardoprunox (SLV308) is less likely to prime for dyskinesia or to lead to the expression of dysKinesia than either levodopa or full dopamine agonists.
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