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A pharmacological profile of the novel, peripherally‐selective k‐opioid receptor agonist, EMD 61753
EMD 61753 in the hyperalgesic pressure test was completely inhibited by injection of the k‐opioid antagonist norbinaltorphimine into the inflamed tissue, a result which indicates that this opioid effect is mediated peripherally.
EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT1A receptor agonistic properties.
Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone.
Effects of sarizotan on the corticostriatal glutamate pathways
The findings suggest that the antidyskinetic properties of sarizotan could be mediated via its 5‐HT1A agonist actions in the motor cortex, leading to reduced activity in the corticostriatal glutamate pathways with reduced activation of the striatopallidal GABA pathway mediating motor inhibition.
Low doses of sarizotan reduce dyskinesias and maintain antiparkinsonian efficacy of L-Dopa in parkinsonian monkeys.
Local administration of sarizotan into the subthalamic nucleus attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats
- C. Marín, E. Aguilar, M. Rodriguez-Oroz, G. Bartoszyk, J. Obeso
- Biology, PsychologyPsychopharmacology
- 22 January 2009
Results suggest that the STN is a target structure for the antidyskinetic action of sarizotan and indicate that drug-mediated modulation of STN activity may be an alternative option for the treatment of levodopa-induced dyskinesias in Parkinson’s disease.
The highly selective 5‐hydroxytryptamine (5‐HT)2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced…
Effect of EMD 281014 produces effects in the forced swim test resembling those of antidepressants.
Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile
- G. Bartoszyk, C. van Amsterdam, H. Greiner, W. Rautenberg, H. Russ, C. Seyfried
- Biology, ChemistryJournal of Neural Transmission
- 1 February 2004
Sarizotan at higher doses decreased DA precursor accumulation in reserpinized rats and induced contralateral rotational behavior in unilaterally substantia nigra lesioned rats, indicating some intrinsic dopaminergic activity.
B-vitamins potentiate the antinociceptive effect of diclofenac in carrageenin-induced hyperalgesia in the rat tail pressure test