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A pharmacological profile of the novel, peripherally‐selective k‐opioid receptor agonist, EMD 61753
TLDR
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.
Effects of sarizotan on the corticostriatal glutamate pathways
TLDR
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.
Local administration of sarizotan into the subthalamic nucleus attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats
TLDR
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.
Sarizotan, a serotonin 5-HT1A receptor agonist and dopamine receptor ligand. 1. Neurochemical profile
TLDR
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.
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