B dopaminergic receptor activation, either by levodopa or by direct dopamine receptor agonists, remains the bulwark of treatment of Parkinson’s disease.1 Levodopa and direct dopamine agonists are often used concurrently. Although it is known that apomorphine does not affect the pharmacokinetics of orally administered levodopa,2 it is not known whether dopamine agonists alter plasma levels of la...

Glutamate is the major excitatory neurotransmitter in central nervous system and, as such, many brain regions, including basal ganglia, are rich glutamatergic neurons. The importance of ganglia control voluntary movement has long been recognised, with effect dysfunction region exemplified by motor symptoms seen Parkinson’s disease (PD). However, and associated also play a role modulation emotio...

In this study, the ligand-receptor-G protein interactions of the dopamine D3 receptor expressed in Chinese hamster ovary cells were investigated using guanosine 5'-[gamma-thio]triphosphate-[35S] ([35S]GTPgammaS) and receptor binding experiments. Dopamine stimulated the [35S]GTPgammaS binding in a guanine nucleotide, magnesium and sodium-dependent manner. Dopamine and quinpirole produced maximal...

It is generally assumed that cannabinoids induce transient modulations of dopamine transmission through indirect regulation of its release. However, we previously described a direct cannabinoid-mediated control of tyrosine hydroxylase (TH) expression, in vitro. We herein report on the influence of cannabinoid agonists on the expression of this key enzyme in catecholamine synthesis as well as on...

PROGRESS TOWARDS DEVELOPMENT OF MULTIFUNCTIONAL, DOPAMINED2/D3 RECEPTOR AGONISTS AS SYMPTOMATIC AND DISEASE-MODIFYINGTHERAPEUTIC AGENTS FOR PARKINSON’S DISEASE

Posttranslational modifications (PTMs) of the beta-2 adrenoceptor (B2AR) play a fundamental role in receptor regulation by agonists. We have examined the effects of several agonists on net levels of B2AR palmitoylation and phosphorylation using epitope tagging in stably transfected human embryonal kidney (HEK) 293 cells, immunoaffinity purification, and mass spectrometry combined with the metho...