Adenosine A2A agonist CGS 21680 decreases the affinity of dopamine D2 receptors for dopamine in human striatum

Z Díaz-Cabiale; Y Hurd; D Guidolin; U B Finnman; M Zoli; L F Agnati; J J Vanderhaeghen; K Fuxe; S Ferré

doi:10.1097/00001756-200107030-00014

Adenosine A2A agonist CGS 21680 decreases the affinity of dopamine D2 receptors for dopamine in human striatum

Neuroreport. 2001 Jul 3;12(9):1831-4. doi: 10.1097/00001756-200107030-00014.

Authors

Z Díaz-Cabiale¹, Y Hurd, D Guidolin, U B Finnman, M Zoli, L F Agnati, J J Vanderhaeghen, K Fuxe, S Ferré

Affiliation

¹ Department of Neuroscience, Karolinska Institute, Stockholm, Sweden.

PMID: 11435907
DOI: 10.1097/00001756-200107030-00014

Abstract

Adenosine A2A receptors (A2AR) and dopamine D2 receptors (D2R) are highly concentrated in the striatum, where they are co-localized and exert reciprocal antagonistic interactions. It has been suggested that the A2R/D2R interactions might provide a therapeutic approach for basal ganglia disorders, such as Parkinson's disease, and schizophrenia. In the present work evidence is presented for the existence of an A2AR/D2R interaction in human brain by using quantitative autoradi- ography. The areas analyzed were the dorsal caudate nucleus and putamen. Parallel studies were performed in rat striatal sections. The A2AR agonist CGS 21680 was found to significantly increase IC50 values of competitive inhibition curves of the D2R/D3R antagonist [125I]iodosulpiride vs dopamine both in rat striatal and human striatal brain sections.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenosine / analogs & derivatives
Adenosine / pharmacology*
Adult
Animals
Antihypertensive Agents / pharmacology*
Binding, Competitive / drug effects
Binding, Competitive / physiology
Dopamine / metabolism
Dopamine / pharmacokinetics*
Dopamine D2 Receptor Antagonists*
Drug Interactions / physiology
Female
Humans
Male
Middle Aged
Neostriatum / cytology
Neostriatum / drug effects*
Neostriatum / metabolism
Neurons / drug effects*
Neurons / metabolism
Nucleus Accumbens / cytology
Nucleus Accumbens / drug effects
Nucleus Accumbens / metabolism
Phenethylamines / pharmacology*
Purinergic P1 Receptor Agonists*
Rats
Rats, Sprague-Dawley
Receptor, Adenosine A2A
Receptors, Dopamine D2 / metabolism
Receptors, Purinergic P1 / metabolism
Sulpiride / analogs & derivatives
Sulpiride / pharmacokinetics

Substances

Antihypertensive Agents
Dopamine D2 Receptor Antagonists
Phenethylamines
Purinergic P1 Receptor Agonists
Receptor, Adenosine A2A
Receptors, Dopamine D2
Receptors, Purinergic P1
iodosulpride
2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine
Sulpiride
Adenosine
Dopamine