Chronic treatment with MK-801 decreases D2 dopamine receptor function in rat striatum.
Present results show that a single treatment with dizocilpine (MK-801, 0.25 mg/kg IP) failed to modify the specific binding to D1 or D2 DA receptors. In contrast, repeated administrations for 3 weeks resulted in a statistically significant decrease of [3H]Spiroperidol binding to cortical or striatal membranes but did not change the number or the apparent affinity of [3H]MK-801 binding in well-washed cortical membranes. Consistent reduction in specific D2 receptor mediated behavior was obtained. The data suggest that the changes in DAergic function following repeated administrations with MK-801 could be suggestive of potential therapeutic uses of negative allosteric drugs in some DA related dysfunctions.
Gandolfi
O
O
Department of Pharmacology, University of Bologna, Italy.
Dall'Olio
R
R
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects*; D016291:Dizocilpine Maleate / Q000494:pharmacology*; D015259:Dopamine Agents / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D004873:Ergolines / Q000378:metabolism / Q000494:pharmacology; D006120:Grooming / Q000187:drug effects; D066298:In Vitro Techniques; D007700:Kinetics; D008024:Ligands; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D019257:Quinpirole; D051381:Rats; D017207:Rats, Sprague-Dawley; D013134:Spiperone / Q000494:pharmacology
D015259:Dopamine Agents; D065127:Dopamine D2 Receptor Antagonists; D004873:Ergolines; D008024:Ligands; D019257:Quinpirole; D013134:Spiperone; D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D016291:Dizocilpine Maleate