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Induction of c-fos mRNA in rat medial prefrontal cortex by antipsychotic drugs: role of dopamine D2 and D3 receptors.
It is hypothesize that blockade of D3 receptors may enhance c-fos gene expression in the medial prefrontal cortex but that of D2 receptors may prevent the same, as well as U-99194A, an antagonist with 20-fold selectivity for D3 over D2 receptor that produced greater induction of c- fos mRNA at lower doses.
Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications.
The results with the antipsychotic agents tested, support the concept that dopamine D4 receptor selectivity may confer clozapine-like antipsychotics efficacy and furthermore that dopamineD2 receptor selectiveness may confer side effect liability (extrapyramidal side effects and tardive dyskinesia).
Dopamine D2 receptor binding properties of [3H]U-86170, a dopamine receptor agonist.
This agonist ligand is especially effective in identifying agonists and partial agonists, as well as antagonists, and affords a more precise evaluation of their affinity for the dopamine D2 receptor, without the use of multiple site analysis, than does an antagonist [3H]-ligand.
Intrinsic activity determinations at the dopamine D2 guanine nucleotide-binding protein-coupled receptor: utilization of receptor state binding affinities.
The maximal effect of several of these compounds on rat striatal homovanillic acid (HVA) levels was determined and the drug-induced changes in tissue HVA levels were found to be consistent with the affinity-derived intrinsic activities of the drugs.
Dopaminergic and serotonergic activities of imidazoquinolinones and related compounds.
The synthesis of 5-(dipropylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij] quinolin-2(1H)-one (5), a potent dopamine D2 agonist showing high dopamine/serotonin (5HT1A) selectivity, is described.
Pre- and postsynaptic dopaminergic activities of U-86170F
It is demonstrated that U-86170F is a potent dopamine autoreceptor agonist, with limited activity at the postsynaptic receptor, in the GBL, prolactin, and HVA models.
Differential Induction of c-fos mRNA in Rat Prefrontal Cortex by Typical Versus Atypical Antipsychotics
Atypical antipsychotic drugs (APDs) typified by clozapine differ from the typical agents (e.g., haloperidol) by displaying superior efficacy in the treatment of negative symptoms and reduced