Abstract
A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D(2) and D(4) receptors. Three compounds having D(2)/D(4) affinity ratios approximating that found for the atypical neuroleptic clozapine were further evaluated in behavioral tests of antipsychotic efficacy and motor side effects.
MeSH terms
-
Amphetamine / antagonists & inhibitors
-
Amphetamine / pharmacology
-
Animals
-
Antipsychotic Agents / metabolism
-
Antipsychotic Agents / pharmacology
-
Binding, Competitive / drug effects
-
Catalepsy / chemically induced
-
Central Nervous System Stimulants / antagonists & inhibitors
-
Central Nervous System Stimulants / pharmacology
-
Clozapine / metabolism
-
Clozapine / pharmacology
-
Dopamine Antagonists / chemical synthesis*
-
Dopamine Antagonists / pharmacology*
-
Dopamine Antagonists / toxicity
-
Dopamine D2 Receptor Antagonists*
-
Drug Evaluation, Preclinical
-
Dyskinesia, Drug-Induced / psychology
-
Half-Life
-
Haloperidol / pharmacology
-
Humans
-
In Vitro Techniques
-
Indicators and Reagents
-
Indoles / chemical synthesis*
-
Indoles / pharmacology*
-
Indoles / toxicity
-
Motor Activity / drug effects
-
Piperazines / chemical synthesis*
-
Piperazines / pharmacology*
-
Piperazines / toxicity
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, Dopamine D4
-
Recombinant Proteins / drug effects
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Antipsychotic Agents
-
Central Nervous System Stimulants
-
DRD4 protein, human
-
Dopamine Antagonists
-
Dopamine D2 Receptor Antagonists
-
Drd4 protein, rat
-
Indicators and Reagents
-
Indoles
-
Piperazines
-
Recombinant Proteins
-
benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone
-
Receptors, Dopamine D4
-
Amphetamine
-
Clozapine
-
Haloperidol