Indoline and piperazine containing derivatives as a novel class of mixed D2/D4 receptor antagonists. Part 2: Asymmetric synthesis and biological evaluation

Autor: Xiao-Shu He, Andrew Thurkauf, Andrzej Kieltyka, Jan W. F. Wasley, Robbin Brodbeck, He Zhao, Diane C. Hoffman, Renee J. Primus
Rok vydání: 2002
Předmět:
Dyskinesia
Drug-Induced
Indoles
medicine.medical_treatment
Clinical Biochemistry
Drug Evaluation
Preclinical
Pharmaceutical Science
Carboxamide
Biochemistry
Chemical synthesis
Piperazines
Rats
Sprague-Dawley
chemistry.chemical_compound
Drug Discovery
Receptor
Clozapine
Biological evaluation
Stereoisomerism
General Medicine
Recombinant Proteins
Dopamine D2 Receptor Antagonists
Indoline
Molecular Medicine
Antipsychotic Agents
Half-Life
medicine.drug
Stereochemistry
medicine.drug_class
In Vitro Techniques
Motor Activity
Binding
Competitive
Structure-Activity Relationship
Dopamine receptor D2
medicine
Animals
Humans
Antipsychotic
Molecular Biology
Catalepsy
Receptors
Dopamine D4
Organic Chemistry
Enantioselective synthesis
Rats
Amphetamine
Piperazine
chemistry
Dopamine Antagonists
Haloperidol
Central Nervous System Stimulants
Indicators and Reagents
Zdroj: Bioorganic & Medicinal Chemistry Letters. 12:3111-3115
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(02)00656-x
Popis: A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D2 and D4 receptors. Three compounds having D2/D4 affinity ratios approximating that found for the atypical neuroleptic clozapine were further evaluated in behavioral tests of antipsychotic efficacy and motor side effects.
Databáze: OpenAIRE
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