期刊
AUSTRALIAN JOURNAL OF CHEMISTRY
卷 63, 期 1, 页码 56-67出版社
CSIRO PUBLISHING
DOI: 10.1071/CH09353
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资金
- Fonds de la Recherche Scientifique FNRS
- Fonds Speciaux pour la Recherche of the University of Liege (Belgium)
- National Institute of Mental Health Psychoactive Drug Screening Program
- [U19MH82441]
A series of substituted 4-aryl-piperazine-ethyl heteroarylcarboxamides were prepared and tested in in vitro radioligand binding studies. The presence of a quinoxaline has a favourable impact in terms of serotonin 5-HT1A versus dopamine D4.2 receptor selectivity. Compounds with a 3-CF3 group at the distal phenyl ring are the most effective in terms of affinity and selectivity for 5-HT1A versus D4.2 receptors. A 4-phenyl-1,2,3,6-tetrahydropyridine in place of the corresponding 4-phenyl-piperazine side chain is also favourable not only for the affinity for 5-HT1A and D4.2 receptors but also in some cases for alpha(2A)-adrenoceptors.
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