Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity |
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| Authors: | Mokrosz M J Charakchieva-Minol S Kozioł A Kłodzińska A Chojnacka-Wójcik E |
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| Institution: | Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków. |
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| Abstract: | Several 1,4-disubstituted arylpiperazine derivatives of 3-arylideneindolin-2(1H)-one (Z and E isomers) were tested for their 5-HT1A and 5-HT2A receptor activity in vitro and in vivo. It was shown that introduction of 3-arylidene substituents to indolin-2(1H)-one moiety allowed to change the mixed 5-HT1A/5-HT2A receptor ligands to 5-HT2A ones with antagonistic in vivo activity. |
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