Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity

M J Mokrosz; S Charakchieva-Minol; A Kozioł; A Kłodzińska; E Chojnacka-Wójcik

doi:10.1016/s0960-894x(01)00181-0

Influence of the terminal amide fragment geometry in some 3-arylideneindolin-2(1H)-ones on their 5-HT1A/5-HT2A receptor activity

Bioorg Med Chem Lett. 2001 May 7;11(9):1229-31. doi: 10.1016/s0960-894x(01)00181-0.

Authors

M J Mokrosz¹, S Charakchieva-Minol, A Kozioł, A Kłodzińska, E Chojnacka-Wójcik

Affiliation

¹ Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków.

PMID: 11354383
DOI: 10.1016/s0960-894x(01)00181-0

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.

MeSH terms

8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
Animals
Behavior, Animal / drug effects
Hippocampus / drug effects
Hippocampus / metabolism
Indoles / chemical synthesis*
Indoles / pharmacology*
Magnetic Resonance Spectroscopy
Rats
Receptor, Serotonin, 5-HT2A
Receptors, Serotonin / drug effects*
Receptors, Serotonin, 5-HT1
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / pharmacology
Serotonin Receptor Agonists / pharmacology
Structure-Activity Relationship

Substances

Indoles
Receptor, Serotonin, 5-HT2A
Receptors, Serotonin
Receptors, Serotonin, 5-HT1
Serotonin Antagonists
Serotonin Receptor Agonists
8-Hydroxy-2-(di-n-propylamino)tetralin