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- W2100583766 abstract "Cycloalkanecarboxamido)ethyl]-1-(2-methoxyphenyl)piperazin es 8a-c, 8e, and 8h were obtained by acylation of 4-(2-aminoethyl)-1-(2-methoxyphenul)piperazine, and their 5-HT 1A , 5-HT 2A and α 1 receptor affinities were determined. It was found that the terminal cycloalkane moiety strongly stabilizes both the 5-HT 1A and 5-HT 2A receptor-ligand complexes. It was demonstrated that the most active 5-HT 1A ligands 8e and 8h (Ki=2.1 and 0.21 nM, respectively) behaved as potent agonists of these receptors, i.e. both derivatives mimicked 8-OH-DPAT in the lower lip retraction (LLR) model and the effect was susceptible to blockade by reasonable doses of the selective 5-HT 1A receptor antagonist (S)-WAY-100135" @default.
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- W2100583766 date "2010-08-12" @default.
- W2100583766 modified "2023-09-28" @default.
- W2100583766 title "ChemInform Abstract: Structure-Activity Relationship Studies of CNS Agents. Part 26. 4-(2-( Cycloalkanecarboxamido)ethyl)-1-(2-methoxyphenyl)-piperazines: High- Affinity 5-HT1A Agonists" @default.
- W2100583766 cites W2950109373 @default.
- W2100583766 doi "https://doi.org/10.1002/chin.199614177" @default.
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