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Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT_1A and 5-HT_7A Receptors.

ABSTRACT: We have previously identified 5-chloro-2-methyl-2-(3-(4-(pyridin-2-yl)piperazin-1-yl)propyl)-2,3-dihydro-1H-inden-1-one (SYA0340) as a dual 5-HT_1A and 5-HT₇ receptor ligand, and we posited such ligands might find utility in the treatment of various CNS related illnesses including cognitive and anxiolytic impairments. However, SYA0340 has a chiral center and its enantiomers may confound the readouts for their functional characteristics. Thus, in this study, we resynthesized SYA0340, separated the enantiomers, identified the absolute configurations, and evaluated their binding affinities and functional characteristics at both the 5-HT_1A and 5-HT_7A receptors. The results of this study show that the (+)-SYA0340-P1 [specific rotation [α] = +18.

SUBMITTER: Bricker BA

PROVIDER: S-EPMC10285950 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature

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Dataset Information

Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT_1A and 5-HT_7A Receptors.

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Dataset Information

Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT1A and 5-HT7A Receptors.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT_1A and 5-HT_7A Receptors.