ArticleBioorganic & medicinal chemistry2016
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands.
Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
8 citing papers in PubMed, 21 citations in OpenAlex.
- Formal nitrogen-to-carbon replacement in isoindolines to form indenesChemical science · 2026Article
- Design and discovery of a high affinity, selective and β-arrestin biased 5-HTMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2022Article
- New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.European journal of medicinal chemistry · 2021Article
- A study of the structure-affinity relationship in SYA16263; is a DBioorganic & medicinal chemistry · 2021Article
- Enantioseparation of 5-chloro-2-{2-[3,4-dihydroisoquinoline-2(1H)-yl]ethyl}-2-methyl-2,3-dihydro-1H-inden-1-one (SYA 40247), a high-affinity 5-HTBiomedical chromatography : BMC · 2019Article
- New analogs of SYA013 as sigma-2 ligands with anticancer activity.Bioorganic & medicinal chemistry · 2019Article
- Recognition of repulsive and attractive regions of selected serotonin receptor binding site using FMO-EDA approach.Journal of molecular modeling · 2019Article
- Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.Bioorganic & medicinal chemistry · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
5-HT1A and 5-HT7 receptors have been at the center of discussions recently due in part to their major role in the etiology of major central nervous system diseases such as depression, sleep disorders, and schizophrenia. As part of our search to identify dual targeting ligands for these receptors, we have carried out a systematic modification of a selective 5HT7 receptor ligand culminating in the identification of several dual 5-HT1A and 5-HT7 receptor ligands. Compound 16, a butyrophenone derivative of tetrahydroisoquinoline (THIQ), was identified as the most potent agent with low nanomolar binding affinities to both receptors. Interestingly, compound 16 also displayed moderate affinity to other clinically relevant dopamine receptors. Thus, it is anticipated that compound 16 may serve as a lead for further exploitation in our quest to identify new ligands with the potential to treat diseases of CNS origin.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.