ArticleACS medicinal chemistry letters2016
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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
18 citing papers in PubMed.
- Dually Acting Ligands Targeting Serotonin Receptors: Implications in CNS Disorders.Journal of medicinal chemistry · 2026Review
- Compound PZ-1262, a 4-isoquinoline-sulfonamide analog of Brexpiprazole, produces potential antidepressant, anxiolytic and procognitive effects in rodent models.Pharmacological reports : PR · 2025Article
- The role of trimethylamine N-oxide in disease pathogenesis and the therapeutic potential of traditional Chinese medicine.Frontiers in pharmacology · 2025Review
- Potential Anti-Amnesic Activity of a Novel Multimodal Derivative of Salicylamide, JJGW08, in Mice.Pharmaceuticals (Basel, Switzerland) · 2023Article
- The Constitutive Activity of Spinal 5-HTBiomolecules · 2023Article
- 1-(Arylsulfonyl-isoindol-2-yl)piperazines as 5-HTBiomolecules · 2022Article
- TMAO as a potential biomarker and therapeutic target for chronic kidney disease: A review.Frontiers in pharmacology · 2022Review
- The Phenoxyalkyltriazine Antagonists for 5-HTInternational journal of molecular sciences · 2021Article
- Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HTJournal of medicinal chemistry · 2021Article
- Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties.Molecules (Basel, Switzerland) · 2021Article
- 2-Phenyl-1ACS chemical neuroscience · 2021Article
- Constitutive Activity of Serotonin Receptor 6 Regulates Human Cerebral Organoids Formation and Depression-like Behaviors.Stem cell reports · 2021Article
- Effect of 5-HTNeuropsychiatric disease and treatment · 2021Article
- Sustainable Synthesis of a Potent and Selective 5-HTThe Journal of organic chemistry · 2020Article
- The Faster-Onset Antidepressant Effects of Hypidone Hydrochloride (YL-0919) in Monkeys Subjected to Chronic Unpredictable Stress.Frontiers in pharmacology · 2020Article
- Drug Discovery and Development of Novel Therapeutics for Inhibiting TMAO in Models of Atherosclerosis and Diabetes.Frontiers in physiology · 2020Review
- Are the Hydantoin-1,3,5-triazine 5-HTMolecules (Basel, Switzerland) · 2019Article
- Serotonin 5-HTCNS drugs · 2017Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of N1-azinylsulfonyl-3-(1,2,3,6,tetrahyrdopyridin-4-yl)-1H-indole derivatives was designed to obtain highly potent 5-HT6 receptor ligands. The study allowed for the identification of 25 (4-{[5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-1-yl]sulfonyl}isoquinoline), a potent and selective 5-HT6 receptor antagonist. The selected compound, was evaluated in vivo in a novel object recognition (NOR) and forced swim (FST) tests in rats, demonstrating distinct pro-cognitive and antidepressant-like properties (MED = 1 mg/kg and 0.1 mg/kg, i.p., respectively). Compound SB-742457, used as comparator, reversed memory deficits in NOR task in similar doses, while in FST it was active in 10-30-fold higher dose (3 mg/kg). In contrast to SB-742457, which was active in Vogel test (MED = 3 mg/kg), compound 25 displayed no anxiolytic activity.
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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.