ArticleActa pharmacologica Sinica2013
SKF83959 is a novel triple reuptake inhibitor that elicits anti-depressant activity.
Article in Acta pharmacologica Sinica, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed, 18 citations in OpenAlex.
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- Efficacy, Tolerability, and Safety of Toludesvenlafaxine for the Treatment of Major Depressive Disorder-A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Allosteric Modulators of Sigma-1 Receptor: A Review.Frontiers in pharmacology · 2019Review
- Dihydromyricetin exerts a rapid antidepressant-like effect in association with enhancement of BDNF expression and inhibition of neuroinflammation.Psychopharmacology · 2018Article
- Recent Advances in the Realm of Allosteric Modulators for Opioid Receptors for Future Therapeutics.ACS chemical neuroscience · 2017Review
- Allosteric Modulation of Sigma-1 Receptors Elicits Rapid Antidepressant Activity.CNS neuroscience & therapeutics · 2016Article
- Allosteric modulation of sigma-1 receptors elicits anti-seizure activities.British journal of pharmacology · 2015Article
- Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor.ACS chemical neuroscience · 2015Article
- Triple reuptake inhibitors as potential next-generation antidepressants: a new hope?Future medicinal chemistry · 2015Review
- SKF83959 produces antidepressant effects in a chronic social defeat stress model of depression through BDNF-TrkB pathway.The international journal of neuropsychopharmacology · 2014Article
- Effects of SKF83959 on the excitability of hippocampal CA1 pyramidal neurons: a modeling study.Acta pharmacologica Sinica · 2014Article
Corrections and comments
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Authors and funding
9 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimSKF83959 (3-methyl-6-chloro-7,8-hydroxy-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine) is an atypical dopamine receptor-1 (D1 receptor) agonist, which exhibits many D1 receptor-independent effects. In the present work, we examined the effects of SKF83959 on monoaminergic transporters in vitro and its anti-depressant activity in vivo.
methodsHuman serotonin transporter (SERT), norepinephrine transporters (NET) or dopamine transporters (DAT) were stably expressed in CHO cells. The uptake kinetics of SERT, NET, and DAT were examined using [(3)H]-serotonin, [(3)H]-norepinephrine or [(3)H]-dopamine, respectively. A triple reuptake inhibitor DOV21947 was used as the positive control. Tail suspension test and forced swimming test were conducted in mice. SKF83959 or DOV21947 (2-8 mg/kg) were intraperitoneally injected 30 min before the tests.
resultsSKF83959 was a competitive inhibitor of SERT (K(i)=1.43±0.45 μmol/L), but a noncompetitive inhibitor of NET (K(i)=0.60±0.07 μmol/L) and DAT (K(i)=9.01±0.80 μmol/L). In contrast, DOV21947 was a competitive inhibitor of SERT (K(i)=0.89±0.24 μmol/L) and DAT (K(i)=1.47±0.31 μmol/L) and a noncompetitive inhibitor of NET (K(i)=0.18±0.04 μmol/L). In mice, both SKF83959 and DOV21947 elicited anti-depressant activity in a dose-dependent manner.
conclusionSKF83959 functions as a novel triple reuptake inhibitor in vitro and exerts anti-depressant effects in vivo.
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