Pharmacological profile of the "triple" monoamine neurotransmitter uptake inhibitor, DOV 102,677.

Cellular and Molecular Neurobiology
Piotr PopikAnthony S Basile

Abstract

1. The molecular and behavioral pharmacology of DOV 102,677 is characterized. 2. This characterization was performed using radioligand binding and neurotransmitter uptake assays targeting the monoamine neurotransmitter receptors. In addition, the effects of DOV 102,677 on extracellular neurotransmitter levels were investigated using in vivo microdialysis. Finally, the effects of DOV 102,677 in the forced swim test, locomotor function, and response to prepulse inhibition was investigated.3. DOV 102,677 is a novel, "triple" uptake inhibitor that suppresses [(3)H]dopamine (DA), [(3)H]norepinephrine (NE) and [(3)H]serotonin (5-HT) uptake by recombinant human transporters with IC(50) values of 129, 103 and 133 nM, respectively. Radioligand binding to the dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters is inhibited with k (i) values of 222, 1030, and 740 nM, respectively. DOV 102,677 (20 mg/kg IP) increased extracellular levels of DA and 5-HT in the prefrontal cortex to 320 and 280% above baseline 100 min after administration. DA levels were stably increased for the duration (240 min) of the study, but serotonin levels declined to baseline by 200 min after administration. NE levels increased linearly to a maxi...Continue Reading

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Citations

May 7, 2008·Psychopharmacology·Piotr PopikGabriel Nowak
Sep 9, 2011·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Xiaohua LiRichard C Shelton
Aug 24, 2007·Expert Opinion on Investigational Drugs·Zhengming Chen, Phil Skolnick
May 12, 2009·Expert Opinion on Investigational Drugs·Shrinivas K Kulkarni, Ashish Dhir
Dec 1, 2015·Future Medicinal Chemistry·Horrick SharmaAloke Dutta
Aug 16, 2008·The Mount Sinai Journal of Medicine, New York·Srijan Sen, Gerard Sanacora
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