Draft:JJC8-088
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| Formula | C28H32F2N2O2S |
| Molar mass | 498.63 g·mol−1 |
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JJC8-088 is a dopamine reuptake inhibitor that was derived from the wakefulness-promoting agent modafinil.[1][2][3] It has substantially higher affinity for the dopamine transporter than modafinil (Ki = 6.72 nM vs. 2,600 nM).[2] In contrast to modafinil and other analogues, which are atypical dopamine reuptake inhibitors, JJC8-088 is a typical cocaine-like dopamine reuptake inhibitor.[1][3] It has potent cocaine-like psychostimulant effects, produces robust and dose-dependent increases in dopamine levels in the nucleus accumbens, and is readily self-administered and substitutes for cocaine in animals.[1][3] Similarly to cocaine, but unlike modafinil and other analogues, JJC8-088 stabilizes the dopamine transporter in an outward-facing open conformation.[1]
See also
[edit]References
[edit]- ^ a b c d Tanda G, Hersey M, Hempel B, Xi ZX, Newman AH (February 2021). "Modafinil and its structural analogs as atypical dopamine uptake inhibitors and potential medications for psychostimulant use disorder". Curr Opin Pharmacol. 56: 13–21. doi:10.1016/j.coph.2020.07.007. PMC 8247144. PMID 32927246.
- ^ a b Aggarwal S, Mortensen OV (2023). "Discovery and Development of Monoamine Transporter Ligands". Adv Neurobiol. Advances in Neurobiology. 30: 101–129. doi:10.1007/978-3-031-21054-9_4. ISBN 978-3-031-21053-2. PMC 10074400. PMID 36928847.
- ^ a b c Hersey M, Bacon AK, Bailey LG, Coggiano MA, Newman AH, Leggio L, Tanda G (2021). "Psychostimulant Use Disorder, an Unmet Therapeutic Goal: Can Modafinil Narrow the Gap?". Front Neurosci. 15: 656475. doi:10.3389/fnins.2021.656475. PMC 8187604. PMID 34121988.
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