Chemistry:JJC8-089

From HandWiki

JJC8-089 is a dopamine reuptake inhibitor (DRI) that was derived from modafinil and is related to JJC8-016, JJC8-088, and JJC8-091.[1][2] Its affinity (Ki) for the dopamine transporter (DAT) is 37.8 nM, for the norepinephrine transporter (NET) is 11,820 nM (313-fold lower than for the DAT), for the serotonin transporter (SERT) is 6,800 nM (180-fold lower than for the DAT), and for the sigma σ1 receptor is 2.24 nM (17-fold higher than for the DAT).[2][3] It also has significant affinity for several dopamine receptors.[3] JJC8-089 has substantially higher affinity for the DAT than modafinil.[1][2][3] The drug shows pro-motivational effects in animals.[4][5] It was first described in the scientific literature by 2016.[6][7]

See also

References

  1. ↑ 1.0 1.1 "Discovery and Development of Monoamine Transporter Ligands". Drug Development in Psychiatry. Advances in Neurobiology. 30. 2023. 101–129. doi:10.1007/978-3-031-21054-9_4. ISBN 978-3-031-21053-2. 
  2. ↑ 2.0 2.1 2.2 "New Drugs, Old Targets: Tweaking the Dopamine System to Treat Psychostimulant Use Disorders". Annu Rev Pharmacol Toxicol 61: 609–628. January 2021. doi:10.1146/annurev-pharmtox-030220-124205. PMID 33411583. 
  3. ↑ 3.0 3.1 3.2 "Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability". Eur J Med Chem 208. December 2020. doi:10.1016/j.ejmech.2020.112674. PMID 32947229. 
  4. ↑ "The Neurobiology of Activational Aspects of Motivation: Exertion of Effort, Effort-Based Decision Making, and the Role of Dopamine". Annu Rev Psychol 75: 1–32. January 2024. doi:10.1146/annurev-psych-020223-012208. PMID 37788571. 
  5. ↑ "Potential therapeutics for effort-related motivational dysfunction: assessing novel atypical dopamine transport inhibitors". Neuropsychopharmacology 49 (8): 1309–1317. July 2024. doi:10.1038/s41386-024-01826-1. PMID 38429498. 
  6. ↑ "Novel and High Affinity 2-[(Diphenylmethyl)sulfinylacetamide (Modafinil) Analogues as Atypical Dopamine Transporter Inhibitors"]. J Med Chem 59 (23): 10676–10691. December 2016. doi:10.1021/acs.jmedchem.6b01373. PMID 27933960. 
  7. ↑ "Atypical dopamine transporter inhibitors attenuate compulsive-like methamphetamine self-administration in rats". Neuropharmacology 131: 96–103. March 2018. doi:10.1016/j.neuropharm.2017.12.006. PMID 29217282. 



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