Draft:RDS03-94
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| Formula | C24H32F2N2OS |
| Molar mass | 434.59 g·mol−1 |
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RDS03-94 is an atypical dopamine reuptake inhibitor that was derived from the wakefulness-promoting agent modafinil.[1][2][3][4] It has substantially higher affinity and potency in terms of dopamine transporter (DAT) inhibition than modafinil (Ki = 39.4 nM vs. 8,160 nM) whilst retaining the atypical DAT blocker profile of modafinil.[1][2] However, RDS03-94 also has high affinity for the sigma σ1 receptor (Ki = 2.19 nM).[2] It is under development for the treatment of psychostimulant use disorder.[1] The drug was first described in the scientific literature in 2020.[1][2]
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.
More recently, by introducing the 2,6-dimethyl substitution on the piperazine ring, some improvement in drug-like properties was realized with RDS03-94 [29]. Nevertheless, the piperazine ring remained a metabolically labile functional group and hence a new series of analogues in which it was replaced with an amino-piperidine function was prepared [30]. These new analogues demonstrated superior metabolic stability and are currently being evaluated in rodent models of [psychostimulant use disorder (PSUD)]. In addition, novel heterocyclic-based analogues that may also be promising new leads for PSUD therapeutics have recently been reported [31,32].
- ^ a b c d Slack RD, Ku TC, Cao J, Giancola JB, Bonifazi A, Loland CJ, Gadiano A, Lam J, Rais R, Slusher BS, Coggiano M, Tanda G, Newman AH (March 2020). "Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability". J Med Chem. 63 (5): 2343–2357. doi:10.1021/acs.jmedchem.9b01188. PMC 9617638. PMID 31661268.
- ^ Ku TC, Cao J, Won SJ, Guo J, Camacho-Hernandez GA, Okorom AV, Salomon KW, Lee KH, Loland CJ, Duff HJ, Shi L, Newman AH (February 2024). "Series of (([1,1'-Biphenyl]-2-yl)methyl)sulfinylalkyl Alicyclic Amines as Novel and High Affinity Atypical Dopamine Transporter Inhibitors with Reduced hERG Activity". ACS Pharmacol Transl Sci. 7 (2): 515–532. doi:10.1021/acsptsci.3c00322. PMID 38357284.
- ^ Okorom AV, Camacho-Hernandez GA, Salomon K, Lee KH, Ku TC, Cao J, Won SJ, Friedman J, Lam J, Paule J, Rais R, Klein B, Xi ZX, Shi L, Loland CJ, Newman AH (January 2024). "Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile". J Med Chem. 67 (1): 709–727. doi:10.1021/acs.jmedchem.3c02037. PMID 38117239.
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