It has substantially higher affinity and potency in terms of dopamine transporter (DAT) inhibition than modafinil (Ki = 39.4nM vs. 8,160nM) whilst retaining the atypical DAT blocker profile of modafinil.[1][2] However, RDS03-94 also has high affinity for the sigma σ1 receptor (Ki = 2.19nM).[2]
RDS03-94 shows some reversal of tetrabenazine-induced motivational deficits in animals and hence may have the capacity to produce pro-motivational effects.[5][6] However, it appears to be less effective than certain other related agents, like JJC8-088.[6][5]
RDS03-94 is under development for the treatment of psychostimulant use disorder.[1] The drug was first described in the scientific literature in 2020.[1][2]
↑ 1.01.11.21.3"Modafinil and its structural analogs as atypical dopamine uptake inhibitors and potential medications for psychostimulant use disorder". Current Opinion in Pharmacology56: 13–21. February 2021. doi:10.1016/j.coph.2020.07.007. PMID32927246. "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].".
↑"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 Pharmacology & Translational Science7 (2): 515–532. February 2024. doi:10.1021/acsptsci.3c00322. PMID38357284.
