RDS03-94, or RDS3-094, is an atypical

dopamine reuptake inhibitor A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dop ...

that was derived from the

wakefulness-promoting agent A wakefulness-promoting agent (WPA), or wake-promoting agent, is a drug that increases wakefulness and arousal. They are similar to but distinct from psychostimulants, which not only promote wakefulness but also produce other more overt central ...

modafinil Modafinil, sold under the brand name Provigil among others, is a central nervous system (CNS) stimulant and wakefulness-promoting agent, eugeroic (wakefulness promoter) medication used primarily to treat narcolepsy, a sleep disorder characteri ...

. It has substantially higher

affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...

and

potency Potency may refer to: * Potency (pharmacology), a measure of the activity of a drug in a biological system * Virility * Cell potency, a measure of the differentiation potential of stem cells * In homeopathic dilutions, potency is a measure of ho ...

in terms of

dopamine transporter The dopamine transporter (DAT, also sodium-dependent dopamine transporter) is a membrane-spanning protein coded for in humans by the ''SLC6A3'' gene (also known as ''DAT1''), that pumps the neurotransmitter dopamine out of the synaptic cleft ba ...

(DAT)

inhibition Inhibitor or inhibition may refer to: Biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotransm ...

than modafinil (K_i = 39.4nM vs. 8,160nM) whilst retaining the atypical DAT blocker profile of modafinil. However, RDS03-94 also has high affinity for the

sigma Sigma ( ; uppercase Σ, lowercase σ, lowercase in word-final position ς; ) is the eighteenth letter of the Greek alphabet. In the system of Greek numerals, it has a value of 200. In general mathematics, uppercase Σ is used as an operator ...

σ₁ receptor (K_i = 2.19nM). RDS03-94 shows some reversal of

tetrabenazine Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the US Food and Drug Administration (FDA) approved the use of tet ...

-induced motivational deficits in animals and hence may have the capacity to produce pro-motivational effects. However, it appears to be less effective than certain other related agents, like

JJC8-088 JJC8-088 is a dopamine reuptake inhibitor (DRI) that was chemical derivative, derived from the wakefulness-promoting agent modafinil. It has substantially higher affinity (pharmacology), affinity for the dopamine transporter (DAT) than modafinil ...

. RDS03-94 is under development for the treatment of psychostimulant use disorder. The drug was first described in the

scientific literature Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical ...

in 2020.

References

4-Fluorophenyl compounds Enantiopure drugs Experimental drugs Piperazines Pro-motivational agents Secondary alcohols Sigma receptor modulators Stimulants Thioethers Modafinil analogues {{Nervous-system-drug-stub

See also

References