RTI-336

RTI-336 is a synthetic phenyltropane derivative that acts as a potent and selective dopamine reuptake inhibitor. It binds to the dopamine transporter (DAT) with approximately 20 times higher affinity than cocaine but produces relatively mild stimulant effects, characterized by a slower onset and longer duration of action compared to cocaine. These pharmacological properties make it a candidate for the treatment of cocaine dependence, functioning as an indirect agonist therapy similar to methadone for opioid addiction. Preclinical studies in animal models have shown that RTI-336 can substitute for cocaine, reduce self-administration of cocaine, and decrease rates of use—especially when combined with SSRIs. In phase 1 clinical trials in healthy volunteers, single oral doses up to 20 mg were well-tolerated with good safety and pharmacokinetic profiles[1][2][3][5][10].

Other names

(−)-2β-(3-(4-methylphenyl)isoxazol-5-yl)-3β-(4-chlorophenyl)tropane