CE-158


CE-158 is an atypical dopamine reuptake inhibitor that was derived from modafinil. It is often but not always referred to as the enantiopure enantiomer -CE-158 instead.
CE-158 is a highly selective DRI with much greater potency than modafinil. As -CE-158, its inhibitory potencies at the monoamine transporters are 227nM at the dopamine transporter, 11,970nM at the norepinephrine transporter , and inactive at the serotonin transporter.
The drug shows pro-motivational effects in animals and reverses tetrabenazine-induced motivational deficits. It increases dopamine levels in the nucleus accumbens, blocks amphetamine-induced dopamine release in vitro, shows no effect on locomotor activity with acute or repeated administration except at a high dose, and enhances learning in animals.
CE-158 was first described by 2020. It is closely related to CE-123, an earlier modafinil analogue. CE-158 and related agents are of interest in the potential treatment of motivational disorders, psychostimulant use disorder, and Alzheimer's disease.