Although best known as a selective estrogen receptor modulator (SERM), tamoxifen is a drug with a wide range of activities. Tamoxifen has demonstrated some efficacy has a therapeutic for bipolar mania and is believed to exert these effects through inhibition of protein kinase C (PKC). As the symptoms of amphetamine treatment in rodents are believed to mimic the symptoms of a manic episode, many of the preclinical studies for this indication have demonstrated that tamoxifen inhibits amphetamine action. The amphetamine-induced increase in extracellular dopamine which gives rise to the ‘manic’ effects is due to interaction of amphetamine with the dopamine transporter. We and others have demonstrated that PKC reduces amphetamine-induced reverse transport through the dopamine transporter. In this review, we will outline the actions of tamoxifen as a SERM and further detail another known action of tamoxifen—inhibition of PKC. We will summarize the literature showing how tamoxifen affects amphetamine action. Finally, we will present our hypothesis that tamoxifen, or an analog, could be used therapeutically to reduce amphetamine abuse in addition to treating mania.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.