Bupropion hydrochloride is a dual effective inhibitor of norepinephrine and dopamine neurotransmitter with the IC50 values of 6.5 ± 0.6μM and 3.4 ± 0.4 μM, respectively [1].
Bupropion hydrochloride is an aminoketone used as non-nicotine aid to smoking cessation. Bupropion hydrochloride is also a typical antidepressant agent that interferes with norepinephrine, serotonin, and dopamine reuptake [2]. In addition, Bupropion hydrochloride has been reported to reduce the expression of tyrosine hydroxylase, a rate-limiting enzyme in dopamine biosynthesis [3]. In vitro, it has been shown that Bupropion hydrochloride can decrease cell viability significantly in SH-SY5Y cells. Furthermore, Bupropion hydrochloride has been revealed to selectively activate an ER stress pathway. Apart from these, the result has also shown that Bupropion hydrochloride can induce cell death as a result of caspase 3 activation through the JNK and ER stress [2].
References:
[1] Dr. R. M. Ferris*, H. L. White,B. R. Cooper, R. A. Maxwell, F. L. M. Tang,O. J. Beaman and A. Russell .Some neurochemical properties of a new antidepressant, bupropion hydrochloride (Wellbutrin™). Drug Development Research Volume 1, Issue 1, pages 21–35, 1981
[2] Jang EH1, Park CS, Kang JH. Bupropion, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells. Toxicology. 2011 Jul 11;285(1-2):1-7.
[3] Nestler, E.J., McMahon, A., Sabban, E.L., Tallman, J.F., Duman, R.S., 1990. Chronicantidepressant administration decreases the expression of tyrosine hydroxylase
in the rat locus coeruleus. Proc. Natl. Acad. Sci. U. S. A. 87, 7522–7526.