Reserpine | VMAT1,2 inhibitor

Reserpine (50-55-5) is an indole alkaloid isolated from Rauwolfia serpentina which acts as a potent antihypertensive agent. Irreversibly inhibits both isoforms of vesicular monoamine transporter VMAT1 and 2, K_i=34 and 12 nM, respectively.^1,2 May be used to pharmacologically deplete monoamines in various animal models.³  Inhibits the multidrug resistance protein P-glycoprotein, IC₅₀=0.5 mM.³ Reserpine-induced hypokinesia is considered a useful animal model of Parkinson’s disease.⁵

References:

1. Schuldiner et al. (1993), Reserpine binding to vesicular amine transporter expressed in Chinese hamster ovary fibroblasts; J. Biol. Chem., 268 29
2. Erickson et al. (1996), Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter; Proc. Natl. Acad. Sci. USA, 93 5166
3. Antkiewicz et al. (2014), Antidepressant-like effect of tetrahydroisoquinoline amines in the animal model of depressive disorder induced by repeated administration of a low dose of reserpine: behavioral and neurochemical studies in the rat; Neurotox. Res., 26 85
4. Wang et al. (2001), Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4; Res. Toxicol., 14 1596
5. Duty et al. (2011), Animal models of Parkinson’s disease: a source of novel treatments and clues to the cause of the disease; Oncotarget, 164 1357