Reserpine
VMAT1,2 inhibitor / Indole alkaloid isolated from Rauwolfia serpentina which acts as a potent antihypertensive agent. Irreversibly inhibits both isoforms of vesicular monoamine transporter VMAT1 and 2, Ki=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
Biochemicals & reagents
50-55-5
NSC59272
Schuldiner et al. (1993), Reserpine binding to vesicular amine transporter expressed in Chinese hamster ovary fibroblasts; J. Biol. Chem., 268 29 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 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 Wang et al. (2001), Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4; Res. Toxicol., 14 1596 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
-20°C
TARGET: Monoamine transporter; Cytochrome/MDR -- PATHWAY: Intracellular transport; Posttranslational modification -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Hypertension; NeurodegenerationMood disorders; Infectious disease