GBR-12909 2HCl (67469-78-7) is a potent and selective inhibitor of dopamine reuptake (Ki = 1 nM) with greater than 100 fold selectivity over serotonin and noradrenaline.1 GBR-12909 2HCl also acts as a potent sigma receptor ligand.2 Very fast acting via i.v. administration.3
References/Citations:
1) Andersen et al. (1989), The dopamine inhibitor GBR 12909: selectivity and molecular mechanism of action; Eur. J. Pharmacol., 166 493
2) Contreras et al. (1990), GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain; Life Sci., 47 PL133
3) Yorgason et al. (2011), Low and high affinity dopamine transporter inhibitors block dopamine uptake within 5 sec of intravenous injection; Neuroscience, 182 125
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