Biochemicals & reagents
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
GBR-12909 2HCl is a potent and selective inhibitor of dopamine reuptake (Ki = 1 nM) with greater than 100 fold selectivity over serotonin and noradrenaline (1) which also acts as a potent sigma receptor ligand (2) and is a very fast acting via i.v. administration (3).