GR103691

GR103691 is a dopamine D₃ receptor antagonist (K_i = 0.32 nM).¹ It is selective for dopamine D₃ receptors over dopamine D₁, D₂, and D₄ receptors (K_is = 398.11, 39.81, and 81 nM, respectively) and over the serotonin (5-HT) receptor subtype 5-HT_1A, α₁-adrenergic receptors, and M₁ muscarinic receptors (K_is = 3.16, 12.59, and >1,000 nM, respectively).^1,2 GR103691 inhibits increases in locomotor activity induced by infusion of the GABA_A and GABA_C receptor agonist muscimol (Item No. 13667) into the rat ventral tegmental area (VTA; ED₅₀ = 0.3 mg/kg) but not infusion into the substantia nigra zona reticulata (SNr; ED₅₀ = >10 mg/kg).¹ It increases the time rats spend in the light area of the light-dark exploration test and the open areas of the elevated plus maze without affecting locomotor activity, indicating anxiolytic-like behavior, when injected into the basolateral amygdala (BLA) at a dose of 5 pmol/animal.³

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1. Murray, P.J., Harrison, L.A., Johnson, M.R., et al. A novel series of arylpiperazines with high affinity and selectivity for the dopamine D₃ receptor. Bioor. Med. Chem. Lett. 5(3), 219-222 (1995).

2. Audinot, V., Newman-Tancredi, A., Gobert, A., et al. A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D₃ receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. J. Pharmacol. Exp. Ther. 287(1), 187-197 (1998).

3. Diaz, M.R., Chappell, A.M., Christian, D.T., et al. Dopamine D₃-like receptors modulate anxiety-like behavior and regulate GABAergic transmission in the rat lateral/basolateral amygdala. Neuropsychopharmacology 36(5), 1090-1103 (2011).