(+)-PD 128907 hydrochloride

(+)-PD 128907 is a potent agonist of the dopamine 3 (D₃) receptor (K_i = 1 nM).^1,2 It shows selectivity for D₃ over D₂ and D₄ receptors (K_is = 1.2 and 7 ?M, respectively).¹ Low doses of (+)-PD 128907 (13 ?g/kg, s.c.) reduce spontaneous locomotor activity in rats.³ It blocks stereotypy induced by the NMDA receptor antagonist (+)-MK-801 in mice.⁴ (+)-PD 128907 is used in animal models to study the role of the D₃ receptor in nervous system disorders, such as schizophrenia, Parkinson’s disease, and depression.^5,6

1.Akunne, H.C., Towers, P., Ellis, G.J., et al.Characterization of binding of [3H]PD 128907, a selective dopamine D3 receptor agonist ligand, to CHO-K1 cellsLife Sci.57(15)1401-1410(1995) 2.Pugsley, T.A., Davis, M.D., Akunne, H.C., et al.Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907J. Pharmacol. Exp. Ther.275(3)1355-1366(1995) 3.Bristow, L.J., Cook, G.P., Gay, J.C., et al.The behavioural and neurochemical profile of the putative dopamine D3 receptor agonist, (+)-PD 128907, in the ratNeuropharmacology35(3)285-294(1996) 4.Witkin, J., Gasior, M., Acri, J., et al.Atypical antipsychotic-like effects of the dopamine D3 receptor agonist, (+)-PD 128,907Eur. J. Pharmacol.347(2-3)R1-R3(1998) 5.Carcinella, S., Drui, G., Boulet, S., et al.Implication of dopamine D3 receptor activation in the reversion of Parkinson's disease-related motivational deficitsTransl. Psychiatry4(6)e401(2014) 6.Gil-Mast, S., Kortagere, S., Kota, K., et al.An amino acid residue in the second extracellular loop determines the agonist-dependent tolerance property of the human D3 dopamine receptorACS Chem Neurosci.4(6)940-951(2013)