A potent D3 receptor agonist
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(+)-PD 128907 is a potent agonist of the dopamine 3 (D3) receptor (Ki = 1 nM).1,2 It shows selectivity for D3 over D2 and D4 receptors (Kis = 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)
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