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PD 168568 dihydrochloride is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 dihydrochloride contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 dihydrochloride can be used for glioblastoma (GBM) research[1][2]. | [Biological Activity]
PD 168568 is a dopamine D4 receptor antagonist (Ki = 8.8 nM).1 It is selective for dopamine D4 over D2 receptors (Ki = 1,842 nM). PD 168568 (3 mg/kg) reverses amphetamine-induced hyperlocomotion in rats. It also inhibits the growth of glioblastoma neural stem cells when used at concentrations of 25 and 50 μM.2 | [in vivo]
PD 168568 dihydrochloride (3 mg/kg, Oral) has ability to inhibit amphetamine-stimulated locomotor activity in the rat[3]. | Animal Model: | Rat[1] | | Dosage: | 3 mg/kg | | Administration: | Oral administration | | Result: | Inhibit amphetamine (0.5 mg/kg, i.p.) stimulated locomotor activity. |
| [IC 50]
D4 Receptor: 8.8 nM (Ki); D2 Receptor: 1842 nM (Ki); D3 Receptor: 2682 nM (Ki) | [storage]
Desiccate at RT | [References]
1.Belliotti, T.R., Brink, W.A., Kesten, S.R., et al.Isoindolinone enantiomers having affinity for the dopamine D4 receptorBioorg. Med. Chem. Lett.8(12)1499-1502(1998)
2.Dolma, S., Selvadurai, H.J., Lan, X., et al.Inhibition of dopamine receptor D4 impedes autophagic flux, proliferation, and survival of glioblastoma stem cellsCancer Cell29(6)859-873(2016)
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