3-[2-[4-(3,4-dimethylphenyl)-1-piperazinyl]ethyl]-2,3-dihydro-1H-isoindol-1-onedihydrochloride

Names

[ Name ]:
3-[2-[4-(3,4-dimethylphenyl)-1-piperazinyl]ethyl]-2,3-dihydro-1H-isoindol-1-onedihydrochloride

Biological Activity

[Description]:

PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 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 can be used for glioblastoma (GBM) research[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

D4 Receptor:8.8 nM (Ki)

D2 Receptor:1842 nM (Ki)

D3 Receptor:2682 nM (Ki)

[In Vitro]

PD 168568 对胶质母细胞瘤神经干细胞 (GNS) 表现出选择性抑制，IC50 为 25-50 µM[1]。

[In Vivo]

PD 168568 (3 mg/kg，口服) 可抑制大鼠 amphetamine 刺激的运动活动[3]。 Animal Model: Rat[1] Dosage: 3 mg/kg Administration: Oral administration Result: Inhibited amphetamine (0.5 mg/kg, i.p.) stimulated locomotor activity.

[References]

[1]. Dolma S, et al. Inhibition of Dopamine Receptor D4 Impedes Autophagic Flux, Proliferation, and Survival of Glioblastoma Stem Cells. Cancer Cell. 2016 Jun 13;29(6):859-873.

[2]. Lindsley CW, et al. Return of D4 Dopamine Receptor Antagonists in Drug Discovery. J Med Chem. 2017 Sep 14;60(17):7233-7243.

[3]. Belliotti TR, et al. Isoindolinone enantiomers having affinity for the dopamine D4 receptor. Bioorg Med Chem Lett. 1998 Jun 16;8(12):1499-502.