PD 144418

产品编号 T16445Cas号 154130-99-1

别名

PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.

PD 144418

产品编号 T16445Cas号 154130-99-1

规格	价格	库存
25 mg	¥ 7,850	5日内发货
50 mg	¥ 10,200	5日内发货
100 mg	¥ 15,900	5日内发货

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产品介绍

生物活性

产品描述	PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.
靶点活性	σ1 receptor:（ki）0.08 nM, σ2 receptor:1377 nM(ki)
体外活性	PD 144418 enhances the reduction in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis. PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, showing that σ1 sites may be important in the regulation of glutamine-induced actions [1].
体内活性	PD 144418 has ED50 values is 7.0 mg/kg i.p. PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) treatment antagonizes Mescaline-induced scratching at doses that did not alter spontaneous motor activity [1].