PD 144418 oxalate 是一种高亲和力，强效和选择性的 sigma 1 受体 (σ1 receptor) 配体 (对 σ1 和 σ2 的 Ki 值分别为 0.08 nM 和 1377 nM)，对其他受体，离子通道和酶没有任何显着的亲和力。PD 144418 oxalate 具有潜在的抗精神病活性。

PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand ( K i values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.

In vitro, PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, suggesting that σ1 sites may be important in the regulation of glutamine-induced actions. PD 144418 potentiates the decrease in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis [1] .

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, with PD 144418 showing ED 50 values of 7.0 mg/kg i.p. [1] . Animal Model: Male CD-1 mice induced with Mescaline [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; once Result: Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity.

1794760-28-3

C20H24N2O5

372.421

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years