Product Introduction
Bioactivity


英文名: PD 144418 oxalate

描述: PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand, displaying a Ki value of 0.08 nM for σ1 and 1377 nM for σ2. It exhibits negligible affinity for other receptors, ion channels, and enzymes. Additionally, PD 144418 oxalate demonstrates potential antipsychotic activity.

体外活性: 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] .

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 10 mg/mL (26.85 mM)


关键字: PD 144418 oxalate | PD 144418 Oxalate | PD-144418 Oxalate | PD144418 Oxalate

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相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Bioactive Compound Library