化合物 T16445

生物活性靶点体外研究体内研究化合物 T16445 试剂级价格

化合物 T16445

CAS号:154130-99-1
英文名:1,2,3,6-TETRAHYDRO-5-[3-(4-METHYLPHENYL)-5-ISOXAZOLYL]-1-PROPYLPYRIDINE OXALATE
中文名:化合物 T16445
CBNumber:CB02446510
分子式:C18H22N2O
分子量:282.38
MOL File:154130-99-1.mol

化合物 T16445化学性质

沸点 :453.2±45.0 °C(Predicted)
密度 :1.067±0.06 g/cm3(Predicted)
储存条件 :Desiccate at RT
溶解度 :<18.62mg/ml in DMSO
形态 :solid
酸度系数(pKa) :8.10±0.40(Predicted)
颜色 :Off-white

化合物 T16445性质、用途与生产工艺

生物活性 PD 144418 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 具有潜在的抗精神病活性。
靶点

Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
体外研究

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.

体内研究

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..

Animal Model:	Male CD-1 mice induced with Mescaline
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection
Result:	Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity.

用途 PD 144418 is high affinity, selective 蟽1 ligand (Ki values are 0.08 and 1377 nM for 蟽1 and 蟽2 respectively). PD 144418 displays no significant activity at a wide range of other receptors, ion channels and enzymes. PD 144418 antagonizes mescaline-induced scratching in mice following i.p. administration.