154130-99-1

中文名称化合物 T16445

英文名称 1,2,3,6-TETRAHYDRO-5-[3-(4-METHYLPHENYL)-5-ISOXAZOLYL]-1-PROPYLPYRIDINE OXALATE

CAS 154130-99-1

分子式 C18H22N2O

分子量 282.38

MOL 文件 154130-99-1.mol

154130-99-1 结构式

基本信息物理化学性质应用领域常见问题列表

基本信息

中文别名

化合物 T16445

英文别名

PD 144418
PD 144418 OXALATE
Pyridine,1,2,3,6-tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propyl-
1,2,3,6-TETRAHYDRO-5-[3-(4-METHYLPHENYL)-5-ISOXAZOLYL]-1-PROPYLPYRIDINE OXALATE

物理化学性质

储存条件Desiccate at RT

溶解度<18.62mg/ml in DMSO

形态固体

颜色米白色

应用领域

用途1

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.

常见问题列表

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.