154130-99-1
中文名稱
化合物 T16445
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16445 英文別名
PD 144418PD 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
應(yīng)用領(lǐng)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.常見問題列表
生物活性
PD 144418 是一種高親和力，強(qiáng)效和選擇性的 sigma 1 受體 (σ1 receptor) 配體 (對 σ1 和 σ2 的 Ki 值分別為 0.08 nM 和 1377 nM)，對其他受體，離子通道和酶沒有任何顯著的親和力。PD 144418 具有潛在的抗精神病活性。靶點(diǎn)
Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
體外研究
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.
體內(nèi)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. |