密朗丁

生物活性靶点体外研究体内研究密朗丁试剂级价格

密朗丁

CAS号:86-34-0
英文名:PHENSUXIMIDE
中文名:密朗丁
CBNumber:CB3480203
分子式:C11H11NO2
分子量:189.21
MOL File:86-34-0.mol

密朗丁化学性质

熔点 :71-73°
沸点 :324.47°C (rough estimate)
密度 :1.1596 (rough estimate)
折射率 :1.5012 (estimate)
储存条件 :Refrigerator
溶解度 :Chloroform (Slightly), Ethyl Acetate (Slightly)
形态 :Solid
酸度系数(pKa) :-1.86±0.40(Predicted)
颜色 :White to Off-White
水溶解性 :4.2g/L(25 ºC)

安全信息

海关编码 :2925190100
毒性 :LD50 orally in mice: 960 mg/kg (Chen, Ensor)

密朗丁化学药品说明书

苯琥胺|药物应用信息

密朗丁性质、用途与生产工艺

生物活性 Phensuximide 是一种琥珀酰亚胺类抗癫痫 (antiepileptic) 和抗惊厥 (anticonvulsant) 试剂。Phensuximide 可以抑制去极化脑组织中 cyclic AMP 和 cyclic GMP 的积累。在动物模型中，Phensuximide 可用于癫痫研究的相关研究。
靶点

IC50: cyclic AMP and cyclic GMP accumulation
体外研究

Phensuximide produce depolarization-induced accumulation of cyclic GMP or cyclic AMP levels with ID ₅₀ values of 8.00 mM or 6.20 mM in incubated slices of mouse cerebral cortex.Phensuximide (0.5-2.0 mM) has the ability to competitively inhibit mephenytoin 4-hydroxylase activity in human liver microsomes, the K _i and K _m values are 559 μM and 235 μM, respectively.

体内研究

Phensuximide (intraperitoneal injection; 1.25 mmol/kg; single dose) induces mild changes in renal function, including: trace hematuria, increased proteinuria and decreased paminohippurate uptake in Sprague-Dawley rats.Phensuximide (intraperitoneal injection; 0.3 or 0.6 mmol/kg; 5-7 days) results in transient hematuria and proteinuria, but no change in the other renal function parameters studied. It is concluded that phensuximide produces mild, transient renal effects in Fischer 344 rats, and that the Fischer 344 rat is a suitable model for studying phensuximide-induced toxicity to the urinary tract.

Animal Model:	Fischer 344 rats
Dosage:	0.3 or 0.6 mmol/kg
Administration:	Intraperitoneal injection; 5-7 days
Result:	Induced urotoxicity following daily administration for 5-7 days in Fischer 344 rats.