溴米索伐
中文名称:
溴米索伐
中文同义词:
α-溴代异戊酰脲;布洛母拉;溴米那;溴米索伐(JP16);溴米那 1G;溴米索伐;溴米索伐(溴米那);溴异戊脲
英文名称:
Bromisoval
英文同义词:
RARECHEM AX KI 5046;1-(2-BROMOISOVALERYL)UREA;A-(BROMOISOVALERYL)UREA;ALPHA(BROMOISOVALERYL)UREA;LABOTEST-BB LT00134620;BROMOVALERYLUREA;BROMOISOVALERYLUREA;BROMO-ISO-VALERYLUREA (ALPHA)
CAS号:
496-67-3
分子式:
C6H11BrN2O2
分子量:
223.07
EINECS号:
207-825-7
相关类别:
医药中间体;脲;医药原料;小分子抑制剂;镇静催眠药;其他原料药;医药、农药及染料中间体;API
Mol文件:
496-67-3.mol
熔点
152 °C
密度
1.6005 (rough estimate)
折射率
1.5410 (estimate)
储存条件
Sealed in dry,Room Temperature
酸度系数(pKa)
10.54±0.70(Predicted)
水溶解性
19.03g/L(temperature not stated)
Merck
14,1397
InChIKey
CMCCHHWTTBEZNM-UHFFFAOYSA-N
CAS 数据库
496-67-3(CAS DataBase Reference)
NIST化学物质信息
Bromisovalum(496-67-3)
EPA化学物质信息
Butanamide, N-(aminocarbonyl)-2-bromo-3-methyl- (496-67-3)
生物活性
Bromisoval (Bromovalerylurea, Isobromyl, Bromaral, BRN 1773255)是一种具有催眠、镇静效果的bromoureide类化合物。具有消炎活性。
体外研究
Bromisoval (BU) suppresses nitric oxide (NO) releasing and proinflammatory cytokine expression in lipopolysaccharide (LPS)-treat BV2 cells, a murine microglial cell line. Bromisoval suppresses LPS-inducing phosphorylation of signal transducer and activator of transcription 1 (STAT1) and expression of interferon regulatory factor 1 (IRF1). The Janus kinase 1 (JAK1) inhibitor filgotinib suppresses the NO release much more weakly than that of Bromisoval, although filgotinib almost completely prevents LPS-inducing STAT1 phosphorylation. Knockdown of JAK1, STAT1, or IRF1 does not affect the suppressive effects of Bromisoval on LPS-inducing NO. A combination of Bromisoval and filgotinib synergistically suppress the NO releasing. The mitochondrial complex I inhibitor rotenone, which does not prevent STAT1 phosphorylation or IRF1 expression, suppresses proinflammatory mediator expression less significantly than Bromisoval. Bromisoval and rotenone reduce intracellular ATP (iATP) levels to a similar extent. A combination of rotenone and filgotinib suppress NO release in LPS-treated BV2 cells as strongly as Bromisoval.
体内研究
Bromisoval (Bromvaletone) and carbromal are the most potent central depressants within each series. Depressant activities (ISD 50 values) and acute toxicities (LD 50 values) in male mice after intraperitoneal injection of Bromisoval are 0.35 (0.30-0.39) and 3.25 (2.89-3.62) mmol/kg, respectively.
化学性质
白色针状结晶。熔点147-149℃，溶于醇、醚、丙酮，不溶于冷水。易溶于热水。无臭，味微苦。
用途
该品具有镇静和轻度催眠作用，服后5分钟即显效，作用时间持续4h，无习惯性，可制成粉、片剂及注射剂。
生产方法
以异戊醇为原料，先氧化生成异戊酸，再溴化生成α-溴代异戊酰溴，最后与尿素缩合生成溴异戊脲。
类别
有毒物质
毒性分级
中毒
急性毒性
口服-大鼠 LD50: 1000 毫克/公斤; 口服-小鼠 LD50: 2000 毫克/公斤
可燃性危险特性
热分解排出有毒溴化物和氮氧化物烟雾
储运特性
库房通风低温干燥
灭火剂
水,干粉、干砂、二氧化碳、泡沫、1211灭火剂
RTECS号
YS3150000
毒性
LD50 in male mice (mmoles/kg): 3.25 i.p. (Mrongovius)
