83846-83-7
83846-83-7 結(jié)構(gòu)式
基本信息
酮舍林酒石酸鹽
3-[2-[4-(4-FLUOROBENZOYL)-1-PIPERDINYL]ETHYL]-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE
3-[2-[4-(4-FLUOROBENZOYL)-1-PIPERIDINYL]ETHYL]-2,4[1H,3H]-QUINAZOLINEDIONE TARTRATE
3-(2-[4-(4-FLUOROBENZOYL)-1-PIPERIDINYL]ETHYL)-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE SALT
3-[2-(4-FLUOROBENZOYL)-1-PIPERDINYL]-ETHYL]-2,4(1H,3H)-QUINAZOLINEDIONE TARTRATE
KETANSERIN TARTRATE
KETANSERIN TARTRATE SALT
R 41468
R 41468 TARTRATE SALT
3-(2-(4-(p-fluorobenzoyl)-1-piperidinyl)ethyl)-2,4(1h,3h)-quinazolinedionel
4(1h,3h)-quinazolinedione,3-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-(
kjk-945
r-(r*,r*))-2,3-dihydroxybutanedioate(1:1)
3-[2-[4-(4-fluorobenzoyl)piperidino]ethyl]quinazoline-2,4(1H,3H)-dione [R-(R*,R*)]-tartrate
KETANSERIN TARTRATE (R 41468) (SELECTIVE 5-HT2/5-HT1C SEROTONI
Ketanserinetartrate
R 41468 (+)-tartrate salt, 3-(2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl)-2,4(1H,3H)-quinazolinedione (+)-tartrate salt
3-[2-[4-(4-Fluorobenzoyl)piperidino]ethyl]-2,4-(1H,3H)-quinazolinedione tartrate
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
雖然酮色林是以抗高血壓藥問(wèn)世，而臨床對(duì)其治療原發(fā)性高血壓的報(bào)道卻很少，而對(duì)酮色林用于妊娠高血壓綜合癥、先兆子癇及HELLP綜合征的預(yù)防和治療的臨床觀察報(bào)道較多。多數(shù)報(bào)道認(rèn)為酮色林對(duì)妊娠高血壓綜合征、先兆子癇及HELLP綜合征有一定的預(yù)防和治療作用。酮色林組顯著降低舒張壓，收縮壓雖亦下降但無(wú)顯著影響，而且這種差異從給藥第7天即可監(jiān)測(cè)到。酮色林對(duì)先兆子癇的療效優(yōu)于氫氯噻嗪。另有臨床病例觀察2例，均為高齡產(chǎn)婦，在初次懷孕時(shí)未使用酮色林均出現(xiàn)溶血、血小板減少、子癇等高危因素，再次妊娠時(shí)給予了口服酮色林和阿司匹林抗凝藥則平安度過(guò)孕期。這2例高危孕婦的自身對(duì)照也提示酮色林對(duì)妊娠高血壓及先兆子癇有預(yù)防作用。酮色林在預(yù)防和治療妊娠高血壓的同時(shí)是否對(duì)胎兒的發(fā)育有不利影響也是人們所關(guān)心的。有研究表明酮色林的胎盤(pán)屏障通過(guò)率較高；分娩后酮色林及其代謝產(chǎn)物在新生兒體內(nèi)需13.8 ～ 34.4h消除。
2.冠狀動(dòng)脈球囊血管成形術(shù)中的應(yīng)用
冠狀動(dòng)脈球囊血管成形術(shù)是治療由于管狀動(dòng)脈狹窄引起的心肌缺血的常用外科方法。但在冠狀動(dòng)脈球囊血管成形術(shù)中由于狹窄的冠狀動(dòng)脈放入冠脈支架后，有時(shí)立即會(huì)出現(xiàn)原狹窄部位遠(yuǎn)端的冠脈收縮，引起心肌缺血，有推測(cè)認(rèn)為這種冠狀動(dòng)脈收縮可能是5-HT引起的。因而對(duì)44名單一血管堵塞引起的穩(wěn)定心絞痛的患者的臨床實(shí)驗(yàn)觀察表明，在冠狀動(dòng)脈球囊血管成形術(shù)術(shù)中冠狀動(dòng)脈內(nèi)注入酮色林（1.5mg溶于10ml 0.9%氯化鈉溶液中，3min注射完）可顯著增加冠狀動(dòng)脈側(cè)枝的血流量減少心肌缺血的發(fā)生。筆者認(rèn)為這一實(shí)驗(yàn)結(jié)果不僅說(shuō)明酮色林在冠狀動(dòng)脈球囊血管成形術(shù)中有預(yù)防心肌缺血的作用，也提示了酮色林在治療心肌缺血方面可能有新的應(yīng)用。
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5-HT 2 Receptor
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hERG current 0.11 μM (IC 50 ) |
Ketanserin at 0.3 μM inhibits the voltage-dependent step current (I hERG.step ) and tail current (I hERG.tail ) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC 50 =22.0±7 μM), Ketanserin (IC 50 =152±23 μM). Ketanserin (50-350 μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC 50 value of Cyproheptadine is 22±7 μM and Ketanserin is 152±23 μM. Ketanserin inhibits platelet aggregation with an IC 50 of 240 (169-339) nM.
Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT 2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions.