CN102028692B - 酮色林的应用 - Google Patents

酮色林的应用 Download PDF

Info

Publication number
CN102028692B
CN102028692B CN2010105688081A CN201010568808A CN102028692B CN 102028692 B CN102028692 B CN 102028692B CN 2010105688081 A CN2010105688081 A CN 2010105688081A CN 201010568808 A CN201010568808 A CN 201010568808A CN 102028692 B CN102028692 B CN 102028692B
Authority
CN
China
Prior art keywords
ketanserin
application
medicine
endotoxin shock
health
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN2010105688081A
Other languages
English (en)
Other versions
CN102028692A (zh
Inventor
苏定冯
刘冲
张谷芳
沈甫明
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Second Military Medical University SMMU
Original Assignee
Second Military Medical University SMMU
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Second Military Medical University SMMU filed Critical Second Military Medical University SMMU
Priority to CN2010105688081A priority Critical patent/CN102028692B/zh
Publication of CN102028692A publication Critical patent/CN102028692A/zh
Application granted granted Critical
Publication of CN102028692B publication Critical patent/CN102028692B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Landscapes

  • Medicines Containing Plant Substances (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明公开了酮色林在制备预防或治疗内毒素休克的药物中的应用，从而拓宽了其应用范围，也为内毒素休克的预防和治疗提供了新途径。

Description

酮色林的应用
技术领域
本发明涉及酮色林在医药领域中的新应用。
背景技术
酮色林(ketanserin)，是近年研制的一种相对特异性的五羟色胺2A受体拮抗药，化学名为3-[2-[4-(4-氟苯甲酰)-1-哌啶基]乙基]-2，4[1H，3H]-喹唑二酮，结构式如式I所示：
Figure BSA00000369265700011
式I
目前，在临床上酮色林主要用于治疗高血压，其作用机制主要与其5HT-2A受体阻断作用和肾上腺α1受体阻断作用有关(Ketanserin in parenteraltreatment of acute essential hypertension：a dose-response curve.Milei J，LemnsJ，Schiavone M，et al.J Cardiovasc Pharmacol 1987；10(suppl 3)：96-100)。然而目前，尚未有报道将酮色林用于内毒素休克的防治。
发明内容
本发明所要解决的技术问题是提供酮色林在医药领域中的一种新应用，从而拓宽其应用范围。
本发明涉及酮色林在制备预防或治疗内毒素休克的药物中的应用。经实验发现，酮色林可显著提高内毒素休克生存率，并可改善身体颤抖、身体冰冷、活动减少、眼角出现分泌物和腹泻等症状。因此，本发明的药物更具体的可为提高内毒素休克生存率，和/或改善身体颤抖、身体冰冷、活动减少、眼角出现分泌物和腹泻的症状中的一种或多种的药物。
本发明中，所述的药物中所含酮色林的用量为治疗有效量以上，具体可根据情况选择，一般为0.033mg/kg-1.1mg/kg。所述的药物可以仅含酮色林作为唯一活性成分，也可还含有除酮色林以外的其它活性成分。所述的其它活性成分为对酮色林的防治内毒素休克药效作用没有不良影响可联合使用的活性成分，如其他可防治内毒素休克的药物活性成分。
本发明所用试剂和原料均市售可得。
本发明的积极进步效果在于：本发明提供了酮色林在制备预防或治疗内毒素休克的药物中的应用，拓宽了其应用范围，也为内毒素休克的预防和治疗提供了新途径。
附图说明
图1为实施例1中各实验组酮色林72小时生存曲线图。
具体实施方式
下面通过实施例的方式进一步说明本发明，但并不因此将本发明限制在所述的实施例范围之中。
实施例酮色林对内毒素休克的作用
小鼠来源及品种：昆明种小鼠，来源于上海斯莱克实验动物有限公司。
内毒素休克模型的建立：参考文献(Borovikova LV，Ivanova S，Zhang M，et al：Vagus nerve stimulation attenuates the systemic inflammatory response toendotoxin.Nature 2000；405：458-462)的方法，以腹腔注射内毒素(30mg/kg，i.p.)诱导小鼠内毒素休克，建立模型。
给药：将小鼠随机分5组，每组21只，分别为不注射酮色林的对照组，以及用不同剂量的酮色林腹腔注射的实验组。观察内毒素休克小鼠72小时生存率，结果如表1所示，生存曲线如图1。
表1各实验组72小时生存情况(n＝21)
Figure BSA00000369265700031
由表1和图1可见，不同剂量的酮色林对内毒素休克小鼠的生存率均有改善作用，并且酮色林治疗剂量为10mg/kg时效果极佳。
此外，在实验过程中观察到对照组的小鼠立毛、颤抖、全身冰冷、活动减少，挤成一团；眼角出现较粘稠的分泌物，严重者可使上下眼睑粘连；腹泻，粪便稀薄。而给予酮色林治疗组的小鼠经过一段时间后活动明显较对照组活跃，眼角分泌物减少，腹泻状况减轻，并且随着剂量增大小鼠的状态越好，有明显的进食及饮水。而10mg/kg治疗剂量组的小鼠无明显的活动减少情况，状态良好。
上述实验结果证明，酮色林具有有效的防治内毒素抗休克的作用。

Claims (3)

1.酮色林在制备治疗内毒素休克的药物中的应用。
2.如权利要求1所述的应用，其特征在于：所述的药物为提高内毒素休克生存率的药物。
3.如权利要求1或2所述的应用，其特征在于：所述的药物为改善身体颤抖、身体冰冷、活动减少、眼角出现分泌物和腹泻的症状中的一种或多种的药物。
CN2010105688081A 2010-12-01 2010-12-01 酮色林的应用 Expired - Fee Related CN102028692B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN2010105688081A CN102028692B (zh) 2010-12-01 2010-12-01 酮色林的应用

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2010105688081A CN102028692B (zh) 2010-12-01 2010-12-01 酮色林的应用

Publications (2)

Publication Number Publication Date
CN102028692A CN102028692A (zh) 2011-04-27
CN102028692B true CN102028692B (zh) 2012-08-22

Family

ID=43882502

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010105688081A Expired - Fee Related CN102028692B (zh) 2010-12-01 2010-12-01 酮色林的应用

Country Status (1)

Country Link
CN (1) CN102028692B (zh)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101394854A (zh) * 2006-03-09 2009-03-25 皮埃尔法布雷医药公司 抗组胺剂在预防或早期治疗炎症综合征，特别是由披膜病毒类引起的炎症综合征中的新用途

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101394854A (zh) * 2006-03-09 2009-03-25 皮埃尔法布雷医药公司 抗组胺剂在预防或早期治疗炎症综合征，特别是由披膜病毒类引起的炎症综合征中的新用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
H.M.OUDEMANS-VAN STRAATEN,et al.Endotoxaemia and postoperative hypermetabolism in coronary artery bypass surgery: the role of ketanserin.《British Journal of Anaesthesia》.1996,(第77期),473-479. *

Also Published As

Publication number Publication date
CN102028692A (zh) 2011-04-27

Similar Documents

Publication Publication Date Title
IL184932A0 (en) Glucagon receptor antagonists, preperation and therapeutic uses
EA200970706A1 (ru) Новые фармацевтические композиции
SI1957484T1 (sl) Antagonisti glukagonskega receptorja, priprava in terapevtske uporabe
CA2939464A1 (en) Use of anti-ccr5 antibodies in graft versus host disease
BRPI0406749A (pt) Métodos relacionados ao tratamento de distúrbios fincionais do intestino e composição farmacêutica
UA99914C2 (ru) Способ применения антагонистов вазопресина со средствами антрациклиновой химиотерапии для снижения кардиотоксичности
US20210008039A1 (en) Promoting sleep using at1 receptor blockers
MX2011012310A (es) Tratamiento de insuficiencia cardiaca con fracción de eyeccion normal (icfen).
TW201817425A (zh) 用於治療非酒精性脂肪肝疾病之醫藥組成物及方法
WO2006133286A3 (en) Treatment of tnf antagonist-resistant inflammatory disorders and related methods
CN102028692B (zh) 酮色林的应用
JP2020510011A5 (zh)
WO2007124045A3 (en) Piperidine and piperazine compounds for use in the treatment of obesity, eating disorders and sexual dysfunction by potentiation of mc4 receptor activity
WO2010060742A1 (en) Combination of bifeprunox and an antipsychotic drug with d2/5-ht2a receptor antagonistic activity for treating cns disorders
Martin et al. Anticipating and managing opioid side effects in the elderly
Xiao et al. Phase II study on EANI combined with hydrochloride palonosetron for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy
EP3534902B1 (en) Combinations of fgfr4 inhibitors and bile acid sequestrants
HK1072012A1 (en) 5-ht4 receptor antagonists for the treatment of heart failure
RU2020120236A (ru) Способы применения феноксипропиламиновых соединений для лечения депрессии
Zalaudek et al. Amitriptyline as therapeutic and not symptomatic approach in the treatment of prurigo nodularis
MX2012003310A (es) Uso del antagonista del receptor opiaceo para los trastornos del tracto gastrointestinal.
CN105816457A (zh) 含有盐酸帕罗西汀的药物组合物及其用途
Luthra et al. Ketamine: a neuroanesthesiologist's friend or foe?
CN101433542A (zh) 一种治疗人急性放射性食管炎的内服药物
RU2009126159A (ru) Травяная композиция и способ ее получения

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20120822

Termination date: 20191201

CF01 Termination of patent right due to non-payment of annual fee