Flumazenil
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Flumazenil 속성
- 녹는점
- 201-203°C
- 끓는 점
- 528.0±50.0 °C(Predicted)
- 밀도
- 1.39±0.1 g/cm3(Predicted)
- 저장 조건
- Sealed in dry,2-8°C
- 용해도
- DMSO에서 25mM까지 용해 가능
- 산도 계수 (pKa)
- 0.86±0.20(Predicted)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 하얀색
- 수용성
- 128mg/L
- Merck
- 14,4135
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
- CAS 데이터베이스
- 78755-81-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xi | ||
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위험 카페고리 넘버 | 36/37/38 | ||
안전지침서 | 26-27-36/37/39 | ||
WGK 독일 | 2 | ||
RTECS 번호 | NI2922170 | ||
HS 번호 | 2933997500 | ||
독성 | LD50 in mice, rats (mg/kg): 4000, 1360 i.p.; 4300, 6000 orally (Hunkeler) |
그림문자(GHS): | |||||||||||||||
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신호 어: | Warning | ||||||||||||||
유해·위험 문구: |
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예방조치문구: |
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Flumazenil C화학적 특성, 용도, 생산
개요
Flumazenil is a benzodiazepine antagonist useful as a fast-acting antidote in the treatment of benzodiazepine intoxication, and in reversing the central sedative effects of benzodiazepines during anesthesia.화학적 성질
Flumazenil is a white to off-white crystalline compound with an octanol:buffer partition coefficient of 14 to 1 at pH 7.4. It is insoluble in water but slightly soluble in acidic aqueous solutions.용도
Flumazenil is an imidazodiazepine which selectively blocks the central effects of classic benzodiazepines. It is used as benzodiazepine antagonist sedation reversal drug.정의
ChEBI: Flumazenil is an organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. It has a role as a GABA antagonist and an antidote to benzodiazepine poisoning. It is an ethyl ester, an organofluorine compound and an imidazobenzodiazepine.제조 방법
The Synthesis of FlumazenilStarting with 4-fluoroaniline (15) the isatin 17 is synthesized via the Sandmeyer synthesis; isatin is then oxidized with peracetic acid to the isatoic anhydride 18. Reaction with sarcosine in DMF leads to the benzodiazepine-2,5-dione 19. This is converted to the iminochloride by reaction with POCI3 . In the key step the imidazoester is built up by reaction with deprotonated ethyl isocyanoacetate [8]. Since ethyl isocyanoacetate is not very stable, an alternative synthesis based on the synthesis of midazolam was developed for large scale-production. Tnthis synthesis diethylmalonate is used. The diester 21 is then transformed to the monoester 22 hy deethoxycarbonylation. Nitrosation and catalytic reduction lead to the amino compound 23. The final carbon atom is introduced by reaction with the orthoester.
생물학적 활성
Flumazenil is a GABAA receptor antagonist with non-selective for α 1, α 2, α 3 or α 5 (IC50 = 2 nM in a radioligand binding assay using rat cortical synaptosomes). Flumazenil also acts as a partial agonist of GABAA receptors, decreasing the amplitude of electrically stimulated population spikes in rat hippocampal CA1 pyramidal neurons. It increases the number of entries into the open arms of the elevated plus maze in high-anxiety BALB/c, but not C57BL/6, mice when administered at doses ranging from 0.1 to 1,000 μg/kg. Flumazenil (5 and 10 mg/kg) prevents a reduction in burying behavior induced by the GABAA receptor positive allosteric modulator allopregnanolone in ovariectomized rats when administered at doses of 5 and 10 mg/kg. Formulations containing flumazenil have been used to reverse sedation induced by benzodiazepines and in the treatment of benzodiazepine overdose or withdrawal.Pharmacokinetics
Flumazenil is a competitive antagonist at the GA BAA benzodiazepine binding site for all other ligands. I t rapidly reverses the CN S and dangerous physiological effects of benzodiazepines following iatrogenic overdose or deliberate self-harm. I t has no effect on benzodiazepine metabolism. Flumazenil is rapidly cleared from plasma and metabolised by the liver and has a very short elimination half-life (<1h). Its duration of action depends on the dose administered and the duration of action of the drug to be antagonised; repeated administration or infusions may be necessary.Mode of action
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. In animal experiments the effects of compounds showing no affinity for the benzodiazepine receptor, e.g. barbiturates, ethanol, meprobamate, GABA mimetics, adenosine receptor agonists and other agents were not affected by flumazenil, but those of nonbenzodiazepine agonists of benzodiazepine receptors, such as cyclopyrrolones (e.g. zopiclone) and triazolopyridazines were blocked.참고 문헌
Flumazenil in benzodiazepine overdoseDOI:10.1503/cmaj.160357
Pharmacological uses of flumazenil in benzodiazepine use disorders: a systematic review of limited data
DOI:10.1177/0269881120981390
Flumazenil 준비 용품 및 원자재
원자재
준비 용품
Flumazenil 공급 업체
글로벌( 376)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
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Hebei Yanxi Chemical Co., Ltd. | +8617531190177 |
peter@yan-xi.com | China | 5993 | 58 |
Dorne Chemical Technology co. LTD | +86-13583358881 +86-18560316533 |
Ethan@dornechem.com | China | 294 | 58 |
LY Global chemicals co.,ltd . | +8618939937369 |
info@lychems.cn | China | 969 | 58 |
Xiamen Wonderful Bio Technology Co., Ltd. | +8613043004613 |
Sara@xmwonderfulbio.com | China | 305 | 58 |
Jinan Million Pharmaceutical Co., Ltd | +86-531-68659554 +8613031714605 |
info@millionpharm.com | China | 153 | 58 |
Nantong Guangyuan Chemicl Co,Ltd | +undefined17712220823 |
admin@guyunchem.com | China | 616 | 58 |
Shandong Hanjiang Chemical Co., Ltd | +86-0533-2066820 +8618369939125 |
hanson@sdhanjiang.com | China | 1527 | 58 |
Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 524 | 58 |
Shanghai Aosiris new Material Technology Co., LTD | 86-15139564871 +8615139564871 |
wrjmoon2000@163.com | China | 354 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21695 | 55 |
Flumazenil 관련 검색:
메틸 바이올렛 (2B) 디하이드로미르세놀 메틸알콜 포름산에틸 1-메틸이미다졸 메틸파라벤 이염화파라콰트 아세토나이트릴 아크릴산메틸 쿠레톡심메틸 우레탄 오소포름산에틸 클로로포름산에틸
4H-Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylicacid, 5,6-dihydro-8-hydroxy-5-methyl-6-oxo-, ethyl ester
7-Fluoro-3,4-dihydro-4-methyl-1H-1,4-benzodiazepine-2,5-dione
N,N-Dimethyformamide diethy acetal
Ro 15-3505
Ro 14-7437