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Merck
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重要文件

SML3467

Sigma-Aldrich

Remimazolam

≥98% (HPLC)

同義詞:

(S)-Methyl 3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate, CNS 7054 methyl ester, CNS 7056, CNS-7054 methyl ester, CNS-7056, CNS7054 methyl ester, CNS7056, Methyl 3-{(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl}propanoate, ONO 2745, ONO-2745, ONO2745

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About This Item

經驗公式(希爾表示法):
C21H19BrN4O2
CAS號碼:
分子量::
439.31
MDL號碼:
分類程式碼代碼:
12352200

品質等級

化驗

≥98% (HPLC)

形狀

powder

藥物控制

USDEA Schedule IV

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

-10 to -25°C

SMILES 字串

CC1=CN=C2[C@H](CCC(OC)=O)N=C(C3=CC=CC=N3)C4=CC(Br)=CC=C4N12

InChI

1S/C21H19BrN4O2/c1-13-12-24-21-17(7-9-19(27)28-2)25-20(16-5-3-4-10-23-16)15-11-14(22)6-8-18(15)26(13)21/h3-6,8,10-12,17H,7,9H2,1-2H3/t17-/m0/s1

InChI 密鑰

CYHWMBVXXDIZNZ-KRWDZBQOSA-N

生化/生理作用

GABAA receptor positive allosteric modulator (PAM) that causes fast onset and short duration of sedative action in vivo with rapid recovery.
Remimazolam (CNS 7056) is a benzodiazepine derivative with positive allosteric modulator (PAM) activity toward γ-aminobutyric acid type A (GABAA) receptor (pKi = 7.53/7.50/7.56 against 2.5 nM flunitrazepam for binding human/rat/yucatan micropig brain homogenates; pEC50/Emax = 6.44/375% (α1β2γ2), 6.18/186% (α2β2γ2), 6.04/210% (α3β2γ2), 5.86/289% (α5β2γ2s) by whole cell patch clamp using cells expressing respective rat αβγ complex). Intravenous injection (25 mg/kg rats, 15-30 mg/kg mice) causes fast onset and short duration of sedative action with rapid recovery when compared with midazolam.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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分析證明 (COA)

Lot/Batch Number

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Metabolism of remimazolam in primary human hepatocytes during continuous long-term infusion in a 3-D bioreactor system
Freyer N, Knospel F, Damm G, Greuel S, Schneider C, Seehofer D, Stohr T, Petersen KU, Zeilinger K
Drug design, development and therapy, 13, 1033-1047 (2019)
Inhaled Remimazolam Potentiates Inhaled Remifentanil in Rodents
Bevans T, Deering-Rice C, Stockmann C, Rower J, Sakata D, Reilly C
Anesthesia and Analgesia, 124, 1484-1490 (2017)
Design, Synthesis, and Biological Evaluation of Novel CNS 7056 Derivatives as Sedatives in Rats and Rabbits
Yan Liu , Xiangqing Xu , Jianyong Xie , Huan Ma , Tao Wang , Guisen Zhang , Qingeng Li
Chemical Biology & Drug Design, 88, 38-42 (2016)
CNS 7056: a novel ultra-short-acting Benzodiazepine
Anesthesiology, 107, 60-66 (2007)
Pharmacokinetics and pharmacodynamics of the short-acting sedative CNS 7056 in sheep
R N Upton , A A Somogyi, A M Martinez, J Colvill, C Grant
British Journal of Anaesthesia, 105, 798-809 (2010)

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