Remimazolam

Research use only, not for human use.

Remimazolam is a benzodiazepine derivative drug as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Remimazolam was found to be both faster acting and shorter lasting than midazolam, and human clinical trials showed a faster recovery time and predictable, consistent pharmacokinetics, suggesting some advantages over existing drugs for these applications.

Remimazolam is a benzodiazepine derivative drug as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures. Remimazolam was found to be both faster acting and shorter lasting than midazolam, and human clinical trials showed a faster recovery time and predictable, consistent pharmacokinetics, suggesting some advantages over existing drugs for these applications. Mice showed significantly increased time to movement outside a set perimeter after 5-minute exposure to increasing concentrations (10-25 mg/mL solutions) of inhaled remimazolam aerosols. Differences in mean (95% confidence interval) time to movement from pretest baseline group (0.05 [0.01-0.09] minutes) were 11 (4-18), 15 (5-26), 30 (19-41), and 109 (103-115) minutes after exposure to remimazolam aerosol of 10, 15, 20, and 25 mg/mL, respectively (P = .007 - P < .0001). Exposure of rats to remimazolam aerosols alone failed to produce sedation or analgesia after a 5-minute exposure. When remimazolam (10 or 25 mg/mL) was administered in combination with 250 μg/mL remifentanil, there was a significant difference in time to tail flick (P < .0001) consistent with a strong analgesic effect. Mean (95% confidence interval) differences in time to tail flick from the pretest baseline group (3.2 [2.5-3.9] seconds) were 14 (10-18) seconds when 250 μg/mL remifentanil was administered with either 10 or 25 mg/mL remimazolam. Remimazolam alone or in combination with remifentanil did not cause lung irritation, bronchospasm, or other adverse pulmonary events to the respiratory tract of mice as assessed by Flexi-Vent pulmonary function tests. Remimazolam can significantly potentiate the analgesic effect of remifentanil when concurrently delivered via inhalation.

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CNS-7056,CNS 7056,CNS7056

Others

Other Targets

Others

nervous system

Anesthesia

308242-62-8

439.31

C21H19BrN4O2

>98% (HPLC)

DMSO:Soluble; Water:Insoluble

CC1=CN=C2N1C3=C(C=C(C=C3)Br)C(=NC2CCC(=O)OC)C4=CC=CC=N4

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(-20℃)

With Ice Pack

≥ 2 years