Drug Information
Drug (ID: DG00274) and It's Reported Resistant Information
Name |
Midazolam
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Synonyms |
Dazolam; Dormicum; Midanium; Midazolamum; Midosed; Versed; Midazolam Base; Dormicum (TN); Hypnovel (TN); Midacum (TN); Midazolamum [INN-Latin]; Ro 21-3981; Versed (TN); Midazolam (JAN/INN); Midazolam [INN:BAN:JAN]; 4H-Imidazo[1,5-a][1,4]benzodiazepine, 8-chloro-6-(2-fluoro-phenyl)-1-methyl-, (Z)-2-butenedioate; 8-Chlor-6-(2-fluorphenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepin; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5a][1,4]benzodiazepine hydrochloride; 8-Chloro-6-(O-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]-benzodiazepine; 8-Chloro-6-(o-fluorophenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepine
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Indication |
In total 2 Indication(s)
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Structure | |||||
Target | Translocator protein (TSPO) | TSPO_HUMAN | [1] | ||
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Formula |
C18H13ClFN3
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IsoSMILES |
CC1=NC=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4F
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InChI |
1S/C18H13ClFN3/c1-11-21-9-13-10-22-18(14-4-2-3-5-16(14)20)15-8-12(19)6-7-17(15)23(11)13/h2-9H,10H2,1H3
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InChIKey |
DDLIGBOFAVUZHB-UHFFFAOYSA-N
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DrugBank ID |
Type(s) of Resistant Mechanism of This Drug
DISM: Drug Inactivation by Structure Modification
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-07: Sleep-wake disorders
Insomnia [ICD-11: 7A00]
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | ||||
Drug Inactivation by Structure Modification (DISM) | ||||
Key Molecule: Cytochrome P450 family 3 subfamily A member1 (CYP3A4) | [1] | |||
Molecule Alteration | Expression | Down-regulation |
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Sensitive Disease | Insomnia [ICD-11: 7A00.0] | |||
Experimental Note | Identified from the Human Clinical Data | |||
In Vitro Model | CaCo2 cells | Colon | Homo sapiens (Human) | CVCL_0025 |
IPS cells | Colon | Homo sapiens (Human) | N.A. | |
Experiment for Molecule Alteration |
qPCR | |||
Experiment for Drug Resistance |
Transcellular transport study assay | |||
Mechanism Description | The extraction ratio of metabolism of midazolam (a substrate of CYP3A4) to 1-OH midazolam in hiPSC-IECs was 0.534 +/- 0.009 (%), and decreased to 0.322 +/- 0.009 (%) and 0.0821 +/- 0.0064 (%) in the presence of 0.5 and 10 uM ketoconazole (an inhibitor of CYP3A4), respectively. The extraction ratio in Caco-2 cells was 0.0623 +/- 0.0038 (%) and also decreased to 0.0404 +/- 0.0023 (%) and 0.0414 +/- 0.0032 (%) in the presence of 0.5 and 10 uM ketoconazole, respectively. |
References
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