Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H15ClN2 |
Molecular Weight | 270.757 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCN=C(C2=CC=CC=C2)C3=C1C=CC(Cl)=C3
InChI
InChIKey=YLCXGBZIZBEVPZ-UHFFFAOYSA-N
InChI=1S/C16H15ClN2/c1-19-10-9-18-16(12-5-3-2-4-6-12)14-11-13(17)7-8-15(14)19/h2-8,11H,9-10H2,1H3
Molecular Formula | C16H15ClN2 |
Molecular Weight | 270.757 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Medazepam is a benzodiazepine drug with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. Marketed in Russia. Indicated for the treatment of neurotic disorders and states, accompanied with sense of fear, anxiety, intension, raised irritability, insomnia, vegetative lability.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: 1.00520936E8 Gene Symbol: NOS1 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11731013 |
170.0 µM [IC50] | ||
Target ID: CHEMBL2093872 |
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Target ID: CHEMBL1907607 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2993620 |
528.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Nobrium Approved UseThis medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety. |
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Primary | Nobrium Approved UseThis medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety. |
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Primary | Nobrium Approved UseThis medication is used in the treatment of anxiety disorders, alcohol withdrawal, tremor, muscle spasms and to control seizures. It may also be used before surgery or procedures to reduce apprehension and anxiety. |
PubMed
Title | Date | PubMed |
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Medazepam compared with amylobarbitone in treatment of anxiety. | 1971 Jan 16 |
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Bromazepam, medazepam, chlordiazepoxide in treatment of neurotic anxiety. | 1974 May |
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Structural requirements of benzodiazepines for the inhibition of pig brain nitric oxide synthase. | 2001 Nov 30 |
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Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. | 2002 Apr |
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Quantitation using GC-TOF-MS: example of bromazepam. | 2002 Aug 14 |
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A population-based case-control teratologic study of nitrazepam, medazepam, tofisopam, alprazolum and clonazepam treatment during pregnancy. | 2002 Mar 10 |
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Square-wave voltammetric techniques for determination of psychoactive 1,4-benzodiazepine drugs. | 2002 Nov |
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[Determination of diazepine derivatives: alprazolam, medazepam, chlordiazepoxid mixture by high performance liquid chromatography]. | 2003 |
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[Comprehensive medical and ecological studies in Pryel'brussi]. | 2003 |
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Pharmacological activity of phenazepam and flunitrazepam in ultralow doses. | 2003 Jan |
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Determination of clofazimine in leprosy patients by high-performance liquid chromatography. | 2003 Sep |
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Mountain sports and total hip arthroplasty: a case report and review of mountaineering with total hip arthroplasty. | 2003 Summer |
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Screening, library-assisted identification and validated quantification of 23 benzodiazepines, flumazenil, zaleplone, zolpidem and zopiclone in plasma by liquid chromatography/mass spectrometry with atmospheric pressure chemical ionization. | 2004 Aug |
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Determination of diazepam in cream biscuits by liquid chromatography. | 2004 May-Jun |
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Diagnostic imaging in Canada. | 2005 |
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Risk and benefit of drug use during pregnancy. | 2005 |
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Cytokinin-binding protein (70 kDa): localization in tissues and cells of etiolated maize seedlings and its putative function. | 2007 |
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Human resource management in the Georgian National Immunization Program: a baseline assessment. | 2007 Jul 31 |
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[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia]. | 2008 |
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The educational background and qualifications of UK medical students from ethnic minorities. | 2008 Apr 16 |
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Randomised controlled trial of Alexander technique lessons, exercise, and massage (ATEAM) for chronic and recurrent back pain. | 2008 Aug 19 |
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A study of the effects of large doses of medazepam used for self-poisoning in 10 pregnant women on fetal development. | 2008 Feb-Mar |
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OSBPL10, a novel candidate gene for high triglyceride trait in dyslipidemic Finnish subjects, regulates cellular lipid metabolism. | 2009 Aug |
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Benzodiazepine prescription and length of hospital stay at a Japanese university hospital. | 2009 Oct 9 |
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Adverse drug effects in hospitalized elderly: data from the healthcare cost and utilization project. | 2010 |
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Evaluation of an hPXR reporter gene assay for the detection of aquatic emerging pollutants: screening of chemicals and application to water samples. | 2010 Jan |
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Barriers to treatment adherence in physiotherapy outpatient clinics: a systematic review. | 2010 Jun |
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Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines. | 2010 Mar 15 |
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[Oxygen consumption by resting humans at different Elbrus altitudes]. | 2010 May-Jun |
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1-(1-Phenyl-ethyl-idene)carbonohydrazide. | 2010 Sep 30 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://omedicine.info/en/medazepam.html
The average dose for adults: single - 10-20 mg, the average daily - 20-30 mg, the maximum - 60-70 mg / day. At the beginning of treatment - for 5 mg 2-3 times a day, then gradually increase the dose to 30-40 mg per day. In outpatient settings recommended by 5 mg in the morning and in the afternoon, and 10 mg in the evening. Elderly patients, teenagers, as well as kidney function - 5-10 mg 1-2 times a day, or 10 mg at night. Babies dose depends on the age and body weight. Treatment duration should be as short as possible (about 2 Sun) and should not exceed 2 Months (including the period of gradual reduction of the dose).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2859216
Medazepam (10 (-5) M) inhibited the contractile response of circular muscle strips from the isolated guinea-pig gallbladder to sulfated cholecystokinin octapeptide (CCK8) in the presence of atropine.
Substance Class |
Chemical
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P0J3387W3S
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Validated (UNII)
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NCI_THESAURUS |
C1012
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QN05BA03
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WHO-ATC |
N05BA03
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DEA NO. |
2836
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ACTIVE MOIETY |