Identification
Name Chlormezanone
Accession Number DB01178 (APRD00865)
Type small molecule
Description A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. [PubChem]
Structure
Categories (*)
Molecular Weight 273.736
Groups approved
Monoisotopic Weight 273.022641652
Pharmacology
Indication Used in the management of anxiety and in the treatment of muscle spasm.
Mechanism of action Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Symptoms of overdose include drowsiness, weakness, nausea, dizziness, abdominal pain, cerebral oedema and renal tubular necrosis, hyperglycaemia and hypoglycaemia, liver damage, encephalopathy, coma and death.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available
Translocator protein
Name Translocator protein
Gene Name TSPO
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.2259
Id Partner name Gene Name Score
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0509
523 Gamma-aminobutyric-acid receptor subunit alpha-5 GABRA5 0.0411
580 Gamma-aminobutyric-acid receptor subunit alpha-3 GABRA3 0.0411
423 Gamma-aminobutyric-acid receptor subunit alpha-2 GABRA2 0.0408
6093 Gamma-aminobutyric acid receptor subunit delta GABRD 0.037
6087 Gamma-aminobutyric acid receptor subunit gamma-1 GABRG1 0.037
6089 Gamma-aminobutyric acid receptor subunit epsilon GABRE 0.0369
4098 Gamma-aminobutyric-acid receptor subunit beta-1 GABRB1 0.0351
4512 Cytochrome P450 3A4 CYP3A4 0.0321
6091 Gamma-aminobutyric acid receptor subunit theta GABRQ 0.0298
6090 Gamma-aminobutyric acid receptor subunit pi GABRP 0.0272
6088 Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3 0.0272
6092 Gamma-aminobutyric acid receptor subunit rho-2 GABRR2 0.0272
6115 Gamma-aminobutyric acid receptor subunit rho-3 GABRR3 0.0272
6086 Gamma-aminobutyric acid receptor subunit gamma-2 GABRG2 0.0269
142 Gamma-aminobutyric-acid receptor subunit rho-1 GABRR1 0.0267
4100 Gamma-aminobutyric-acid receptor subunit beta-2 GABRB2 0.0263
4099 Gamma-aminobutyric-acid receptor subunit beta-3 GABRB3 0.0251
530 Gamma-aminobutyric-acid receptor subunit alpha-4 GABRA4 0.0243
841 Gamma-aminobutyric-acid receptor subunit alpha-6 GABRA6 0.0211
4757 Cytochrome P450 2C9 CYP2C9 0.0198
4924 Cytochrome P450 2C8 CYP2C8 0.0162
6107 Cytochrome P450 3A7 CYP3A7 0.0152
4118 Cytochrome P450 3A5 CYP3A5 0.0143
20 Prostaglandin G/H synthase 1 PTGS1 0.0139
6020 Aldehyde oxidase AOX1 0.0137
6013 Cytochrome P450 2E1 CYP2E1 0.013
587 Serum albumin ALB 0.0099
6030 Cytochrome P450 2B6 CYP2B6 0.0073
6016 Cytochrome P450 2C19 CYP2C19 0.0066
1588 Multidrug resistance protein 1 ABCB1 0.0065
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0048
6102 Arylamine N-acetyltransferase 2 NAT2 0.0046
4200 Cytochrome P450 1A2 CYP1A2 0.0045
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0045
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0044
5718 Cytochrome P450 2A6 CYP2A6 0.0038
6106 Cytochrome P450 2C18 CYP2C18 0.0024