DT-Web

DB00801 - Halazepam


Identification
Name Halazepam
Accession Number DB00801 (APRD01009)
Type small molecule
Description Halazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoromethyl derivative of nordazepam. While its structure may be similar to chlordiazepoxide and diazepam, it has both less toxicity and less tendency to cause paradoxical hostility and aggression than either of them. [Wikipedia]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 352.738
Groups illicit
Monoisotopic Weight 352.059025338
Pharmacology
Indication Used to relieve anxiety, nervousness, and tension associated with anxiety disorders.
Mechanism of action Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Absorption Not Available
Protein binding Not Available
Biotransformation Hepatic.
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Cimetidine Cimetidine may increase the effect of the benzodiazepine, halazepam.
Clozapine Increased risk of toxicity
Fluconazole Fluconazole may increase the effect of the benzodiazepine, halazepam.
Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, halazepam.
Itraconazole Itraconazole may increase the effect of the benzodiazepine, halazepam.
Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, halazepam.
Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, halazepam.
Omeprazole Omeprazole may increase the effect of the benzodiazepine, halazepam.
Food Interactions Not Available

Targets


Gamma-aminobutyric-acid receptor subunit alpha-1
Name Gamma-aminobutyric-acid receptor subunit alpha-1
Gene Name GABRA1
Pharmacological action yes
Actions potentiator
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
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.0379
Gamma-aminobutyric-acid receptor subunit alpha-2
Name Gamma-aminobutyric-acid receptor subunit alpha-2
Gene Name GABRA2
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9563
Gamma-aminobutyric-acid receptor subunit alpha-3
Name Gamma-aminobutyric-acid receptor subunit alpha-3
Gene Name GABRA3
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9512
Gamma-aminobutyric-acid receptor subunit alpha-5
Name Gamma-aminobutyric-acid receptor subunit alpha-5
Gene Name GABRA5
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9781
Gamma-aminobutyric acid receptor subunit gamma-1
Name Gamma-aminobutyric acid receptor subunit gamma-1
Gene Name GABRG1
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9388
Gamma-aminobutyric acid receptor subunit gamma-2
Name Gamma-aminobutyric acid receptor subunit gamma-2
Gene Name GABRG2
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9719
Gamma-aminobutyric acid receptor subunit gamma-3
Name Gamma-aminobutyric acid receptor subunit gamma-3
Gene Name GABRG3
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9201
Gamma-aminobutyric-acid receptor subunit beta-1
Name Gamma-aminobutyric-acid receptor subunit beta-1
Gene Name GABRB1
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9481
Gamma-aminobutyric-acid receptor subunit beta-2
Name Gamma-aminobutyric-acid receptor subunit beta-2
Gene Name GABRB2
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.933
Gamma-aminobutyric-acid receptor subunit beta-3
Name Gamma-aminobutyric-acid receptor subunit beta-3
Gene Name GABRB3
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9526
Gamma-aminobutyric acid receptor subunit delta
Name Gamma-aminobutyric acid receptor subunit delta
Gene Name GABRD
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9279
Gamma-aminobutyric acid receptor subunit epsilon
Name Gamma-aminobutyric acid receptor subunit epsilon
Gene Name GABRE
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9261
Gamma-aminobutyric acid receptor subunit pi
Name Gamma-aminobutyric acid receptor subunit pi
Gene Name GABRP
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9112
Gamma-aminobutyric-acid receptor subunit rho-1
Name Gamma-aminobutyric-acid receptor subunit rho-1
Gene Name GABRR1
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9188
Gamma-aminobutyric acid receptor subunit rho-2
Name Gamma-aminobutyric acid receptor subunit rho-2
Gene Name GABRR2
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9221
Gamma-aminobutyric acid receptor subunit rho-3
Name Gamma-aminobutyric acid receptor subunit rho-3
Gene Name GABRR3
Pharmacological action yes
Actions potentiator
References
  • Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. - Pubmed
  • Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. - Pubmed
DTHybrid score 0.9192

Predictions


Id Partner name Gene Name Score
530 Gamma-aminobutyric-acid receptor subunit alpha-4 GABRA4 0.5917
841 Gamma-aminobutyric-acid receptor subunit alpha-6 GABRA6 0.5647
6091 Gamma-aminobutyric acid receptor subunit theta GABRQ 0.5481
4512 Cytochrome P450 3A4 CYP3A4 0.3507
811 Translocator protein TSPO 0.3299
6016 Cytochrome P450 2C19 CYP2C19 0.1782
4095 Neuronal acetylcholine receptor subunit alpha-7 CHRNA7 0.1657
947 Neuronal acetylcholine receptor subunit alpha-4 CHRNA4 0.1656
918 Glutamate receptor, ionotropic kainate 2 GRIK2 0.1618
6013 Cytochrome P450 2E1 CYP2E1 0.1588
921 Glutamate receptor 2 GRIA2 0.1475
4757 Cytochrome P450 2C9 CYP2C9 0.1375
6030 Cytochrome P450 2B6 CYP2B6 0.1211
1588 Multidrug resistance protein 1 ABCB1 0.1041
6107 Cytochrome P450 3A7 CYP3A7 0.1015
4118 Cytochrome P450 3A5 CYP3A5 0.0956
6106 Cytochrome P450 2C18 CYP2C18 0.0883
4924 Cytochrome P450 2C8 CYP2C8 0.0786
587 Serum albumin ALB 0.0767
4200 Cytochrome P450 1A2 CYP1A2 0.0594
4119 Cytochrome P450 2D6 CYP2D6 0.0505
5718 Cytochrome P450 2A6 CYP2A6 0.0429
20 Prostaglandin G/H synthase 1 PTGS1 0.0426
482 Glycine receptor subunit alpha-1 GLRA1 0.0423
276 Sodium- and chloride-dependent GABA transporter 1 SLC6A1 0.0407
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0406
6102 Arylamine N-acetyltransferase 2 NAT2 0.0405
6027 Alkaline phosphatase, tissue-nonspecific isozyme ALPL 0.035
461 Glycine receptor subunit alpha-3 GLRA3 0.0344
6031 Cytochrome P450 3A43 CYP3A43 0.0316
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0305
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0302
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0297
820 Glycine receptor subunit alpha-2 GLRA2 0.0284
6144 Solute carrier family 22 member 2 SLC22A2 0.0229
6145 Solute carrier family 22 member 1 SLC22A1 0.0195
2981 Phospholipase A2, membrane associated PLA2G2A 0.0182
3426 Glutamine synthetase glnA 0.0182
3987 Glutamine synthetase GLUL 0.0182
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0159
3937 Fatty-acid amide hydrolase FAAH 0.0156
6024 Cytochrome P450 1A1 CYP1A1 0.0154
240 Gamma-aminobutyric acid type B receptor, subunit 1 GABBR1 0.0151
172 Potassium channel subfamily K member 1 KCNK1 0.0144
241 Calcium-transporting ATPase type 2C member 1 ATP2C1 0.0138
62 Glycine receptor subunit beta GLRB 0.0132
537 ATP synthase delta chain, mitochondrial ATP5D 0.0132
705 Glutamate receptor 1 GRIA1 0.0127
559 NADH-ubiquinone oxidoreductase chain 1 MT-ND1 0.0124
489 Monocarboxylate transporter 2 SLC16A7 0.0121
500 Monocarboxylate transporter 4 SLC16A3 0.0118
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0116
738 Monocarboxylate transporter 1 SLC16A1 0.0104
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0091
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0086
862 Multidrug resistance-associated protein 1 ABCC1 0.0077
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0073
6017 Cholesterol side-chain cleavage enzyme, mitochondrial CYP11A1 0.0072
1898 Cytochrome P450 1B1 CYP1B1 0.0071
4209 ATP-sensitive inward rectifier potassium channel 8 KCNJ8 0.0069
3802 Sodium channel protein type 2 subunit alpha SCN2A 0.0065
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0065
3804 Sodium channel protein type 4 subunit alpha SCN4A 0.006
468 Cytochrome P450 4A11 CYP4A11 0.0056
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0054
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0052
1680 Solute carrier family 2, facilitated glucose transporter member 1 SLC2A1 0.0049
23 D(1A) dopamine receptor DRD1 0.0046
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0045
382 Glutamate receptor, ionotropic kainate 1 GRIK1 0.0045
318 Alpha-2A adrenergic receptor ADRA2A 0.0045
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0042
556 Alpha-1A adrenergic receptor ADRA1A 0.0042
6152 Solute carrier organic anion transporter family member 2A1 SLCO2A1 0.0037
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0037
6020 Aldehyde oxidase AOX1 0.0037
610 Calcium-activated potassium channel subunit alpha 1 KCNMA1 0.0034
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0032
629 Alpha-2B adrenergic receptor ADRA2B 0.0031
776 Bile salt export pump ABCB11 0.003
3811 Cytochrome P450 19A1 CYP19A1 0.003
592 Carbonic anhydrase 4 CA4 0.003
502 5-hydroxytryptamine 2A receptor HTR2A 0.0027
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0023
357 Carbonic anhydrase 2 CA2 0.0021
251 Alcohol dehydrogenase 1A ADH1A 0.0019
465 Calmodulin CALM1 0.0018
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0018
824 Sodium-dependent serotonin transporter SLC6A4 0.0018
444 Alcohol dehydrogenase 1B ADH1B 0.0016
831 D(2) dopamine receptor DRD2 0.0016
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0016
1768 Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit GNG2 0.0015
1581 G protein-activated inward rectifier potassium channel 2 KCNJ6 0.0015
1268 Neuropeptide S receptor NPSR1 0.0015
1571 G protein-activated inward rectifier potassium channel 1 KCNJ3 0.0015
517 Alcohol dehydrogenase 1C ADH1C 0.0014
6073 Potassium channel subfamily K member 9 KCNK9 0.0014
6072 Potassium channel subfamily K member 3 KCNK3 0.0014
462 Intermediate conductance calcium-activated potassium channel protein 4 KCNN4 0.0012
591 Glutamate [NMDA] receptor subunit 3B GRIN3B 0.0011
837 Glutamate [NMDA] receptor subunit epsilon-1 GRIN2A 0.001
2207 Rhodopsin RHO 0.001
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