DT-Web

DB01336 - Metocurine


Identification
Name Metocurine
Accession Number DB01336
Type small molecule
Description Dimethyltubocurarinium (INN) or metocurine (USAN), also known as dimethyltubocurarine, is a non-depolarizing muscle relaxant. Patients on chronic anticonvulsant drugs are relatively resistant to metocurine.(PMID: 9915319)
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 652.8189
Groups approved
Monoisotopic Weight 652.351237278
Pharmacology
Indication Metocurine is a muscle relaxant.
Mechanism of action Metocurine antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions
Drug Mechanism of interaction
Amikacin The agent increases the effect of muscle relaxant
Aminophylline Theophylline decreases the effect of muscle relaxant
Azathioprine The agent decreases the effect of the muscle relaxant
Carbamazepine Decreases the effect of muscle relaxant
Clindamycin The agent increases the effect of muscle relaxant
Fosphenytoin Phenytoin decreases the effect of muscle relaxant
Gentamicin The agent increases the effect of muscle relaxant
Lincomycin The agent increases the effect of muscle relaxant
Mercaptopurine The agent dereases the effect of the muscle relaxant
Netilmicin The agent increases the effect of muscle relaxant
Oxtriphylline Theophylline decreases the effect of muscle relaxant
Phenytoin Phenytoin decreases the effect of the muscle relaxant
Piperacillin The agent increases the effect of the muscle relaxant
Quinidine The quinine derivative increases the effect of the muscle relaxant
Quinine The quinine derivative increases the effect of the muscle relaxant
Theophylline Theophylline decreases the effect of the muscle relaxant
Tobramycin The agent increases the effect of the muscle relaxant
Food Interactions Not Available

Targets


Neuronal acetylcholine receptor subunit alpha-2
Name Neuronal acetylcholine receptor subunit alpha-2
Gene Name CHRNA2
Pharmacological action yes
Actions antagonist
References
  • Liu M, Dilger JP: Synergy between pairs of competitive antagonists at adult human muscle acetylcholine receptors. Anesth Analg. 2008 Aug;107(2):525-33. - Pubmed
  • Liu M, Dilger JP: Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholine receptor. Mol Pharmacol. 2009 Jan;75(1):166-73. Epub 2008 Oct 8. - Pubmed
  • Groebe DR, Dumm JM, Abramson SN: Irreversible inhibition of nicotinic acetylcholine receptors by the bipinnatins. Toxin activation and kinetics of receptor inhibition. J Biol Chem. 1994 Mar 25;269(12):8885-91. - Pubmed
  • Wang HL, Gao F, Bren N, Sine SM: Curariform antagonists bind in different orientations to the nicotinic receptor ligand binding domain. J Biol Chem. 2003 Aug 22;278(34):32284-91. Epub 2003 Jun 10. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.6012
Muscarinic acetylcholine receptor M2
Name Muscarinic acetylcholine receptor M2
Gene Name CHRM2
Pharmacological action unknown
Actions antagonist
References
  • Son SL, Waud DR: Effects of non-depolarizing neuromuscular blocking agents on the cardiac vagus nerve in the guineapig. Br J Anaesth. 1980 Oct;52(10):981-7. - Pubmed
DTHybrid score 0.3685

Predictions


Id Partner name Gene Name Score
51 Muscarinic acetylcholine receptor M3 CHRM3 0.1669
103 Muscarinic acetylcholine receptor M1 CHRM1 0.1656
3923 Cholinesterase BCHE 0.0983
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0829
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0649
6145 Solute carrier family 22 member 1 SLC22A1 0.0483
474 Acetylcholinesterase ACHE 0.0475
341 5-hydroxytryptamine 3 receptor HTR3A 0.0395
4119 Cytochrome P450 2D6 CYP2D6 0.0341
1588 Multidrug resistance protein 1 ABCB1 0.0333
492 Histamine H1 receptor HRH1 0.0286
4512 Cytochrome P450 3A4 CYP3A4 0.026
6144 Solute carrier family 22 member 2 SLC22A2 0.0247
723 Cytosolic phospholipase A2 PLA2G4A 0.0228
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0186
502 5-hydroxytryptamine 2A receptor HTR2A 0.0158
556 Alpha-1A adrenergic receptor ADRA1A 0.0123
4757 Cytochrome P450 2C9 CYP2C9 0.0122
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0121
590 5-hydroxytryptamine 2C receptor HTR2C 0.0119
831 D(2) dopamine receptor DRD2 0.0117
6013 Cytochrome P450 2E1 CYP2E1 0.0116
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0114
6016 Cytochrome P450 2C19 CYP2C19 0.0113
198 Sodium channel protein type 10 subunit alpha SCN10A 0.011
23 D(1A) dopamine receptor DRD1 0.0105
4924 Cytochrome P450 2C8 CYP2C8 0.0102
4200 Cytochrome P450 1A2 CYP1A2 0.0098
6030 Cytochrome P450 2B6 CYP2B6 0.0096
713 Sodium-dependent dopamine transporter SLC6A3 0.0095
824 Sodium-dependent serotonin transporter SLC6A4 0.0095
833 Organic cation/carnitine transporter 1 SLC22A4 0.0092
6082 Neuronal acetylcholine receptor subunit beta-3 CHRNB3 0.0092
6080 Neuronal acetylcholine receptor subunit alpha-5 CHRNA5 0.0092
948 Neuronal acetylcholine receptor subunit beta-2 CHRNB2 0.0091
4118 Cytochrome P450 3A5 CYP3A5 0.0087
789 Alpha-1D adrenergic receptor ADRA1D 0.0086
6081 Neuronal acetylcholine receptor subunit alpha-6 CHRNA6 0.0085
4097 Neuronal acetylcholine receptor subunit alpha-9 CHRNA9 0.0081
540 Sodium-dependent noradrenaline transporter SLC6A2 0.008
632 Alpha-1B adrenergic receptor ADRA1B 0.008
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0078
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0078
118 Organic cation/carnitine transporter 2 SLC22A5 0.0074
6024 Cytochrome P450 1A1 CYP1A1 0.0074
432 D(4) dopamine receptor DRD4 0.0072
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0071
319 Opioid receptor, sigma 1 OPRS1 0.006
436 5-hydroxytryptamine 2B receptor HTR2B 0.0059
638 D(3) dopamine receptor DRD3 0.0059
947 Neuronal acetylcholine receptor subunit alpha-4 CHRNA4 0.0058
6107 Cytochrome P450 3A7 CYP3A7 0.0057
5718 Cytochrome P450 2A6 CYP2A6 0.0054
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0054
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0054
4095 Neuronal acetylcholine receptor subunit alpha-7 CHRNA7 0.0053
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0052
320 5-hydroxytryptamine 1A receptor HTR1A 0.0051
2129 Sucrase-isomaltase, intestinal SI 0.0051
378 Alpha-2C adrenergic receptor ADRA2C 0.005
318 Alpha-2A adrenergic receptor ADRA2A 0.0049
629 Alpha-2B adrenergic receptor ADRA2B 0.0049
174 Sigma 1-type opioid receptor SIGMAR1 0.0048
528 5-hydroxytryptamine 1E receptor HTR1E 0.0045
1256 5-hydroxytryptamine 6 receptor HTR6 0.0041
163 D(1B) dopamine receptor DRD5 0.0041
716 5-hydroxytryptamine 7 receptor HTR7 0.0038
220 Sodium channel protein type 5 subunit alpha SCN5A 0.0035
725 5-hydroxytryptamine 1D receptor HTR1D 0.0034
885 5-hydroxytryptamine 1B receptor HTR1B 0.0033
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0032
6147 Solute carrier family 22 member 3 SLC22A3 0.0032
6014 Cytochrome P450 2A13 CYP2A13 0.0026
465 Calmodulin CALM1 0.0025
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0024
6432 Transporter snf 0.0021
3941 Amine oxidase [flavin-containing] A MAOA 0.0017
587 Serum albumin ALB 0.0016
3939 Amine oxidase [flavin-containing] B MAOB 0.0016
6106 Cytochrome P450 2C18 CYP2C18 0.0015
1360 Sphingomyelin phosphodiesterase SMPD1 0.0015
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0015
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0014
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0013
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0013
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.001
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.001
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.001
1618 High affinity nerve growth factor receptor NTRK1 0.001
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.001
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.001
124 Histamine H2 receptor HRH2 0.0009
164 Histamine H4 receptor HRH4 0.0009
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0009
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0008
20 Prostaglandin G/H synthase 1 PTGS1 0.0008
193 Beta-1 adrenergic receptor ADRB1 0.0007
766 Beta-2 adrenergic receptor ADRB2 0.0007
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0007
467 Delta-type opioid receptor OPRD1 0.0006
696 Kappa-type opioid receptor OPRK1 0.0006
1898 Cytochrome P450 1B1 CYP1B1 0.0005
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