DT-Web

DB00416 - Metocurine Iodide


Identification
Name Metocurine Iodide
Accession Number DB00416 (APRD01318)
Type small molecule
Description Metocurine iodide is a benzylisoquinolinium competitive nondepolarizing neuromuscular blocking agent. It is used as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy Metocurine iodide has a moderate risk of inducing histamine release and has some ganglion blocking activity. Metocurine iodide can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 906.6279
Groups approved
Monoisotopic Weight 906.160174118
Pharmacology
Indication For use as an anesthesia adjunct to induce skeletal muscle relaxation and to reduce the intensity of muscle contractions in convulsive therapy.
Mechanism of action Metocurine iodide 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 35% in plasma
Biotransformation Not Available
Route of elimination Not Available
Toxicity Excessive doses can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
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
  • 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
  • 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
  • Iwatsuki N, Hashimoto Y, Amaha K, Obara S, Iwatsuki K: Inotropic effects of non-depolarizing muscle relaxants in isolated canine heart muscle. Anesth Analg. 1980 Oct;59(10):717-21. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.5502

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0997
3923 Cholinesterase BCHE 0.0672
474 Acetylcholinesterase ACHE 0.0412
6145 Solute carrier family 22 member 1 SLC22A1 0.0389
341 5-hydroxytryptamine 3 receptor HTR3A 0.0313
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0295
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0208
1588 Multidrug resistance protein 1 ABCB1 0.0203
6144 Solute carrier family 22 member 2 SLC22A2 0.0173
723 Cytosolic phospholipase A2 PLA2G4A 0.0161
4119 Cytochrome P450 2D6 CYP2D6 0.0129
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0128
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0094
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
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0086
6081 Neuronal acetylcholine receptor subunit alpha-6 CHRNA6 0.0085
713 Sodium-dependent dopamine transporter SLC6A3 0.0081
4097 Neuronal acetylcholine receptor subunit alpha-9 CHRNA9 0.0081
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0078
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0071
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0068
319 Opioid receptor, sigma 1 OPRS1 0.006
947 Neuronal acetylcholine receptor subunit alpha-4 CHRNA4 0.0058
4095 Neuronal acetylcholine receptor subunit alpha-7 CHRNA7 0.0053
174 Sigma 1-type opioid receptor SIGMAR1 0.0048
4512 Cytochrome P450 3A4 CYP3A4 0.0047
6030 Cytochrome P450 2B6 CYP2B6 0.0038
6013 Cytochrome P450 2E1 CYP2E1 0.0037
4924 Cytochrome P450 2C8 CYP2C8 0.0035
6016 Cytochrome P450 2C19 CYP2C19 0.0034
4757 Cytochrome P450 2C9 CYP2C9 0.0032
824 Sodium-dependent serotonin transporter SLC6A4 0.0031
6014 Cytochrome P450 2A13 CYP2A13 0.0026
6107 Cytochrome P450 3A7 CYP3A7 0.0025
4118 Cytochrome P450 3A5 CYP3A5 0.0023
6147 Solute carrier family 22 member 3 SLC22A3 0.0017
833 Organic cation/carnitine transporter 1 SLC22A4 0.0017
3941 Amine oxidase [flavin-containing] A MAOA 0.0017
3939 Amine oxidase [flavin-containing] B MAOB 0.0016
118 Organic cation/carnitine transporter 2 SLC22A5 0.0015
5718 Cytochrome P450 2A6 CYP2A6 0.0014
6024 Cytochrome P450 1A1 CYP1A1 0.0014
4200 Cytochrome P450 1A2 CYP1A2 0.0011
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