Identification
Name Metiamide
Accession Number DB08805
Type small molecule
Description Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine.
Structure
Categories (*)
Molecular Weight 244.38
Groups experimental
Monoisotopic Weight 244.081637912
Pharmacology
Indication Potential in the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
Mechanism of action Metiamide binds to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. This competitive inhibition results in reduced gastric acid secretion and a reduction in gastric volume and acidity.
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 Not Available
Food Interactions Not Available
Histamine H2 receptor
Name Histamine H2 receptor
Gene Name HRH2
Pharmacological action yes
Actions antagonist
References
  • Black JW, Duncan WA, Emmett JC, Ganellin CR, Hesselbo T, Parsons ME, Wyllie JH: Metiamide--an orally active histamine H2-receptor antagonist. 1973. Agents Actions. 1994 Dec;43(3-4):91-5; discussion 96. - Pubmed
DTHybrid score 0.5519
Id Partner name Gene Name Score
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0339
1588 Multidrug resistance protein 1 ABCB1 0.0301
6142 Solute carrier family 22 member 8 SLC22A8 0.0253
6144 Solute carrier family 22 member 2 SLC22A2 0.0247
6016 Cytochrome P450 2C19 CYP2C19 0.0225
3923 Cholinesterase BCHE 0.0222
4119 Cytochrome P450 2D6 CYP2D6 0.0198
4512 Cytochrome P450 3A4 CYP3A4 0.0178
492 Histamine H1 receptor HRH1 0.0168
6145 Solute carrier family 22 member 1 SLC22A1 0.015
716 5-hydroxytryptamine 7 receptor HTR7 0.0129
318 Alpha-2A adrenergic receptor ADRA2A 0.0122
1341 Histamine H3 receptor HRH3 0.0121
502 5-hydroxytryptamine 2A receptor HTR2A 0.0118
4200 Cytochrome P450 1A2 CYP1A2 0.0117
556 Alpha-1A adrenergic receptor ADRA1A 0.0114
164 Histamine H4 receptor HRH4 0.0109
6147 Solute carrier family 22 member 3 SLC22A3 0.0094
4203 Histamine N-methyltransferase HNMT 0.0088
118 Organic cation/carnitine transporter 2 SLC22A5 0.0083
4118 Cytochrome P450 3A5 CYP3A5 0.0081
4757 Cytochrome P450 2C9 CYP2C9 0.0078
436 5-hydroxytryptamine 2B receptor HTR2B 0.0067
378 Alpha-2C adrenergic receptor ADRA2C 0.0062
629 Alpha-2B adrenergic receptor ADRA2B 0.0061
590 5-hydroxytryptamine 2C receptor HTR2C 0.0059
6030 Cytochrome P450 2B6 CYP2B6 0.0058
320 5-hydroxytryptamine 1A receptor HTR1A 0.0056
831 D(2) dopamine receptor DRD2 0.0052
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0047
1256 5-hydroxytryptamine 6 receptor HTR6 0.0043
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0041
6154 Multidrug and toxin extrusion protein 1 SLC47A1 0.0041
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0039
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0035
432 D(4) dopamine receptor DRD4 0.0035
638 D(3) dopamine receptor DRD3 0.0034
885 5-hydroxytryptamine 1B receptor HTR1B 0.0033
193 Beta-1 adrenergic receptor ADRB1 0.0032
833 Organic cation/carnitine transporter 1 SLC22A4 0.0031
766 Beta-2 adrenergic receptor ADRB2 0.0031
23 D(1A) dopamine receptor DRD1 0.003
789 Alpha-1D adrenergic receptor ADRA1D 0.0029
776 Bile salt export pump ABCB11 0.0029
1024 Solute carrier family 22 member 11 SLC22A11 0.0029
6143 Solute carrier family 22 member 7 SLC22A7 0.0028
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0028
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0028
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0027
824 Sodium-dependent serotonin transporter SLC6A4 0.0026
632 Alpha-1B adrenergic receptor ADRA1B 0.0026
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0026
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0025
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0024
1729 Solute carrier family 22 member 6 SLC22A6 0.0023
6013 Cytochrome P450 2E1 CYP2E1 0.0023
6107 Cytochrome P450 3A7 CYP3A7 0.0023
4924 Cytochrome P450 2C8 CYP2C8 0.0021