Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM78IME)

Drug Name
Ergotidine Drug Info
Synonyms
Eramin; Ergamine; Histamine; Histaminum; Istamina; Theramine; Free histamine; Histamine Base; Histamine [USAN]; Istamina [Italian]; H7125_SIGMA; [3H]histamine; ALBB-005968; Beta-Aminoethylglyoxaline; Beta-Aminoethylimidazole; Beta-aminothethylglyoxaline; Histamine (DCF); Histamine, Free Base; Histaminum (TN); L-histamine; ZERO/004089; Imidazole-4-ethylamine; Beta-Imidazolyl-4-ethylamine; F411C768-A159-4FC0-A195-291A08BB03AA; 1H-Imidazole-4-ethanamine; 1H-Imidazole-5-ethanamine; 2-(1H-Imidazol-4-yl)ethanamine; 2-(1H-imidazol-4-yl)ethan-1-amine; 2-(1H-imidazol-5-yl)ethanamine; 2-(3H-Imidazol-4-yl)-ethylamine; 2-(4-Imidazolyl)ethylamine; 2-Imidazol-4-ylethylamine; 2-[4-Imidazolyl]ethylamine; 4-(2-Aminoethyl)-1H-imidazole; 4-Imidazoleethylamine; 5-Imidazoleethylamine
Indication
Disease Entry ICD 11 Status REF
Osteoarthritis FA00-FA05 Approved [1]
Respiratory allergy 4A80 Approved [2]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
774
ChEBI ID
CHEBI:18295
CAS Number
CAS 51-45-6
TTD Drug ID
DM78IME
VARIDT Drug ID
DR00081
INTEDE Drug ID
DR0810

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Agonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Equilibrative nucleoside transporter 4 (SLC29A4) DT3EAQP S29A4_HUMAN Approved [4]
Vesicular amine transporter 2 (SLC18A2) DTT7VPB VMAT2_HUMAN Approved [5]
Vesicular amine transporter 1 (SLC18A1) DTM953D VMAT1_HUMAN Approved [6]
Organic cation transporter 3 (SLC22A3) DT6201N S22A3_HUMAN Approved [7]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Approved [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [9]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [9]
Thiopurine methyltransferase (TPMT) DEFQ8VO TPMT_HUMAN Approved [10]
Histamine N-methyltransferase (HNMT) DE3PZ0I HNMT_HUMAN Approved [11]
Amiloride-sensitive amine oxidase (AOC1) DETECWH AOC1_HUMAN Approved [12]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Histamine H1 receptor (H1R) DTT HRH1 5.972 5.7 5.816 6.002
Vesicular amine transporter 2 (SLC18A2) DTP VMAT2 0.766 3 2.263 3.35
Vesicular amine transporter 1 (SLC18A1) DTP VMAT1 3.828 5.166 2.807 3.597
Organic cation transporter 2 (SLC22A2) DTP `OCT2 3.766 3.548 7.303 3.548
Organic cation transporter 3 (SLC22A3) DTP `OCT3 5.289 1.963 3.472 3.621
Amiloride-sensitive amine oxidase (AOC1) DME AOC1 5.536 10.003 9.42 10.759
Thiopurine methyltransferase (TPMT) DME TPMT 6.753 5.907 6.614 6.712
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Histamine N-methyltransferase (HNMT) DME HNMT 5.986 5.657 5.387 4.938
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Osteoarthritis
ICD Disease Classification FA00-FA05
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Histamine H1 receptor (H1R) DTT HRH1 6.74E-01 0.13 0.43
Vesicular amine transporter 2 (SLC18A2) DTP VMAT2 1.35E-03 -2.70E+00 -1.58E+00
Vesicular amine transporter 1 (SLC18A1) DTP VMAT1 2.09E-01 -1.66E-01 -3.68E-01
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 1.57E-01 -2.96E-01 -1.02E+00
Organic cation transporter 3 (SLC22A3) DTP SLC22A3 2.42E-01 2.18E-01 8.46E-01
Equilibrative nucleoside transporter 4 (SLC29A4) DTP ENT4 6.77E-01 7.67E-02 2.27E-01
Amiloride-sensitive amine oxidase (AOC1) DME AOC1 6.20E-01 -8.36E-03 -8.18E-02
Thiopurine methyltransferase (TPMT) DME TPMT 7.06E-01 -1.87E-01 -5.89E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.35E-01 2.78E-02 2.09E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.76E-01 1.26E-01 8.27E-01
Histamine N-methyltransferase (HNMT) DME HNMT 6.70E-01 1.08E-01 5.85E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 A standard database for drug repositioning. Sci Data. 2017 Mar 14;4:170029.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1247).
3 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
4 Histamine uptake mediated by plasma membrane monoamine transporter and organic cation transporters in rat mast cell lines. Eur J Pharmacol. 2019 Apr 15;849:75-83.
5 The vesicular monoamine transporter 2: an underexplored pharmacological target. Neurochem Int. 2014 Jul;73:89-97.
6 Gastrin-producing endocrine cells: a novel source of histamine in the rat stomach. Endocrinology. 1998 Oct;139(10):4404-15.
7 Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
8 The organic cation transporters (OCT1, OCT2, EMT) and the plasma membrane monoamine transporter (PMAT) show differential distribution and cyclic expression pattern in human endometrium and early pregnancy decidua. Mol Reprod Dev. 2007 Oct;74(10):1303-11.
9 Atazanavir for the treatment of human immunodeficiency virus infection. Pharmacotherapy. 2004 Dec;24(12):1732-47.
10 Histamine-N-methyl transferase polymorphism and risk for multiple sclerosis. Eur J Neurol. 2010 Feb;17(2):335-8.
11 Histamine pharmacogenomics. Pharmacogenomics. 2009 May;10(5):867-83.
12 Human kidney diamine oxidase: heterologous expression, purification, and characterization. J Biol Inorg Chem. 2002 Jun;7(6):565-79.