General Information of Drug (ID: DMOFCRY)

Drug Name
SEROTONIN Drug Info
Synonyms
serotonin; 5-HYDROXYTRYPTAMINE; 3-(2-Aminoethyl)-1H-indol-5-ol; 50-67-9; Enteramine; 5-HT; Serotonine; Thrombotonin; Thrombocytin; Antemovis; Ds substance; Hippophain; Antemoqua; Substance DS; Substanz DS; 1H-Indol-5-ol, 3-(2-aminoethyl)-; 5-Hta; Tryptamine, 5-hydroxy-; 3-(2-Aminoethyl)indol-5-ol; Enteramin; UNII-333DO1RDJY; Indol-5-ol, 3-(2-aminoethyl)-; 5-Hydroxy-3-(beta-aminoethyl)indole; 3-(beta-Aminoethyl)-5-hydroxyindole; EINECS 200-058-9; 3-(2-Amino-ethyl)-1H-indol-5-ol; BRN 0143524; 333DO1RDJY; CHEBI:28790
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5202
ChEBI ID
CHEBI:28790
CAS Number
CAS 50-67-9
TTD Drug ID
DMOFCRY
VARIDT Drug ID
DR00189
INTEDE Drug ID
DR1961

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Inhibitor [2]
5-HT 1B receptor (HTR1B) TTK8CXU 5HT1B_HUMAN Inhibitor [3]
5-HT 1D receptor (HTR1D) TT6MSOK 5HT1D_HUMAN Inhibitor [4]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Inhibitor [2]
5-HT 2B receptor (HTR2B) TT0K1SC 5HT2B_HUMAN Inhibitor [5]
5-HT 2C receptor (HTR2C) TTWJBZ5 5HT2C_HUMAN Inhibitor [6]
5-HT 3A receptor (HTR3A) TTPC4TU 5HT3A_HUMAN Inhibitor [7]
5-HT 3B receptor (HTR3B) TTR6K75 5HT3B_HUMAN Inhibitor [7]
5-HT 4 receptor (HTR4) TT07C3Y 5HT4R_HUMAN Inhibitor [6]
5-HT 5A receptor (HTR5A) TTRUFDT 5HT5A_HUMAN Inhibitor [8]
5-HT 6 receptor (HTR6) TTJS8PY 5HT6R_HUMAN Inhibitor [9]
5-HT 7 receptor (HTR7) TTO9X1H 5HT7R_HUMAN Inhibitor [8]
Adenosine A3 receptor (ADORA3) TTJFY5U AA3R_HUMAN Inhibitor [10]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Sodium-dependent serotonin transporter (SLC6A4) DTAV4SY SC6A4_HUMAN Investigative [11]
Equilibrative nucleoside transporter 4 (SLC29A4) DT3EAQP S29A4_HUMAN Investigative [12]
Vesicular amine transporter 2 (SLC18A2) DTT7VPB VMAT2_HUMAN Investigative [13]
Vesicular amine transporter 1 (SLC18A1) DTM953D VMAT1_HUMAN Investigative [13]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Investigative [14]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Monoamine oxidase type A (MAO-A) DERE4TU AOFA_HUMAN Investigative [15]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
5-HT 2C receptor (HTR2C) DTT HTR2C 4.233 3.329 3.843 3.888
5-HT 1A receptor (HTR1A) DTT HTR1A 4.661 5.289 3.053 3.472
5-HT 3B receptor (HTR3B) DTT HTR3B 5.952 4.931 5.597 5.933
5-HT 3A receptor (HTR3A) DTT HTR3A 5.693 5.728 5.986 6.087
5-HT 7 receptor (HTR7) DTT HTR7 1.561 1.233 0.848 1.485
5-HT 1B receptor (HTR1B) DTT HTR1B 5.781 3.121 6.267 4.986
5-HT 6 receptor (HTR6) DTT HTR6 5.594 5.781 5.271 3.963
5-HT 2A receptor (HTR2A) DTT HTR2A 4.84 4.904 4.652 4.129
Adenosine A3 receptor (ADORA3) DTT ADORA3 6.57 6.966 6.564 6.787
5-HT 1D receptor (HTR1D) DTT HTR1D 3.307 1.263 2.585 5.833
5-HT 2B receptor (HTR2B) DTT HTR2B 0.485 3.536 0.379 4.667
5-HT 4 receptor (HTR4) DTT HTR4 5.776 4.945 5.062 4.828
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
Sodium-dependent serotonin transporter (SLC6A4) DTP SERT 6.278 5.469 6.075 6.966
Organic cation transporter 2 (SLC22A2) DTP `OCT2 3.766 3.548 7.303 3.548
Monoamine oxidase type A (MAO-A) DME MAOA 7.207 8.159 9.043 7.711
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 Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vesicular amine transporter 2 (SLC18A2) DTP VMAT2 1.71E-01 -6.86E-01 -8.11E-01
Vesicular amine transporter 1 (SLC18A1) DTP VMAT1 3.06E-01 -2.04E-01 -7.90E-01
Sodium-dependent serotonin transporter (SLC6A4) DTP SERT 2.81E-02 -2.78E-01 -1.13E+00
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 4.95E-01 -1.32E-01 -3.77E-01
Equilibrative nucleoside transporter 4 (SLC29A4) DTP ENT4 9.03E-01 1.44E-01 4.54E-01
Monoamine oxidase type A (MAO-A) DME MAOA 2.61E-01 -1.87E-01 -8.22E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 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: 5).
2 Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characteri... J Med Chem. 2009 Nov 12;52(21):6946-50.
3 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
4 Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-pip... J Med Chem. 2008 Jun 26;51(12):3609-16.
5 Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Bioorg Med Chem Lett. 2006 Feb;16(3):677-80.
6 Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. J Nat Prod. 2006 Oct;69(10):1421-4.
7 Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy ... J Med Chem. 1999 May 6;42(9):1556-75.
8 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. J Med Chem. 2008 Jul 24;51(14):4150-69.
9 5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists. J Med Chem. 2010 Mar 25;53(6):2521-7.
10 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
11 Serotonin transporter gene, depressive symptoms, and interleukin-6. Circ Cardiovasc Genet. 2009 Dec;2(6):614-20.
12 Autism spectrum disorder associated with low serotonin in CSF and mutations in the SLC29A4 plasma membrane monoamine transporter (PMAT) gene. Mol Autism. 2014 Aug 13;5:43.
13 SLC18: Vesicular neurotransmitter transporters for monoamines and acetylcholine. Mol Aspects Med. 2013 Apr-Jun;34(2-3):360-72.
14 Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
15 Do monomeric vs dimeric forms of MAO-A make a difference? A direct comparison of the catalytic properties of rat and human MAO-A's. J Neural Transm (Vienna). 2007;114(6):721-4.