General Information of Drug (ID: DM6SFYH)

Drug Name
[14C]TEA Drug Info
Synonyms
Tetraethylammonium; Tetrylammonium; TETRAETHYLAMMONIUM ION; Tetramon; tetraethylazanium; N,N,N-Triethylethanaminium; tetraethylamine; UNII-5AV7G7EIEE; Tetraetilammonio [Italian]; 66-40-0; 5AV7G7EIEE; BRN 1738225; CHEMBL9324; AMMONIUM, TETRAETHYL-; CHEBI:44296; C8H20N; Tetraetilammonio; [14C]-TEA; tetraethyl ammonium; AC1L1KAW; Lopac-T-2265; 77-98-5 (hydroxide); 71-91-0 (bromide); 56-34-8 (chloride); 68-05-3 (iodide); SCHEMBL16267; 4-04-00-00331 (Beilstein Handbook Reference); NEt4(+); GTPL4575; GTPL2343; Ethanaminium,; [14C]-TEA ; tetraethylammonium
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5413
ChEBI ID
CHEBI:44296
CAS Number
CAS 66-40-0
TTD Drug ID
DM6SFYH
VARIDT Drug ID
DR00106

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Aquaporin-1 (AQP1) TTSF1KH AQP1_HUMAN Inhibitor [2]
Calcium-activated potassium channel KCa2.1 (KCNN1) TT9R6BE KCNN1_HUMAN Blocker (channel blocker) [3]
Calcium-activated potassium channel KCa2.2 (KCNN2) TT2T5M0 KCNN2_HUMAN Blocker (channel blocker) [3]
Calcium-activated potassium channel KCa2.3 (KCNN3) TT9JH25 KCNN3_HUMAN Blocker (channel blocker) [3]
Calcium-activated potassium channel KCa4.1 (KCNT1) TTGJFK1 KCNT1_HUMAN Blocker (channel blocker) [4]
Calcium-activated potassium channel KCa4.2 (KCNT2) TTLU5FO KCNT2_HUMAN Blocker (channel blocker) [5]
Calcium-activated potassium channel KCa5.1 (KCNU1) TTI9XK6 KCNU1_HUMAN Blocker (channel blocker) [6]
Charybdotoxin receptor beta-4 (BKbeta4) TT1AQ50 KCMB4_HUMAN Inhibitor [7]
Inward rectifier potassium channel Kir2.3 (KCNJ4) TTXF0ZW KCNJ4_HUMAN Blocker (channel blocker) [8]
Multidrug and toxin extrusion protein 2 (MATE2) TT7HXSL S47A2_HUMAN Modulator [9]
Solute carrier family 47 member 1 (SLC47A1) TTMHCGA S47A1_HUMAN Modulator [10]
Transient receptor potential cation channel V2 (TRPV2) TTBECWA TRPV2_HUMAN Blocker (channel blocker) [11]
Voltage-gated potassium channel Kv1.1 (KCNA1) TTS3DIK KCNA1_HUMAN Blocker (channel blocker) [12]
Voltage-gated potassium channel Kv1.2 (KCNA2) TTVFB0O KCNA2_HUMAN Blocker (channel blocker) [12]
Voltage-gated potassium channel Kv1.3 (KCNA3) TTY3UE6 KCNA3_HUMAN Blocker (channel blocker) [12]
Voltage-gated potassium channel Kv1.5 (KCNA5) TTW0CMT KCNA5_HUMAN Blocker (channel blocker) [12]
Voltage-gated potassium channel Kv1.6 (KCNA6) TTJ2W69 KCNA6_HUMAN Blocker (channel blocker) [13]
Voltage-gated potassium channel Kv1.7 (KCNA7) TTCVBT7 KCNA7_HUMAN Blocker (channel blocker) [14]
Voltage-gated potassium channel Kv1.8 (KCNA10) TTT4Y0X KCA10_HUMAN Blocker (channel blocker) [15]
Voltage-gated potassium channel Kv2.1 (KCNB1) TT5OEKU KCNB1_HUMAN Blocker (channel blocker) [16]
Voltage-gated potassium channel Kv2.2 (KCNB2) TT5PFNG KCNB2_HUMAN Blocker (channel blocker) [17]
Voltage-gated potassium channel Kv3.1 (KCNC1) TTVUWHQ KCNC1_HUMAN Blocker (channel blocker) [12]
Voltage-gated potassium channel Kv3.2 (KCNC2) TTGK3ZO KCNC2_HUMAN Blocker (channel blocker) [18]
Voltage-gated potassium channel Kv3.3 (KCNC3) TTALSY9 KCNC3_HUMAN Blocker (channel blocker) [19]
Voltage-gated potassium channel Kv3.4 (KCNC4) TTODZF1 KCNC4_HUMAN Blocker (channel blocker) [20]
Voltage-gated potassium channel Kv4.1 (KCND1) TT4DI0J KCND1_HUMAN Blocker (channel blocker) [21]
Voltage-gated potassium channel Kv7.2 (KCNQ2) TTPXI3S KCNQ2_HUMAN Blocker (channel blocker) [22]
Voltage-gated potassium channel Kv7.3 (KCNQ3) TTIVDM3 KCNQ3_HUMAN Blocker (channel blocker) [23]
Voltage-gated potassium channel Kv7.4 (KCNQ4) TT8HGRW KCNQ4_HUMAN Blocker (channel blocker) [24]
Voltage-gated potassium channel Kv7.5 (KCNQ5) TTWVL5Q KCNQ5_HUMAN Blocker (channel blocker) [25]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic cation/carnitine transporter 1 (SLC22A4) DT2EG60 S22A4_HUMAN Phase 2 [26]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Phase 2 [27]
Multidrug and toxin extrusion protein 2 (SLC47A2) DT3TX4H S47A2_HUMAN Phase 2 [28]
Multidrug and toxin extrusion protein 1 (SLC47A1) DTZGT0P S47A1_HUMAN Phase 2 [29]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Phase 2 [30]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Voltage-gated potassium channel Kv1.5 (KCNA5) DTT KCNA5 5.533 4.459 2.907 2.868
Voltage-gated potassium channel Kv7.3 (KCNQ3) DTT KCNQ3 4.912 5.057 3.459 6.135
Voltage-gated potassium channel Kv7.4 (KCNQ4) DTT KCNQ4 2.766 3.104 3.678 2.585
Calcium-activated potassium channel KCa2.2 (KCNN2) DTT KCNN2 5.34 4.233 1.485 2.536
Multidrug and toxin extrusion protein 1 (SLC47A1) DTP MATE1 8.272 1.766 7.501 1.202
Organic cation transporter 1 (SLC22A1) DTP `OCT1 10.261 4.162 4.07 3.797
Organic cation transporter 2 (SLC22A2) DTP `OCT2 3.766 3.548 7.303 3.548
Organic cation/carnitine transporter 1 (SLC22A4) DTP OCTN1 5.517 5.725 7.443 7.062
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
Multidrug and toxin extrusion protein 1 (SLC47A1) DTP MATE1 7.26E-02 -7.73E-01 -1.16E+00
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 5.44E-01 1.29E-01 3.80E-01
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 4.95E-01 -1.32E-01 -3.77E-01
Multidrug and toxin extrusion protein 2 (SLC47A2) DTP MATE2 5.64E-01 -1.09E-01 -1.98E-01
Organic cation/carnitine transporter 1 (SLC22A4) DTP OCTN1 3.41E-01 -7.96E-02 -1.50E-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: 4575).
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. (Target id: 688).
3 Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55.
4 For K+ channels, Na+ is the new Ca2+. Trends Neurosci. 2005 Aug;28(8):422-8.
5 Opposite regulation of Slick and Slack K+ channels by neuromodulators. J Neurosci. 2006 May 10;26(19):5059-68.
6 Block of mouse Slo1 and Slo3 K+ channels by CTX, IbTX, TEA, 4-AP and quinidine. Channels (Austin). 2010 Jan-Feb;4(1):22-41.
7 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. (Target id: 380).
8 Cloning and expression of a novel human brain inward rectifier potassium channel. J Biol Chem. 1994 Aug 12;269(32):20468-74.
9 Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71.
10 Molecular cloning, functional characterization and tissue distribution of rat H+/organic cation antiporter MATE1. Pharm Res. 2006 Aug;23(8):1696-701.
11 Pharmacological characterization and molecular determinants of the activation of transient receptor potential V2 channel orthologs by 2-aminoethoxy... Mol Pharmacol. 2007 Nov;72(5):1258-68.
12 Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines. Mol Pharmacol. 1994 Jun;45(6):1227-34.
13 Cloning and expression of a human voltage-gated potassium channel. A novel member of the RCK potassium channel family. EMBO J. 1990 Jun;9(6):1749-56.
14 Characterisation of the human voltage-gated potassium channel gene, KCNA7, a candidate gene for inherited cardiac disorders, and its exclusion as cause of progressive familial heart block I (PFHBI). Eur J Hum Genet. 2002 Jan;10(1):36-43.
15 KCNA10: a novel ion channel functionally related to both voltage-gated potassium and CNG cation channels. Am J Physiol Renal Physiol. 2000 Jun;278(6):F1013-21.
16 Modulation of Kv2.1 channel gating and TEA sensitivity by distinct domains of SNAP-25. Biochem J. 2006 Jun 1;396(2):363-9.
17 Molecular identification of a component of delayed rectifier current in gastrointestinal smooth muscles. Am J Physiol. 1998 May;274(5 Pt 1):G901-11.
18 Gating, modulation and subunit composition of voltage-gated K(+) channels in dendritic inhibitory interneurones of rat hippocampus. J Physiol. 2002 Jan 15;538(Pt 2):405-19.
19 Cloning of ShIII (Shaw-like) cDNAs encoding a novel high-voltage-activating, TEA-sensitive, type-A K+ channel. Proc Biol Sci. 1992 Apr 22;248(1321):9-18.
20 Characterization of a Shaw-related potassium channel family in rat brain. EMBO J. 1992 Jul;11(7):2473-86.
21 Endogenous Kv channels in human embryonic kidney (HEK-293) cells. Mol Cell Biochem. 2002 Sep;238(1-2):69-79.
22 Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol Pharmacol. 2000 Sep;58(3):591-600.
23 Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels. Br J Pharmacol. 2000 Feb;129(3):413-5.
24 Homomeric and heteromeric assembly of KCNQ (Kv7) K+ channels assayed by total internal reflection fluorescence/fluorescence resonance energy transfer and patch clamp analysis. J Biol Chem. 2008 Nov 7;283(45):30668-76.
25 KCNQ5, a novel potassium channel broadly expressed in brain, mediates M-type currents. J Biol Chem. 2000 Aug 4;275(31):24089-95.
26 Functional effects of protein sequence polymorphisms in the organic cation/ergothioneine transporter OCTN1 (SLC22A4). Pharmacogenet Genomics. 2007 Sep;17(9):773-82.
27 Involvement of human organic cation transporter 1 in the hepatic uptake of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel, small molecule survivin suppressant. Drug Metab Dispos. 2009 Sep;37(9):1856-63.
28 Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71.
29 A human transporter protein that mediates the final excretion step for toxic organic cations. Proc Natl Acad Sci U S A. 2005 Dec 13;102(50):17923-8.
30 Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes. Biochim Biophys Acta. 1999 Mar 4;1417(2):224-31.