DT-Web

DB01251 - Gliquidone


Identification
Name Gliquidone
Accession Number DB01251
Type small molecule
Description Gliquidone is an anti-diabetic drug in the sulfonylurea class. It is used in the treatment of diabetes mellitus type 2. It is an ATP-dependent K+ (KATP) channel blocker. This block causes a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and eventually increases insulin release.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 527.632
Groups approved
Monoisotopic Weight 527.209006493
Pharmacology
Indication Used in the treatment of diabetes mellitus type 2.
Mechanism of action The mechanism of action of gliquidone in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Gliquidone likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


ATP-binding cassette transporter sub-family C member 8
Name ATP-binding cassette transporter sub-family C member 8
Gene Name ABCC8
Pharmacological action yes
Actions inhibitor
References
  • Gribble FM, Ashcroft FM: Sulfonylurea sensitivity of adenosine triphosphate-sensitive potassium channels from beta cells and extrapancreatic tissues. Metabolism. 2000 Oct;49(10 Suppl 2):3-6. - Pubmed
  • Harrower A: Gliclazide modified release: from once-daily administration to 24-hour blood glucose control. Metabolism. 2000 Oct;49(10 Suppl 2):7-11. - Pubmed
  • Lawrence CL, Proks P, Rodrigo GC, Jones P, Hayabuchi Y, Standen NB, Ashcroft FM: Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia. 2001 Aug;44(8):1019-25. - Pubmed
  • Reimann F, Ashcroft FM, Gribble FM: Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9. - Pubmed
  • Proks P, Reimann F, Green N, Gribble F, Ashcroft F: Sulfonylurea stimulation of insulin secretion. Diabetes. 2002 Dec;51 Suppl 3:S368-76. - Pubmed
DTHybrid score 0.4082
ATP-sensitive inward rectifier potassium channel 8
Name ATP-sensitive inward rectifier potassium channel 8
Gene Name KCNJ8
Pharmacological action yes
Actions inhibitor
References
  • Szewczyk A, Wojcik G, Lobanov NA, Nalecz MJ: The mitochondrial sulfonylurea receptor: identification and characterization. Biochem Biophys Res Commun. 1997 Jan 23;230(3):611-5. - Pubmed
  • Sato T, Costa AD, Saito T, Ogura T, Ishida H, Garlid KD, Nakaya H: Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection. J Pharmacol Exp Ther. 2006 Jan;316(1):182-8. Epub 2005 Sep 20. - Pubmed
  • Hill RA, Rudra S, Peng B, Roane DS, Bounds JK, Zhang Y, Adloo A, Lu T: Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomes. Bioorg Med Chem. 2003 May 1;11(9):2099-113. - Pubmed
DTHybrid score 0.7284

Predictions


Id Partner name Gene Name Score
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.147
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.0931
4757 Cytochrome P450 2C9 CYP2C9 0.0747
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0534
238 Peroxisome proliferator-activated receptor gamma PPARG 0.0528
748 5'-AMP-activated protein kinase catalytic subunit alpha-1 PRKAA1 0.0516
485 cGMP-inhibited 3',5'-cyclic phosphodiesterase A PDE3A 0.0461
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0329
587 Serum albumin ALB 0.0267
6144 Solute carrier family 22 member 2 SLC22A2 0.0265
6145 Solute carrier family 22 member 1 SLC22A1 0.0254
6016 Cytochrome P450 2C19 CYP2C19 0.0238
183 Vascular endothelial growth factor A VEGFA 0.023
1974 Oligopeptide transporter, kidney isoform SLC15A2 0.0228
4512 Cytochrome P450 3A4 CYP3A4 0.0222
4119 Cytochrome P450 2D6 CYP2D6 0.0221
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.022
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0202
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0188
1729 Solute carrier family 22 member 6 SLC22A6 0.0187
4924 Cytochrome P450 2C8 CYP2C8 0.0137
20 Prostaglandin G/H synthase 1 PTGS1 0.0114
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.011
521 ATP-binding cassette transporter sub-family C member 9 ABCC9 0.0108
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.01
1588 Multidrug resistance protein 1 ABCB1 0.0095
132 ATP-binding cassette sub-family A member 1 ABCA1 0.0091
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0088
3961 G protein-activated inward rectifier potassium channel 4 KCNJ5 0.0076
6106 Cytochrome P450 2C18 CYP2C18 0.0071
776 Bile salt export pump ABCB11 0.0053
2184 Cystic fibrosis transmembrane conductance regulator CFTR 0.005
738 Monocarboxylate transporter 1 SLC16A1 0.0049
340 Apoptotic protease-activating factor 1 APAF1 0.0049
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0048
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.0045
2164 Multidrug resistance-associated protein 4 ABCC4 0.0044
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0044
825 Arsenical pump-driving ATPase ASNA1 0.0043
3435 Arsenical pump-driving ATPase arsA 0.0043
2105 ATP-binding cassette sub-family G member 1 ABCG1 0.0043
510 Serine/threonine-protein kinase receptor R3 ACVRL1 0.0043
733 Activin receptor type 1B ACVR1B 0.0043
745 Anti-Muellerian hormone type-2 receptor AMHR2 0.0043
486 Serine/threonine-protein kinase ALS2CR7 CDK15 0.0043
483 A-Raf proto-oncogene serine/threonine-protein kinase ARAF 0.0043
21 Beta-adrenergic receptor kinase 2 ADRBK2 0.0043
377 Beta-adrenergic receptor kinase 1 ADRBK1 0.0043
154 AFG3-like protein 2 AFG3L2 0.0043
225 NEDD8-activating enzyme E1 regulatory subunit NAE1 0.0043
395 ALK tyrosine kinase receptor Not Available 0.0043
292 Activin receptor type-1 ACVR1 0.0038
849 Activated CDC42 kinase 1 TNK2 0.0038
704 Long-chain-fatty-acid--CoA ligase 1 ACSL1 0.0038
297 Adenylate cyclase type 1 ADCY1 0.0038
821 Acetyl-coenzyme A synthetase 2-like, mitochondrial ACSS1 0.0038
386 Acetyl-coenzyme A synthetase, cytoplasmic ACSS2 0.0038
289 Cytosolic purine 5'-nucleotidase NT5C2 0.0038
6107 Cytochrome P450 3A7 CYP3A7 0.0036
484 Tyrosine-protein kinase ABL2 ABL2 0.0035
4118 Cytochrome P450 3A5 CYP3A5 0.0034
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0033
740 Argininosuccinate synthase ASS1 0.0032
865 Argininosuccinate synthase ASS1 0.0032
2680 Argininosuccinate synthase argG 0.0032
3194 Argininosuccinate synthase argG 0.0032
6143 Solute carrier family 22 member 7 SLC22A7 0.0031
242 Asparagine synthetase [glutamine-hydrolyzing] ASNS 0.0031
476 RAC-alpha serine/threonine-protein kinase AKT1 0.0031
6021 Adenosine kinase ADK 0.003
661 ADP/ATP translocase 1 SLC25A4 0.0029
862 Multidrug resistance-associated protein 1 ABCC1 0.0029
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0026
17 Proto-oncogene tyrosine-protein kinase ABL1 ABL1 0.0025
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