Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H21N3O3S |
| Molecular Weight | 323.411 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2C[C@@H]3CCC[C@@H]3C2
InChI
InChIKey=BOVGTQGAOIONJV-BETUJISGSA-N
InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)/t12-,13+
| Molecular Formula | C15H21N3O3S |
| Molecular Weight | 323.411 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.medicines.org.uk/emc/medicine/31089Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68005907 | https://www.drugs.com/cons/gliclazide.html
Sources: http://www.medicines.org.uk/emc/medicine/31089
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68005907 | https://www.drugs.com/cons/gliclazide.html
Gliclazide (BILXONA®) is an oral sulfonylurea hypoglycemic agent which is used in type 2 diabetes to stimulate insulin production. It differs from other related compounds by an N-containing heterocyclic ring with an endocyclic bond. Gliclazide (BILXONA®) reduces blood glucose levels by stimulating insulin secretion from the beta-cells of the islets of Langerhans. Increase in postprandial insulin and C-peptide secretion persists after two years of treatment. In addition to these metabolic properties, Gliclazide (BILXONA®) has haemovascular properties. It is not available for sale in the United States.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23671878
Curator's Comment: Known to be CNS penetrant in rat. Human data not available.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 3.0 mM [Ki] | |||
Target ID: CHEMBL1944490 Sources: https://www.drugbank.ca/drugs/DB01120 |
50.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | BILXONA Approved UseNon insulin-dependent diabetes (type 2) in adults when dietary measures, physical exercise and weight loss alone are not sufficient to control blood glucose. Launch Date2015 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.6 μg/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2.2 μg/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.6 μg/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4.3 μg/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2.8 μg/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.5 μg/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7.7 μg/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4 μg/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
6.3 μg/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
23.6 μg × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
55.65 μg × h/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
37.2 μg × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
71.8 μg × h/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
92.5 μg × h/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
8.6 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12.3 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
9.6 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
9.1 h |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
12.3 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.6 h |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
11.4 h |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
11.8 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
|
20.5 h |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE unknown | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
8% |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9% |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
7% |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
GLICLAZIDE serum | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
6.3% |
GLICLAZIDE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
||
5% |
GLICLAZIDE plasma | Homo sapiens |
||
5% |
GLICLAZIDE plasma | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
Disc. AE: Metabolic acidosis, Vomiting... AEs leading to discontinuation/dose reduction: Metabolic acidosis (grade 3-4) Sources: Vomiting Abdominal pain (grade 3) Hypoglycaemia Encephalopathy Acute kidney injury Haemodynamic instability (grade 3) Distributive shock (grade 3) |
1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
Disc. AE: Hepatitis, Hemiplegia... AEs leading to discontinuation/dose reduction: Hepatitis Sources: Hemiplegia (grade 3) Dysphasia Lethargy Tonic-clonic convulsion Consciousness abnormal Stupor |
198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Other AEs: Hypoglycaemia, Diarrhoea... Other AEs: Hypoglycaemia (10.1%) Sources: Diarrhoea (3.4%) Nausea (5.1%) Oedema (4.5%) Dizziness (6.5%) Headache (8.9%) Hypertension (3.8%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Acute kidney injury | Disc. AE | 2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Encephalopathy | Disc. AE | 2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Hypoglycaemia | Disc. AE | 2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Vomiting | Disc. AE | 2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Metabolic acidosis | grade 3-4 Disc. AE |
2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Abdominal pain | grade 3 Disc. AE |
2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Distributive shock | grade 3 Disc. AE |
2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Haemodynamic instability | grade 3 Disc. AE |
2.1 g single, oral Overdose |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
| Consciousness abnormal | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Dysphasia | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hepatitis | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Lethargy | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Stupor | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Tonic-clonic convulsion | Disc. AE | 1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hemiplegia | grade 3 Disc. AE |
1200 mg single, oral Overdose Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: |
| Hypoglycaemia | 10.1% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Diarrhoea | 3.4% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Hypertension | 3.8% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Oedema | 4.5% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Nausea | 5.1% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Dizziness | 6.5% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Headache | 8.9% | 198 mg 1 times / day multiple, oral Recommended Dose: 198 mg, 1 times / day Route: oral Route: multiple Dose: 198 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Phosphatidylinositol 3-kinase activation is required for sulfonylurea stimulation of glucose transport in rat skeletal muscle. | 2004-02 |
|
| Effects of rosiglitazone maleate when added to a sulfonylurea regimen in patients with type 2 diabetes mellitus and mild to moderate renal impairment: a post hoc analysis. | 2003-11 |
|
| Comparison of repaglinide vs. gliclazide in combination with bedtime NPH insulin in patients with Type 2 diabetes inadequately controlled with oral hypoglycaemic agents. | 2003-11 |
|
| Genetic cause of hyperglycaemia and response to treatment in diabetes. | 2003-10-18 |
|
| [Medication of the month. Gliclazide modified release (Uni Diamicron)]. | 2003-10 |
|
| Risk of hypoglycaemia with oral antidiabetic agents in patients with Type 2 diabetes. | 2003-10 |
|
| Monotherapy of type 2 diabetes with once-daily gliclazide modified release in primary care. | 2003-10 |
|
| Effect of rifampin on the pharmacokinetics and pharmacodynamics of gliclazide. | 2003-10 |
|
| Reflex epilepsy and non-ketotic hyperglycemia. | 2003-09 |
|
| Gliclazide modified release: A critical review of pharmacodynamic, metabolic, and vasoprotective effects. | 2003-08 |
|
| Benefits of gliclazide in the atherosclerotic process: decrease in monocyte adhesion to endothelial cells. | 2003-08 |
|
| Pharmacokinetic and pharmacodynamic characterization of gliclazide in healthy volunteers. | 2003-07 |
|
| The application of the convective diffusion model and the film equilibrium model to surfactant-facilitated dissolution of gliclazide. | 2003-07 |
|
| Bioequivalence study of generic gliclazide and Diamicron formulations in healthy Thai male volunteers. | 2003-07 |
|
| Sulfonylureas and cardiovascular effects: from experimental data to clinical use. Available data in humans and clinical applications. | 2003-06 |
|
| Diabetes and vascular disease: a new international trial. | 2003-06 |
|
| Comparison of the micro- and macro-vascular effects of glimepiride and gliclazide in metformin-treated patients with Type 2 diabetes: a double-blind, crossover study. | 2003-06 |
|
| Functional involvement of sulphonylurea receptor (SUR) type 1 and 2B in the activity of pig urethral ATP-sensitive K+ channels. | 2003-06 |
|
| Upregulation of cyclooxygenase-2 is accompanied by increased expression of nuclear factor-kappa B and I kappa B kinase-alpha in human colorectal cancer epithelial cells. | 2003-05-19 |
|
| Spectrofluorimetric and spectrophotometric determination of gliclazide in pharmaceuticals by derivatization with 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole. | 2003-05-02 |
|
| Urinary PC-1 and N-acetyl-beta-D-glucosaminidase activity in patients with type 2 diabetes treated with metformin, gliclazide or glibenclamide. | 2003-05 |
|
| Study of the solubilization of gliclazide by aqueous micellar solutions. | 2003-04 |
|
| Gliclazide protects pancreatic beta-cells from damage by hydrogen peroxide. | 2003-03-28 |
|
| Monocyte matrix metalloproteinase production in Type 2 diabetes and controls--a cross sectional study. | 2003-03-10 |
|
| Diabetic endothelial dysfunction: effect of free radical scavenging in Type 2 diabetic patients. | 2003-03-08 |
|
| Monocyte adhesion in diabetic angiopathy: effects of free-radical scavenging. | 2003-03-08 |
|
| Differential selectivity of insulin secretagogues: mechanisms, clinical implications, and drug interactions. | 2003-03-08 |
|
| Effects of sulfonylureas on K(ATP) channel-dependent vasodilation. | 2003-03-08 |
|
| A simple and sensitive HPLC method for determination of gliclazide in human serum. | 2003-03-05 |
|
| Severe relapsing sulphonylurea-induced hypoglycaemia: a diagnostic and therapeutic challenge. | 2003-02 |
|
| Diabetes mellitus and weight control: differences of respiratory quotient in type 2 diabetic obese subjects receiving sulfonylureas and non-diabetic obese controls. | 2003-02 |
|
| Differential effects of sulphonylureas on the vasodilatory response evoked by K(ATP) channel openers. | 2003-02 |
|
| Population PKPD modelling of the long-term hypoglycaemic effect of gliclazide given as a once-a-day modified release (MR) formulation. | 2003-02 |
|
| Effects of inhibition of ATP-sensitive potassium channels on metabolic vasodilation in the human forearm. | 2003-01 |
|
| [A 50-year history of new drugs in Japan-the development and progress of anti-diabetic drugs and the epidemiological aspects of diabetes mellitus]. | 2003 |
|
| Addition of rosiglitazone to existing sulfonylurea treatment in chinese patients with type 2 diabetes and exposure to hepatitis B or C. | 2003 |
|
| The mechanisms of inhibitory actions of gliclazide on neutrophils-endothelial cells adhesion and surface expression of endothelial adhesion molecules mediated by a high glucose concentration. | 2002-12-31 |
|
| Effect of ethanolic extract of Embelia ribes on dyslipidemia in diabetic rats. | 2002-12-03 |
|
| High-frequency insulin pulsatility and type 2 diabetes: from physiology and pathophysiology to clinical pharmacology. | 2002-12 |
|
| [Molecular mechanisms of insulin secretion]. | 2002-12 |
|
| Hypoglycaemic activity of Alpinia galanga rhizome and its extracts in rabbits. | 2002-12 |
|
| Combination therapy of alpha-glucosidase inhibitor and a sulfonylurea compound prolongs the duration of good glycemic control. | 2002-12 |
|
| Gliclazide directly inhibits arginine-induced glucagon release. | 2002-12 |
|
| Interaction of the cytosolic domains of the Kir6.2 subunit of the K(ATP) channel is modulated by sulfonylureas. | 2002-12 |
|
| Sulfonylurea stimulation of insulin secretion. | 2002-12 |
|
| Effect of gliclazide on islet transplants. | 2002-11 |
|
| Remodelling of zero-stress state of small intestine in streptozotocin-induced diabetic rats. Effect of gliclazide. | 2002-10 |
|
| Gateways to Clinical Trials. | 2002-09 |
|
| Oral hypoglycaemic agent failure. | 2002-07 |
|
| [Effects of gliclazide on blood rheology of diabetes Wistar rat]. | 2001-06 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.medicines.org.uk/emc/medicine/31089
The daily dose may vary from 1 to 4 tablets per day, i.e. from 30 to 120 mg taken orally in a single intake at breakfast time.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11484080
Gliclazide blocked whole-cell murine beta-cell Katp currents with an IC50 of 184 +/- 30 nmol/l (n = 6-10) but was much less effective in rat cardiac and smooth muscle (IC50s of 19.5 +/- 5.4 micromol/l (n = 6-12) and 37.9 +/- 1.0 micromol/l (n = 5-10), respectively). In all three tissues, the action of the drug on whole-cell Katp currents was rapidly reversible. In inside-out patches on beta-cells, gliclazide (1 micromol/l) produced a maximum of 66 +/- 13 % inhibition (n = 5), compared with more than 98 % block in the whole-cell configuration.
| Substance Class |
Chemical
Created
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admin
on
Edited
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| Record UNII |
G4PX8C4HKV
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Validated (UNII)
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NCI_THESAURUS |
C97936
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WHO-VATC |
QA10BB09
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WHO-ATC |
A10BB09
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DB01120
Created by
admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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3056
Created by
admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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m5744
Created by
admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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CHEMBL427216
Created by
admin on Mon Mar 31 19:40:52 GMT 2025 , Edited by admin on Mon Mar 31 19:40:52 GMT 2025
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TRANSPORTER -> SUBSTRATE |
Compared with the OATP1B1*1a, mutants OATP1B1*5 and OATP1B1*15 showed significantly decreased transport capacity.
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METABOLIC ENZYME -> SUBSTRATE |
Clearance of gliclazide in CYP2C9*2 and *3 was significantly reduced compared to the wild-type.
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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IMPURITY -> PARENT |
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ACTIVE MOIETY |
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