cyclothiazide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
diuretics, chlorothiazide derivatives 761 2259-96-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cyclothiazide
  • ciclotiazide
inhibits the desensitization of AMPA-type receptors; structure
  • Molecular weight: 389.87
  • Formula: C14H16ClN3O4S2
  • CLOGP: 1.98
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 118.36
  • ALOGS: -3.15
  • ROTB: 2

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
5 mg O
5 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 8, 1982 FDA PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C03AA09 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides, plain
ATC C03AB09 CARDIOVASCULAR SYSTEM
DIURETICS
LOW-CEILING DIURETICS, THIAZIDES
Thiazides and potassium in combination
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004232 Diuretics
MeSH PA D045283 Natriuretic Agents
CHEBI has role CHEBI:35498 diuretics
CHEBI has role CHEBI:35674 antihypertensive

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.89 acidic
pKa2 11.0 acidic
pKa3 1.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Solute carrier family 12 member 3 Transporter INHIBITOR CHEMBL CHEMBL
Glutamate receptor 2 Ion channel EC50 5.65 CHEMBL
Glutamate receptor 1 Ion channel EC50 5.70 CHEMBL
Glutamate receptor 3 Ion channel ALLOSTERIC MODULATOR EC50 4.86 IUPHAR
Glutamate receptor 4 Ion channel ALLOSTERIC MODULATOR EC50 5.41 IUPHAR
Glutamate receptor ionotropic, AMPA Ion channel IC50 5.21 CHEMBL

External reference:

IDSource
4017504 VUID
N0000145889 NUI
D01256 KEGG_DRUG
4017504 VANDF
C0056831 UMLSCUI
CHEBI:31448 CHEBI
CYZ PDB_CHEM_ID
CHEMBL61593 ChEMBL_ID
DB00606 DRUGBANK_ID
C004639 MESH_SUPPLEMENTAL_RECORD_UI
2910 PUBCHEM_CID
4167 IUPHAR_LIGAND_ID
1138 INN_ID
P71U09G5BW UNII
22033 RXNORM
002304 NDDF
37006008 SNOMEDCT_US

Pharmaceutical products:

None