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

Stem definition	Drug id	CAS RN
diuretics, chlorothiazide derivatives	761	2259-96-3

Description:

Molecule

Description

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:

Dose	Unit	Route
5	mg	O
5	mg	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.28 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
June 8, 1982	FDA	PHARMACIA AND UPJOHN

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Solute carrier family 12 member 3	Transporter	P55017	S12A3_HUMAN	INHIBITOR				CHEMBL	CHEMBL
Glutamate receptor 1	Ion channel	P42261	GRIA1_HUMAN		EC50	5.70		CHEMBL
Glutamate receptor 2	Ion channel	P42262	GRIA2_HUMAN		EC50	5.65		CHEMBL
Glutamate receptor 4	Ion channel	P48058	GRIA4_HUMAN	ALLOSTERIC MODULATOR	EC50	5.41		IUPHAR
Glutamate receptor 3	Ion channel	P42263	GRIA3_HUMAN	ALLOSTERIC MODULATOR	EC50	4.86		IUPHAR
Glutamate receptor ionotropic, AMPA	Ion channel		GRIA1_RAT GRIA2_RAT GRIA3_RAT GRIA4_RAT		IC50	5.21		CHEMBL

External reference:

ID	Source
4017504	VUID
N0000145889	NUI
D01256	KEGG_DRUG
22033	RXNORM
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
002304	NDDF
37006008	SNOMEDCT_US

Pharmaceutical products:

None