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

Stem definition	Drug id	CAS RN
diazepam derivatives	809	2886-65-9

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

desalkylflurazepam
dealkylflurazepam
descarbethoxyloflazepate
norfludiazepam
norflurazepam
norflutoprazepam

Molecular weight: 288.71
Formula: C15H10ClFN2O
CLOGP: 2.81
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 41.46
ALOGS: -4.19
ROTB: 1

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.21 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1968	YEAR INTRODUCED

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
CHEBI has role	CHEBI:35474	anti-anxiety agents
CHEBI has role	CHEBI:35623	anticonvulsants
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:91016	GABAA receptor agonists

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	11.63	acidic
pKa2	2.85	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
GABA-A receptor alpha-1/beta-2/gamma-2	Ion channel	P14867 P18507 P47870	GBRA1_HUMAN GBRG2_HUMAN GBRB2_HUMAN		IC50	8.70		WOMBAT-PK

External reference:

ID	Source
C0484961	UMLSCUI
CHEBI:143439	CHEBI
CHEMBL1201372	ChEMBL_ID
C020965	MESH_SUPPLEMENTAL_RECORD_UI
115558004	SNOMEDCT_US
4540	PUBCHEM_CID
X9U41NXR6M	UNII

Pharmaceutical products:

None