indoramin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1443 26844-12-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Wy21901
  • Wy 21901
  • Wy-21901
  • indoramin
  • indoramine
An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.
  • Molecular weight: 347.46
  • Formula: C22H25N3O
  • CLOGP: 2.84
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 48.13
  • ALOGS: -4.60
  • ROTB: 5

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.22 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 18 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 4.90 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 20 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.15 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.30 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1981 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Lower urinary tract symptoms 38.07 31.50 3 3 46 63488970

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02CA02 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING
Alpha-adrenoreceptor antagonists
MeSH PA D018663 Adrenergic Agents
MeSH PA D058668 Adrenergic alpha-1 Receptor Antagonists
MeSH PA D000317 Adrenergic alpha-Antagonists
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents

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

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.08 acidic
pKa2 13.42 acidic
pKa3 7.43 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
Alpha-2A adrenergic receptor GPCR Ki 5.65 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 8.43 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 6.28 CHEMBL
Alpha-2C adrenergic receptor GPCR Ki 6.32 CHEMBL
D(4) dopamine receptor GPCR Ki 7.75 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 6.96 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 7.60 CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 6.21 CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 7.92 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 4.92 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 7.61 CHEMBL

External reference:

IDSource
N0000167199 NUI
D04531 KEGG_DRUG
C0021252 UMLSCUI
CHEBI:135470 CHEBI
CHEMBL279516 ChEMBL_ID
DB08950 DRUGBANK_ID
D007217 MESH_DESCRIPTOR_UI
33625 PUBCHEM_CID
501 IUPHAR_LIGAND_ID
3064 INN_ID
0Z802HMY7H UNII
5784 RXNORM
003737 NDDF
349913001 SNOMEDCT_US
395748009 SNOMEDCT_US

Pharmaceutical products:

None