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indoramin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1443 | 26844-12-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 24 % | 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,ALK,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 46 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,EIF2AK3,GRK2,PRKCD,SIK2,SIK3,STK33 | 9 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1981 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Lower urinary tract symptoms | 36.60 | 32.24 | 3 | 3 | 111 | 90628330 |
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 | C02CA02 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Alpha-adrenoreceptor antagonists |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D058668 | Adrenergic alpha-1 Receptor Antagonists |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Related Drugs by ATC class:
C02CA Alpha-adrenoreceptor antagonists 4 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 | 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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 |
| 0Z802HMY7H | INXIGHT DRUGS |
Pharmaceutical products:
None