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pinacidil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 2173 | 60560-33-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.91 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 57 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.68 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.60 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.50 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.04 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.041 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.413 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 38.994 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.644 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 56.690 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 62.510 | % | High | 1 |
| herg | hERG pIC50 | 4.326 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.280 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.217 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 52.190 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,MAP3K21,MAPK7,MARK4,NTRK2,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 32 | |||
| kinase-selectivity-class | GRK2,PDK4 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.295 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.754 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 63.530 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 10.641 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 54.590 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.831 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.480 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 64.110 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 877.001 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | LEO PHARM |
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 | C02DG01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON Guanidine derivatives |
| ATC | C02LX01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Other antihypertensives and diuretics |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.09 | Basic |
| pKa2 | 0.0 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sulfonylurea receptor 2, Kir6.2 | Ion channel | OPENER | Ki | 6.49 | CHEMBL | CHEMBL | |||
| ATP-binding cassette sub-family C member 9 | Ion channel | EC50 | 5.45 | CHEMBL | |||||
| Calcium-activated potassium channel subunit alpha-1 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4025256 | VUID |
| N0000171786 | NUI |
| D05482 | KEGG_DRUG |
| 4025256 | VANDF |
| C0071074 | UMLSCUI |
| CHEBI:34923 | CHEBI |
| CHEMBL1200338 | ChEMBL_ID |
| DB06762 | DRUGBANK_ID |
| CHEMBL1159 | ChEMBL_ID |
| D020110 | MESH_DESCRIPTOR_UI |
| 55329 | PUBCHEM_CID |
| 2412 | IUPHAR_LIGAND_ID |
| 7B0ZZH8P2W | UNII |
| 33717 | RXNORM |
| 003753 | NDDF |
| 003777 | NDDF |
| 85371-64-8 | SECONDARY_CAS_RN |
| 7B0ZZH8P2W | INXIGHT DRUGS |
Pharmaceutical products:
None