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pentagastrin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2088 | 5534-95-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.066 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.207 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.219 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.281 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 22.380 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 19.560 | % | High | 1 |
| herg | hERG pIC50 | 4.163 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 24.266 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 13.677 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 19.890 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,ZAP70 | 35 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.005 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 98.401 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 15.070 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.791 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.720 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 78.343 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 57.430 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 14.810 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 653.131 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 26, 1974 | FDA |
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 | V04CG04 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for gastric secretion |
Related Drugs by ATC class:
V04CG Tests for gastric secretion 5 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 | 3.79 | acidic |
| pKa2 | 12.72 | acidic |
| pKa3 | 13.16 | acidic |
| pKa4 | 13.54 | acidic |
| pKa5 | 13.97 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Gastrin/cholecystokinin type B receptor | GPCR | Ki | 7.84 | CHEMBL | |||||
| Cholecystokinin receptor type A | GPCR | IC50 | 6.22 | CHEMBL | |||||
| Gastrin/cholecystokinin type B receptor | GPCR | IC50 | 8.17 | CHEMBL | |||||
| Gastrin/cholecystokinin type B receptor | GPCR | IC50 | 9.10 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018500 | VUID |
| N0000146822 | NUI |
| D01631 | KEGG_DRUG |
| 4018500 | VANDF |
| C0030859 | UMLSCUI |
| CHEBI:31974 | CHEBI |
| CHEMBL1328 | ChEMBL_ID |
| D010418 | MESH_DESCRIPTOR_UI |
| DB00183 | DRUGBANK_ID |
| 870 | IUPHAR_LIGAND_ID |
| 2387 | INN_ID |
| EF0NX91490 | UNII |
| 9853654 | PUBCHEM_CID |
| 204262 | RXNORM |
| 2234 | MMSL |
| 5249 | MMSL |
| d04022 | MMSL |
| 001146 | NDDF |
| 10782005 | SNOMEDCT_US |
| 358180008 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pentagastrin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51808-207 | SOLUTION | 250 ug | INTRAVENOUS | Unapproved drug other | 6 sections |