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rescinnamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| derivatives of Rauwolfia alkaloids | 2369 | 24815-24-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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 | 3.299 | High | 0.81 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.838 | High | 0.81 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 38.905 | 10^-6 cm/s | High | 0.81 |
| dh-clint | Dog hepatocyte intrinsic clearance | 46.559 | uL/min/10^6 cells | High | 0.81 |
| dppb | Dog plasma protein binding (% unbound) | 4.030 | % | High | 0.81 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 11.090 | % | High | 0.81 |
| herg | hERG pIC50 | 5.146 | pIC50 | High | 0.81 |
| hh-clint | Human hepatocyte intrinsic clearance | 88.512 | uL/min/10^6 cells | High | 0.81 |
| hlm-clint | Human liver microsomal intrinsic clearance | 144.544 | uL/min/mg protein | High | 0.81 |
| hppb | Human plasma protein binding (% unbound) | 3.260 | % | High | 0.81 |
| kinase-safety-class | ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK,ZAP70 | 43 | |||
| kinase-selectivity-class | AXL,ERBB2,GRK2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.483 | High | 0.81 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 183.231 | High | 0.81 | |
| mppb | Mouse plasma protein binding (% unbound) | 5 | High | 0.81 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.194 | High | 0.81 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.110 | % | High | 0.81 |
| rh-clint | Rat hepatocyte intrinsic clearance | 248.886 | uL/min/10^6 cells | High | 0.81 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 35.830 | % | High | 0.81 |
| rppb | Rat plasma protein binding (% unbound) | 2.920 | % | High | 0.81 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 8.453 | uM | High | 0.81 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 31, 1956 | FDA | PFIZER |
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 | C02AA01 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Rauwolfia alkaloids |
| ATC | C02LA02 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Rauwolfia alkaloids and diuretics in combination |
| ATC | C02LA52 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Rauwolfia alkaloids and diuretics in combination |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Related Drugs by ATC class:
C02AA Rauwolfia alkaloids 4 drugs
C02LA Rauwolfia alkaloids and diuretics in combination 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 | 11.2 | acidic |
| pKa2 | 6.9 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Synaptic vesicular amine transporter | Transporter | INHIBITOR | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018628 | VUID |
| N0000146941 | NUI |
| D00198 | KEGG_DRUG |
| 4018628 | VANDF |
| C0035167 | UMLSCUI |
| CHEBI:28572 | CHEBI |
| CHEMBL1668 | ChEMBL_ID |
| DB01180 | DRUGBANK_ID |
| C084826 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7098 | IUPHAR_LIGAND_ID |
| 683 | INN_ID |
| Q6W1F7DJ2D | UNII |
| 5280954 | PUBCHEM_CID |
| 9259 | RXNORM |
| 000643 | NDDF |
| 2927004 | SNOMEDCT_US |
Pharmaceutical products:
None