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strychnine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2484 | 57-24-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.450 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 9.441 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 8.318 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.858 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 50.520 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 57.880 | % | High | 1 |
| herg | hERG pIC50 | 4.738 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.155 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 29.107 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 34.260 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,NTRK2,PDK1,PDK4,PRKDC,TGFBR1 | 19 | |||
| kinase-selectivity-class | EIF2AK3 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.204 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.204 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 41.900 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 36.475 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 68.280 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 8.872 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 81.880 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 30.930 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 837.529 | uM | High | 1 |
Approvals:
None
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 |
|---|---|---|
| MeSH PA | D000697 | Central Nervous System Stimulants |
| MeSH PA | D003292 | Convulsants |
| MeSH PA | D011042 | Poisons |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018684 | Glycine Agents |
| CHEBI has role | CHEBI:33288 | rodenticide |
| CHEBI has role | CHEBI:33289 | avicide |
| CHEBI has role | CHEBI:35942 | neurotransmitter agent |
| CHEBI has role | CHEBI:48873 | cholinergic antagonist |
| CHEBI has role | CHEBI:62754 | glycine receptor antagonist |
| CHEBI has role | CHEBI:64909 | poison |
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 | 8.32 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | GPCR | ALLOSTERIC MODULATOR | Kd | 5 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M2 | GPCR | ALLOSTERIC MODULATOR | Kd | 5 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M3 | GPCR | ALLOSTERIC MODULATOR | Kd | 5.70 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M4 | GPCR | ALLOSTERIC MODULATOR | Kd | 5 | IUPHAR | ||||
| Glycine receptor subunit alpha-1 | Ion channel | IC50 | 4.70 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 4.68 | CHEMBL | |||||
| Taste receptor type 2 member 10 | GPCR | EC50 | 5.30 | CHEMBL | |||||
| Taste receptor type 2 member 46 | GPCR | AGONIST | EC50 | 6.37 | SCIENTIFIC LITERATURE | ||||
| Glycine receptor subunit alpha-1 | Ion channel | Ki | 7.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019934 | VUID |
| N0000148019 | NUI |
| 4019131 | VANDF |
| 4019934 | VANDF |
| C0202474 | UMLSCUI |
| CHEBI:28973 | CHEBI |
| SY9 | PDB_CHEM_ID |
| CHEMBL227934 | ChEMBL_ID |
| DB15954 | DRUGBANK_ID |
| CHEMBL2165710 | ChEMBL_ID |
| CHEMBL2103753 | ChEMBL_ID |
| D013331 | MESH_DESCRIPTOR_UI |
| 441071 | PUBCHEM_CID |
| 347 | IUPHAR_LIGAND_ID |
| 1421-86-9 | SECONDARY_CAS_RN |
| 60-41-3 | SECONDARY_CAS_RN |
| H9Y79VD43J | UNII |
| 236074 | RXNORM |
| NOCODE | MMSL |
| 001377 | NDDF |
| 005031 | NDDF |
| 005063 | NDDF |
| 354051007 | SNOMEDCT_US |
| 51200005 | SNOMEDCT_US |
| H9Y79VD43J | INXIGHT DRUGS |
Pharmaceutical products:
None