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gallamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quaternary ammonium compounds | 1273 | 153-76-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.27 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.51 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.52 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 58 | |||
| kinase-selectivity-class | AXL,BRAF,CAMK2D,CDK4,EPHB4,GRK2,MAPK7,NUAK1,PDK4,PRKCD,SIK2,STK33 | 12 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | DAVIS AND GECK |
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 | M03AC02 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS Other quaternary ammonium compounds |
| MeSH PA | D003473 | Neuromuscular Nondepolarizing Agents |
| MeSH PA | D009465 | Neuromuscular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018680 | Cholinergic Antagonists |
| MeSH PA | D018733 | Nicotinic Antagonists |
| CHEBI has role | CHEBI:48873 | cholinergic antagonist |
| CHEBI has role | CHEBI:51371 | muscle relaxant |
| CHEBI has role | CHEBI:88188 | drug allergen |
Related Drugs by ATC class:
M03AC Other quaternary ammonium compounds 10 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
None
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 M2 | GPCR | NEGATIVE ALLOSTERIC MODULATOR | Ki | 6.15 | DRUG MATRIX | SCIENTIFIC LITERATURE | |||
| Acetylcholinesterase | Enzyme | Ki | 4.43 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.07 | CHEMBL | |||||
| Acetylcholine receptor subunit alpha | Ion channel | BLOCKER | IC50 | 6 | IUPHAR | ||||
| Acetylcholinesterase | Enzyme | Ki | 4.82 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | EC50 | 6.89 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | ALLOSTERIC MODULATOR | Ki | 5.60 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4018916 | VUID |
| N0000147209 | NUI |
| D02292 | KEGG_DRUG |
| 65-29-2 | SECONDARY_CAS_RN |
| 4018916 | VANDF |
| GMN | PDB_CHEM_ID |
| CHEMBL360055 | ChEMBL_ID |
| CHEMBL1200993 | ChEMBL_ID |
| 356 | IUPHAR_LIGAND_ID |
| DB13584 | DRUGBANK_ID |
| 1146X1WTNM | UNII |
| DB00483 | DRUGBANK_ID |
| 151770 | RXNORM |
| 002402 | NDDF |
| 005160 | NDDF |
| 387097006 | SNOMEDCT_US |
| 387435005 | SNOMEDCT_US |
| 76286000 | SNOMEDCT_US |
| C0016971 | UMLSCUI |
| D005703 | MESH_DESCRIPTOR_UI |
| CHEBI:94609 | CHEBI |
| 67425 | PUBCHEM_CID |
| 1928 | INN_ID |
Pharmaceutical products:
None