gallamine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
quaternary ammonium compounds 1273 153-76-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • flaxedil
  • gallamine triethochloride
  • gallamonium iodide
  • gallamine triethyl iodide
  • gallamine triethiodide
  • gallamine
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)
  • Molecular weight: 510.83
  • Formula: C30H60N3O3
  • CLOGP: -5.40
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 0
  • TPSA: 27.69
  • ALOGS: -8.97
  • ROTB: 21

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
None FDA DAVIS AND GECK

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03AC02 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
Other quaternary ammonium compounds
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D009465 Neuromuscular Agents
MeSH PA D009466 Neuromuscular Blocking Agents
MeSH PA D003473 Neuromuscular Nondepolarizing Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018733 Nicotinic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents

Drug Use (View source of the data)

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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M2 GPCR NEGATIVE ALLOSTERIC MODULATOR Ki 6.15 DRUG MATRIX SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M1 GPCR Ki 5.07 CHEMBL
Acetylcholinesterase Enzyme Ki 4.43 CHEMBL
Acetylcholine receptor subunit alpha Ion channel BLOCKER IC50 6 IUPHAR
Muscarinic acetylcholine receptor M2 GPCR EC50 6.89 CHEMBL
Acetylcholinesterase Enzyme Ki 4.82 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ALLOSTERIC MODULATOR Ki 5.60 IUPHAR

External reference:

IDSource
D005703 MESH_DESCRIPTOR_UI
4018916 VUID
N0000147209 NUI
C0016972 UMLSCUI
D02292 KEGG_DRUG
1146X1WTNM UNII
76286000 SNOMEDCT_US
4638 RXNORM
387435005 SNOMEDCT_US
002402 NDDF
CHEMBL360055 ChEMBL_ID
DB00483 DRUGBANK_ID
1928 INN_ID
65-29-2 SECONDARY_CAS_RN
GMN PDB_CHEM_ID
CHEBI:94609 CHEBI
CHEMBL1200993 ChEMBL_ID
67425 PUBCHEM_CID
356 IUPHAR_LIGAND_ID
DB13584 DRUGBANK_ID

Pharmaceutical products:

None