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Inhibitor Report for: Hexamethonium

A nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool


General
Type Bisquaternary, Nicotinic antagonist, Trimethylammonium
Chemical_Nomenclature 1,6-bis(trimethylammonium)hexane
Canonical SMILES C[N+](C)(C)CCCCCC[N+](C)(C)C.[OH-].[OH-]
InChI InChI=1S/C12H30N2.2H2O/c1-13(2,3)11-9-7-8-10-12-14(4,5)6;;/h7-12H2,1-6H3;2*1H2/q+2;;/p-2
InChIKey GYLUMIIRFKDCKI-UHFFFAOYSA-L
Other name(s) UNII-RVL393940Z ; Hexamethonium hydroxide solution ; Hexamethonum ; Bistrium ; Depressin ; Hexanium
________________________________________________________________________________________________
MW|273.29
Formula|C12H30N2Cl2
CAS_number|60-25-3
PubChem|6059
UniChem|GYLUMIIRFKDCKI-UHFFFAOYSA-L
IUPHAR|
Wikipedia|Hexamethonium

Target
Families | Hexamethonium ligand of proteins in family: ACHE

References:
Search PubMed for references concerning: Hexamethonium

27 more
    Title: Evaluation of the nature of camel retinal acetylcholinesterase: inhibition by hexamethonium
    Alhomida AS, Kamal MA, Al-Jafari AA
    Ref: J Enzyme Inhib, 12:303, 1997 : PubMed

            

    Title: Acetylcholinesterase peripheral anionic site degeneracy conferred by amino acid arrays sharing a common core
    Barak D, Kronman C, Ordentlich A, Ariel N, Bromberg A, Marcus D, Lazar A, Velan B, Shafferman A
    Ref: Journal of Biological Chemistry, 269:6296, 1994 : PubMed

            

    Title: Structure-activity relationship of reversible cholinesterase inhibitors including paraquat
    Seto Y, Shinohara T
    Ref: Archives of Toxicology, 62:37, 1988 : PubMed

            


chick-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 242 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335

human-ACHE
MutationKiKsiIc50SubstrateConditionPaper
> Mutations for human-ACHE (19)

torma-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 84 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
chick-ACHE242 uM-- Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHE0.2 mM-- Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
torma-ACHE84 uM-- Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335