title: The effect of HI-6 on cholinesterases and on the cholinergic system of the rat bladder.
abstract: OBJECTIVE
  The current standard treatment of organophosphate poisoning consists of an administration of anticholinergic drugs and cholinesterase reactivators (oximes). Oximes can react - except their reactivating effect on cholinesterases - directly with cholinoreceptors. HI-6 is an oxime that may have an inhibitory effect on the muscarinic receptors, too.
  
  
  METHODS
  In our work, we have investigated an influence of HI-6 on the acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and on the muscarinic receptors in vitro. The study was conducted using biosensor technique and on the rat bladder using in vitro test (tissue bath; methacholine as muscarinic agonist). IC50 for BChE from human serum was determined to be 1.01x10-6 M and for human erythrocytes AChE 3.31x10-6 M, respectively.
  
  
  CONCLUSIONS
  We assume that the demonstrated contractile response can be attributed to the inhibition of the AChE at the lower concentration and to a predominant inhibition of muscarinic receptor at higher concentration of compound tested.
authors.affiliation: Department of Toxicology, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.
authors.forename: Ondrej
authors.initials: O
authors.lastname: Soukup
authors.forename: Miroslav
authors.initials: M
authors.lastname: Pohanka
authors.forename: Gunnar
authors.initials: G
authors.lastname: Tobin
authors.forename: Daniel
authors.initials: D
authors.lastname: Jun
authors.forename: Josef
authors.initials: J
authors.lastname: Fusek
authors.forename: Kamil
authors.initials: K
authors.lastname: Musilek
authors.forename: Jan
authors.initials: J
authors.lastname: Marek
authors.forename: Jiri
authors.initials: J
authors.lastname: Kassa
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuca
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000818:Animals; D015374:Biosensing Techniques; D002091:Butyrylcholinesterase / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D016210:Methacholine Chloride / Q000494:pharmacology; D018721:Muscarinic Agonists / Q000494:pharmacology; D010091:Oximes; D010275:Parasympathetic Nervous System / Q000187:drug effects*; D010865:Pilot Projects; D011726:Pyridinium Compounds / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D001743:Urinary Bladder / Q000187:drug effects* / Q000294:innervation*
chemical_list: D002800:Cholinesterase Inhibitors; D018721:Muscarinic Agonists; D010091:Oximes; D011726:Pyridinium Compounds; D016210:Methacholine Chloride; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; C022870:asoxime chloride