title: Effects of triethyl lead on various cholinergic parameters in the rat brain in vitro.
abstract: The effects of triethyl lead acetate (triethyl Pb) on the cholinergic system in the brain of the rats were investigated in vitro. Triethyl Pb, at concentrations below 10(-4) M, inhibited the depolarized release of acetylcholine (ACh) from slices of cortex and they synthesis of ACh in such slices, while it potentiated in a dose-dependent manner the non-depolarized release of ACh. In contrast, lead inhibited noncompetitively the high-affinity uptake of choline into synaptosomes with a Ki of 4.03 X 10(-6) M and the activity of choline acetyltransferase with a Ki of 4.07 X 10(-5) M. Triethyl Pb has an inhibitory effect (IC50 not equal to 5 X 10(-5) M) on the binding of [3H]quinuclidinyl benzilate to muscarinic ACh receptors. Triethyl Pb inhibited acetylcholinesterase activity slightly at 5 X 10(-5) and 10(-4) M. It is suggested that ACh transmission, in particular the synthesis of ACh and the release of ACh, is susceptible to organolead neurotoxicity.
authors.affiliation: Department of Veterinary Internal Medicine, School of Veterinary Medicine and Animal Sciences, Kitasato University, Aomori, Japan.
authors.forename: F
authors.initials: F
authors.lastname: Hoshi
authors.forename: H
authors.initials: H
authors.lastname: Kobayashi
authors.forename: A
authors.initials: A
authors.lastname: Yuyama
authors.forename: N
authors.initials: N
authors.lastname: Matsusaka
mesh_terms: D000109:Acetylcholine / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002794:Choline / Q000378:metabolism; D002795:Choline O-Acetyltransferase / Q000378:metabolism; D066298:In Vitro Techniques; D007854:Lead / Q000494:pharmacology*; D008297:Male; D009942:Organometallic Compounds / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011976:Receptors, Muscarinic / Q000187:drug effects; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
chemical_list: D009942:Organometallic Compounds; D011976:Receptors, Muscarinic; D007854:Lead; C010360:triethyllead; D002795:Choline O-Acetyltransferase; D002794:Choline; D000109:Acetylcholine