Search results for "Vesamicol"
showing 3 items of 3 documents
Suppression by cholinesterase inhibition of a Ca(2+)-independent efflux of [3H]acetylcholine from the neuromuscular junction of the isolated rat diap…
1992
Abstract Endplate preparations of the left rat hemidiaphragm were incubated with [ 3 H]choline to label neuronal acetylcholine stores. Elevation of the concentration (13.5–135 mmol/l) of extracellular potassium chloride (KC1) stimulated the release of [ 3 H]acetylcholine in a concentration-dependent manner. KC1 (27 mmol/l) still caused a significant efflux of [ 3 H]acetylcholine in a Ca 2+ -free medium. Inhibitors of cholinesterase (physostigmine, diisopropylfluorophosphate) suppressed by 80% this Ca 2+ -independent efflux of [ 3 H]acetylcholine. Vesamicol (10 μmol/l), the blocker of the vesicular acetylcholine carrier, also suppressed the stimulated, Ca 2+ -independent efflux of [ 3 H]acet…
Release of non-neuronal acetylcholine from the isolated human placenta is mediated by organic cation transporters
2001
1. The release of acetylcholine was investigated in the human placenta villus, a useful model for the characterization of the non-neuronal cholinergic system. 2. Quinine, an inhibitor of organic cation transporters (OCT), reduced acetylcholine release in a reversible and concentration-dependent manner with an IC(50) value of 5 microM. The maximal effect, inhibition by 99%, occurred at a concentration of 300 microM. 3. Procaine (100 microM), a sodium channel blocker, and vesamicol (10 microM), an inhibitor of the vesicular acetylcholine transporter, were ineffective. 4. Corticosterone, an inhibitor of OCT subtype 1, 2 and 3 reduced acetylcholine in a concentration-dependent manner with an IC…
Vesamicol blocks the recovery, by recycling cholinergic electromotor synaptic vesicles, of the biophysical characteristics of the reserve population.
1993
The effect of vesamicol on the ability of recycling cholinergic synaptic vesicles to recover, during a period of post-stimulation rest, the biophysical properties of the reserve pool was studied in prestimulated perfused blocks of the electric organ of the electric ray, Torpedo marmorata, a tissue rich in cholinergic synapses. The effect of the drug was analysed by high-resolution centrifugal density-gradient fractionation in a zonal rotor of the extracted vesicles. The two vesicle fractions were identified by their ATP and acetylcholine content and the recycled vesicles by their acquisition of [3H]acetylcholine derived from [3H]acetate in the perfusate. Vesamicol (10 microM) blocked the up…