Direct Inhibitory Effect of Hemicholinium
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Inhibition of choline uptake in syncytial microvillus membrane vesicles of human term placenta. Specificity and nature of interaction.
The potency and nature of the inhibitory effect of various cationic drugs on the transport of choline across the placental syncytial microvillus membrane was investigated. Tetraethylammonium, a model substrate for organic cation transport, was a poor inhibitor. Enlarging the degree of alkylation of the quaternary ammonium increased the inhibitory effect, in proportion with increasing lipophilic...
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CF-1 male mice were trained in an inhibitory avoidance task using a high footshock (1,2 mA, 50 Hz, 1 sec) in order to reduce the influence of extinction on retention performance. At 2, 7, 14, or 30 d after training, the first retention test was performed and hemicholinium (HC-3, 1.0 microg/mice), a specific inhibitor of high-affinity choline uptake in brain cholinergic neurons, was given intrac...
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The effect of hemicholinium-3 on the incorporation of [Me-%]choline into the phospholipids of the subcellular fractions of the canine caudate nucleus was studied. A correlation between the amount of hemicholinium-3 administered and increased choline incorporation into phospholipids was obtained. The analysis of the labeled phospholipids revealed that 93% of the radioactivity was in phosphatidyl...
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Centrophenoxine exhibited some interesting actions at the neuromuscular junction. The drug was ineffective in rat or chick preparations, but blocked neuromuscular transmission in frog preparations. The blockade was reversed by adrenaline, potassium, choline and physostigmine. The drug had no effect on muscle contractility or endplate cholinoceptor. Hemicholinium 3 induced a neuromuscular blocka...
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Acetylcholine is directly perfused into the canine sinus node in vivo through its cannulated nutrient artery. After atropinization, the chronotropic action from intranodal administration of acetylcholine was identical to that of control injections of Ringer's solution alone. Eserine produced only a negative chronotropic action before, and no significant action after, atropinization. Direct perf...
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