Agonist and blocking effects of choline at the neuromuscular junction.
The effects of choline chloride were studied at the voltage-clamped frog neuromuscular junction by measuring miniature endplate currents and equilibrium dose response curves for acetylcholine applied by microionophoresis. Choline reduced the amplitude and shortened the time constant of miniature endplate currents in a dose dependent manner. Dose response curves carried out in the presence of low doses of choline (200 microM) were shifted to the right and the apparent dissociation constant for ACh was increased without affecting the Hill coefficient or the maximum conductance at the endplate. Higher doses of choline shifted the curve even further to the right but reduced the Hill coefficient and maximum conductance. Choline ionophoretic dose response curves were carried out but the conductance response was only about 1% of the response to comparable concentrations of ACh. In the presence of ethanol, which reduces the agonist dissociation constant, choline responses were increased and the dose response curve analysis revealed that the efficacy of choline was about 17% in comparison to ACh. Similar effects were measured at rat endplates. Rat nerve-muscle preparations were used to investigate the effects of choline upon neuromuscular transmission.
D000109:Acetylcholine / Q000502:physiology*; D000818:Animals; D002217:Carbachol / Q000494:pharmacology; D002794:Choline / Q000502:physiology*; D000431:Ethanol / Q000494:pharmacology; D066298:In Vitro Techniques; D007478:Iontophoresis; D008297:Male; D008564:Membrane Potentials / Q000187:drug effects; D009469:Neuromuscular Junction / Q000187:drug effects / Q000502:physiology*; D009538:Nicotine / Q000494:pharmacology; D011893:Rana esculenta; D051381:Rats; D011919:Rats, Inbred Strains; D013390:Succinylcholine / Q000494:pharmacology; D014403:Tubocurarine / Q000494:pharmacology
D000431:Ethanol; D009538:Nicotine; D002217:Carbachol; D013390:Succinylcholine; D002794:Choline; D000109:Acetylcholine; D014403:Tubocurarine