Interaction of cholinergic ligands and local anesthetics with plasma membrane fragments from lobster axon.
- 1 June 1977
- journal article
- research article
- Published by Proceedings of the National Academy of Sciences in Proceedings of the National Academy of Sciences
- Vol. 74 (6), 2278-2282
- https://doi.org/10.1073/pnas.74.6.2278
Abstract
Isologous local anesthetics containing the ester, thiolester or selenolester grouping and their quaternary ammonium analogs were studied for their ability to displace 3H-nicotine from plasma membrane fragments of lobster [Homarus americanus] nerve. Tertiary and quaternary analogs were equiactive. The relative ability of oxo, thio and seleno analogs to displace nicotine was the same as their relative ability to block axonal conduction and synaptic transmission. Among cholinergic ligands, choline and aminocholine, previously inactive as depolarizing agents, were uniquely unable to displace nicotine. The findings are compatible with the presence of a biopolymer capable of binding cholinergic ligands in axonal membranes and support the postulate that the relative inactivity of quaternary compounds in intact axons is due to permeability barriers.This publication has 34 references indexed in Scilit:
- Constitution and properties of axonal membranes of crustacean nervesBiochemistry, 1975
- Use of a fluorescent probe for the study of ligand binding by the isolated cholinergic receptor of Torpedo californicaBiochemical and Biophysical Research Communications, 1973
- Molecular properties of the cholinergic receptor purified from Electrophorus electricusBiochemistry, 1973
- Tetrodotoxin receptors in plasma membranes isolated from lobster nerve fibersBiochimica et Biophysica Acta (BBA) - Biomembranes, 1973
- Axonal cholinergic binding macromolecule. Response to neuroactive drugsJournal of Medicinal Chemistry, 1973
- Progress in the purification of the cholinergic receptor protein from Electrophorus electricus by affinity chromatographyFEBS Letters, 1972
- Solubilization of a specific tetrodotoxin-binding component from garfish olfactory nerve membraneBiochemistry, 1972
- An axon plasma membrane preparation from the walking legs of the lobster Homarus americanusBiochimica et Biophysica Acta (BBA) - Biomembranes, 1972
- Isolation of Acetylcholine ReceptorsAnnual Review of Pharmacology, 1972
- Acetylcholine Receptor: Similarity in Axons and JunctionsScience, 1967