Effects of aliphatic alcohols and food additives on nicotinic acetylcholine receptors in Xenopus oocytes.
To study the effects of food additives on nicotinic acetylcholine receptors (nAChR), they were expressed in Xenopus oocytes that received an injection of mRNA prepared from electroplax of Electrophorus electricus. The response of nAChR elicited by acetylcholine (ACh) was measured electrophysiologically in the presence and absence of aliphatic alcohols and food additives. All compounds examined inhibited nAChR non-competitively in a concentration-dependent way. The inhibition was stronger when the inhibitors were perfused 1 min before ACh, than when they were perfused simultaneously with ACh. The inhibition of nAChR by aliphatic alcohols (propanol to hexanol) increased as the number of carbon chains increased. The addition of alcohols and food additives did not affect the desensitization of nAChR caused by 2 microM ACh. These results suggest that alcohols and food additives bind to the anesthetic binding site in nAChR and inhibit it noncompetitively. However, these compounds will not hinder signal transmission in neuromuscular junctions under physiological conditions, because their inhibition constants are more than 1 mM and muscles usually have more receptors than the number necessary for signal transmission.
Aoshima
H
H
Department of Chemistry, Faculty of Liberal Arts, Yamaguchi University, Japan.
Mitsusada
N
N
Nishino
T
T
D000818:Animals; D004593:Electrophorus; D004594:Electrophysiology; D005233:Fatty Alcohols / Q000494:pharmacology*; D005503:Food Additives / Q000494:pharmacology*; D018733:Nicotinic Antagonists; D009865:Oocytes / Q000187:drug effects / Q000378:metabolism*; D018408:Patch-Clamp Techniques; D012333:RNA, Messenger / Q000096:biosynthesis; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014982:Xenopus laevis
D005233:Fatty Alcohols; D005503:Food Additives; D018733:Nicotinic Antagonists; D012333:RNA, Messenger; D011978:Receptors, Nicotinic