[Ion channel topography of the neuronal nicotinic acetylcholine receptor : pharmacochemical approaches].
Forty-three bisammonium ganglionic blockers were synthesized to study the structure of the ion channel of nicotinic acetylcholine receptor. The conformational parameters of these blockers were studied, and their effects toward the ganglionic transmission in situ on the sympathetic feline upper cervical ganglions and in vitro on the parasympathetic guinea-pig small intestine ganglions were determined. A model of the binding site for the bisammonium ganglionic blockers in the neuronal ion channel was proposed.
Gmiro
V E
VE
Institute of Experimental Medicine, Russian Academy of Medical Sciences, Kamennoostrvskii pr. 69/71, St. Petersburg, 197022 Russia. g2119@online.ru
Brovtsyna
N B
NB
Serdiuk
S E
SE
Lukomskaia
N Ia
NIa
D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D002415:Cats; D005726:Ganglia, Parasympathetic / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D008969:Molecular Sequence Data; D009474:Neurons / Q000378:metabolism; D000644:Quaternary Ammonium Compounds / Q000737:chemistry / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000737:chemistry* / Q000187:drug effects / Q000378:metabolism*; D017386:Sequence Homology, Amino Acid; D013329:Structure-Activity Relationship
D000644:Quaternary Ammonium Compounds; D011978:Receptors, Nicotinic