[N-methylcytisine--a selective ligand of nicotinic receptors of acetylcholine in the CNS].
The ability of cytisine and its N-methyl derivatives to bind to nicotinic acetylcholine receptors (nAChR) from different tissues was studied. Cytisine and N-methylcytisine have high affinity (KD = 50 nM) to nAChR from squid optical ganglia. N,N-dimethylcytisine did not show high affinity to this receptor. In the case of nAChR from T. marmorata, cytisine was the only effective inhibitor of 14C-tubocurarine specific binding (Ki = 700 nM). N-methyl- and N,N-dimethylcytisine did not displace 14C-tubocurarine at a concentration of 0.1 mM. The results obtained indicate that there are some differences in the structure of nAChR binding sites from squid and T. marmorata optical ganglia.
Pliashkevich
Iu G
IuG
Demushkin
V P
VP
D000109:Acetylcholine / Q000378:metabolism*; D000470:Alkaloids / Q000378:metabolism*; D000818:Animals; D002490:Central Nervous System / Q000378:metabolism*; D049832:Decapodiformes; D008024:Ligands; D011807:Quinolizines; D011978:Receptors, Nicotinic / Q000378:metabolism*; D014101:Torpedo; D000093843:Quinolizidine Alkaloids
D000109:Acetylcholine; D000470:Alkaloids; D008024:Ligands; D011807:Quinolizines; D011978:Receptors, Nicotinic; C034245:N-methylcytisine; D000093843:Quinolizidine Alkaloids
N-metiltsitizin--selektivnyĭ ligand nikotinovykh retseptorov atsetilkholina v TsNS.