Inhibition by neosurugatoxin of nicotine-induced antinociception.
We have found a selective inhibition of nicotine-induced antinociception in mice by neosurugatoxin (NSTX, 0.4-3.8 nmol/kg), a neurotoxin with a high affinity for ganglionic nicotinic receptors (ED50 = 0.65 nmol/kg). The toxin also reduced specific [3H]nicotine binding in mouse brain membranes (IC50 = 95 nM). The anti-nicotinic activity of NSTX was markedly greater than that of mecamylamine and pempidine. These data indicate that NSTX may block functional nicotinic cholinoceptors possibly in the central nervous system.
Yamada
S
S
Kagawa
Y
Y
Takayanagi
N
N
Hayashi
E
E
Tsuji
K
K
Kosuge
T
T
D000818:Animals; D002490:Central Nervous System / Q000187:drug effects*; D018738:Hexamethonium; D006584:Hexamethonium Compounds / Q000494:pharmacology; D008297:Male; D008464:Mecamylamine / Q000494:pharmacology; D051379:Mice; D008978:Mollusk Venoms / Q000494:pharmacology*; D009538:Nicotine / Q000037:antagonists & inhibitors*; D010146:Pain / Q000188:drug therapy*; D010393:Pempidine / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000187:drug effects*
D006584:Hexamethonium Compounds; D008978:Mollusk Venoms; D011978:Receptors, Nicotinic; D018738:Hexamethonium; D008464:Mecamylamine; D009538:Nicotine; C036793:neosurugatoxin; D010393:Pempidine