Synthesis and pharmacology of alkanediguanidinium compounds that block the neuronal nicotinic acetylcholine receptor

…, S Cueto, JL García-Navio, J Alvarez-Builla

Index: Villarroya, Mercedes; Gandia, Luis; Lopez, Manuela G.; Garcia, Antonio G.; Cueto, Senida; Garcia-Navio, Jose-Luis; Alvarez-Builla, Julio Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 8 p. 1177 - 1183

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Citation Number: 18

Abstract

Taking as models the polyamine toxin fraction FTX from the funnel-web spider venom, and the guanidinium moiety of guanethidine, a series of azaalkane-1, ω-diguanidinium salts were obtained. Some of them blocked ion fluxes through the neuronal nicotinic receptors for acetylcholine (nAChR). The blockade was exerted at submicromolar concentrations, suggesting a highly selective interaction with the nAChR. In fact, the active compounds on ...