RT info:eu-repo/semantics/article
T1 Synthesis and pharmacology of alkanediguanidinium compounds that block the neuronal nicotinic acetylcholine receptor
A1 Villarroya, Mercedes
A1 Gandía, Luis
A1 López, Manuela G.
A1 García, Antonio G.
A1 Cueto, Sénida
A1 García Navío, José Luis
A1 Álvarez-Builla Gómez, Julio
K1 Bovine chromaffin cells
K1 Calcium channels
K1 FTX
K1 Separation
K1 Toxin
K1 Biochemistry & Molecular Biology
K1 Ciencia
K1 Química orgánica
K1 Science
K1 Chemistry, organic
AB 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,omega-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 the nAChR ion channel did not recognize the voltage-dependent Na+ or Ca2+ channels of bovine adrenal chromaffin cells. Therefore, these compounds may be useful tools to clarify the functions of nAChR receptors in the central and peripheral nervous systems.
PB Pergamon
SN 0968-0896
YR 1996
FD 1996
LK http://hdl.handle.net/10017/3513
UL http://hdl.handle.net/10017/3513
LA eng
NO Fundación Ramón Areces
DS MINDS@UW
RD 29-abr-2024