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

Authors
Villarroya, Mercedes; Gandía, Luis; López, Manuela G.; García, Antonio G.; Cueto, Sénida; [et al.]
Identifiers
Permanent link (URI): http://hdl.handle.net/10017/3513
DOI: 10.1016/0968-0896(96)00108-3
ISSN: 0968-0896
Publisher
Pergamon
Date
1996
Affiliation
Universidad de Alcalá. Departamento de Química Orgánica
Funders
Fundación Ramón Areces
Bibliographic citation
Bioorganic & Medicinal Chemistry, 1996, v.4, n.8, p.1177-1183
Keywords
Bovine chromaffin cells
Calcium channels
FTX
Separation
Toxin
Biochemistry & Molecular Biology
Project
PM92-0039 (Ministerio de Educación y Ciencia)
PB94-0150 (Ministerio de Educación y Ciencia)
Document type
info:eu-repo/semantics/article
Version
info:eu-repo/semantics/publishedVersion
Publisher's version
http://dx.doi.org/10.1016/0968-0896(96)00108-3
Rights
© Elsevier, 1996
Access rights
info:eu-repo/semantics/openAccess
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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,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.
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