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Artículo

Alpha9 nicotinic acetylcholine receptors and the treatment of pain

McIntosh, J. Michael; Absalom, Nathan; Chebib, Mary; Elgoyhen, Ana BelenIcon ; Vincler, Michelle
Fecha de publicación: 10/2009
Editorial: Pergamon-Elsevier Science Ltd
Revista: Biochemical Pharmacology
ISSN: 0006-2952
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Bioquímica y Biología Molecular

Resumen

Chronic pain is a vexing worldwide problem that causes substantial disability and consumes significant medical resources. Although there are numerous analgesic medications, these work through a small set of molecular mechanisms. Even when these medications are used in combination, substantial amounts of pain often remain. It is therefore highly desirable to develop treatments that work through distinct mechanisms of action. While agonists of nicotinic acetylcholine receptors (nAChRs) have been intensively studied, new data suggest a role for selective antagonists of nAChRs. α-Conotoxins are small peptides used offensively by carnivorous marine snails known as Conus. A subset of these peptides known as α-conotoxins RgIA and Vc1.1 produces both acute and long lasting analgesia. In addition, these peptides appear to accelerate the recovery of function after nerve injury, possibly through immune mediated mechanisms. Pharmacological analysis indicates that RgIA and Vc1.1 are selective antagonists of α9α10 nAChRs. A recent study also reported that these α9α10 antagonists are also potent GABA-B agonists. In the current study, we were unable to detect RgIA or Vc1.1 binding to or action on cloned GABA-B receptors expressed in HEK cells or Xenopus oocytes. We review the background, findings and implications of use of compounds that act on α9* nAChRs.11* indicates the possible presence of additional subunits.
Palabras clave: Α-Conotoxin Vc1.1 , Α-Contoxin Rgia , Alpha9 Nicotinic , Gaba-B , Pain
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/79623
URL: https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/19477168/
DOI: http://dx.doi.org/10.1016/j.bcp.2009.05.020
URL: https://www.sciencedirect.com/science/article/pii/S0006295209004298
Colecciones
Articulos(INGEBI)
Articulos de INST.DE INVEST.EN ING.GENETICA Y BIOL.MOLECULAR "DR. HECTOR N TORRES"
Citación
McIntosh, J. Michael; Absalom, Nathan; Chebib, Mary; Elgoyhen, Ana Belen; Vincler, Michelle; Alpha9 nicotinic acetylcholine receptors and the treatment of pain; Pergamon-Elsevier Science Ltd; Biochemical Pharmacology; 78; 7; 10-2009; 693-702
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