Details

Autor(en) / Beteiligte

• Lozona, Yosra
• Sultana, Ahmed
• Lansdellb, Stuart J
• Prytkovac, Tatiana
• Sadeka, Bassem
• Yangc, Keun-Hang Susan
• Howarthd, Frank Christopher
• Millarb, Neil S
• Oza, Murat

Titel

Inhibition of human alpha 7 nicotinic acetylcholine receptors by cyclic monoterpene carveol

Ist Teil von

• European journal of pharmacology, 2016-04, Vol.776, p.44-51

Erscheinungsjahr

2016

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• Cyclic monoterpenes are a group of phytochemicals with antinociceptive, local anesthetic, and anti-inflammatory actions. Effects of cyclic monoterpenes including vanilin, pulegone, eugenole, carvone, carvacrol, carveol, thymol, thymoquinone, menthone, and limonene were investigated on the functional properties of the cloned alpha 7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes. Monoterpenes inhibited the alpha 7 nicotinic acetylcholine receptor in the order carveol>thymoquinone>carvacrol>menthone>thymol>limonene>eugenole>p u legone greater than or equal to carvone greater than or equal to vanilin. Among the monoterpenes, carveol showed the highest potency on acetylcholine-induced responses, with IC sub(50) of 8.3 mu M. Carveol-induced inhibition was independent of the membrane potential and could not be reversed by increasing the concentration of acetylcholine. In line with functional experiments, docking studies indicated that cyclic monoterpenes such as carveol may interact with an allosteric site located in the alpha 7 transmembrane domain. Our results indicate that cyclic monoterpenes inhibit the function of human alpha 7 nicotinic acetylcholine receptors, with varying potencies.