Biotransformation of an α4β2 Nicotinic Acetylcholine Receptor Partial Agonist in Sprague-Dawley Rats and the Dispositional Characterization of Its N-Carbamoyl Glucuronide Metabolite

2009 ◽  
Vol 37 (7) ◽  
pp. 1480-1489 ◽  
Author(s):  
Christopher L. Shaffer ◽  
Tim F. Ryder ◽  
Karthik Venkatakrishnan ◽  
Ilana K. Henne ◽  
Thomas N. O'Connell
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Partial Agonist ◽  
Sprague Dawley ◽  
Nicotinic Acetylcholine ◽  
Sprague Dawley Rats ◽  
Glucuronide Metabolite

P4-373: APN1125: A NOVEL A7 NICOTINIC ACETYLCHOLINE RECEPTOR PARTIAL AGONIST

2014 ◽  
Vol 10 ◽  
pp. P925-P925
Author(s):  
Gerald Koelsch ◽  
Leonard T. Meltzer ◽  
Ryan F. Yoshimura ◽  
Alvin V. Terry ◽  
Patrick M. Callahan ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Partial Agonist ◽  
Nicotinic Acetylcholine

APN1125: A clinical stage α7 nicotinic acetylcholine receptor partial agonist

2015 ◽  
Vol 97 (4) ◽  
pp. 636 ◽  
Author(s):  
Gerald Koelsch ◽  
Michael J. Detke ◽  
Karen E. Stevens ◽  
Leonard T. Meltzer ◽  
Alvin V. Terry ◽  
...  
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Partial Agonist ◽  
Clinical Stage ◽  
Α7 Nicotinic Acetylcholine Receptor ◽  
Nicotinic Acetylcholine

scholarly journals Mode of Action of Neonicotinoid Insecticides Imidacloprid and Thiacloprid to the Cockroach Pameα7 Nicotinic Acetylcholine Receptor

2021 ◽  
Vol 22 (18) ◽  
pp. 9880
Author(s):  
Alison Cartereau ◽  
Emiliane Taillebois ◽  
Jean-Yves Le Questel ◽  
Steeve H. Thany
Keyword(s):  
Acetylcholine Receptor ◽  
Nicotinic Acetylcholine Receptor ◽  
Partial Agonist ◽  
Functional Expression ◽  
Binding Pocket ◽  
Xenopus Laevis Oocytes ◽  
Nicotinic Acetylcholine ◽  
Neonicotinoid Insecticides ◽  
Neonicotinoid Insecticide ◽  
Inward Currents

The functional expression of the cockroach Pameα7 nicotinic acetylcholine receptor subunit has been previously studied, and was found to be able to form a homomeric receptor when expressed in Xenopus laevis oocytes. In this study, we found that the neonicotinoid insecticide imidacloprid is unable to activate the cockroach Pameα7 receptor, although thiacloprid induces low inward currents, suggesting that it is a partial agonist. In addition, the co-application or 5 min pretreatment with 10 µM imidacloprid increased nicotine current amplitudes, while the co-application or 5 min pretreatment with 10 µM thiacloprid decreased nicotine-evoked current amplitudes by 54% and 28%, respectively. This suggesting that these two representatives of neonicotinoid insecticides bind differently to the cockroach Pameα7 receptor. Interestingly, the docking models demonstrate that the orientation and interactions of the two insecticides in the cockroach Pameα7 nAChR binding pocket are very similar. Electrophysiological results have provided evidence to suggest that imidacloprid and thiacloprid could act as modulators of the cockroach Pameα7 receptors.

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