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Chemical Senses Advance Access published online on November 10, 2006
Chemical Senses, doi:10.1093/chemse/bjl041
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© The Author 2006. Published by Oxford University Press. All rights reserved. For permissions, please e-mail: journals.permissions@oxfordjournals.org
Accepted October 17, 2006

Article

Block by Amiloride Derivatives of Odor-Evoked Discharge in Lobster Olfactory Receptor Neurons through Action on a Presumptive TRP Channel

Y.V. Bobkov 1 * and B.W. Ache 1

1 Whitney Laboratory for Marine Bioscience, Center for Smell and Taste and McKnight Brain Institute, University of Florida, Gainesville, FL, USA

* To whom correspondence should be addressed.
Y.V. Bobkov, E-mail: bobkov{at}whitney.ufl.edu


  Abstract

Amiloride and its derivatives inhibit a number of sensory transduction processes, including some types of chemosensory transduction. Here, we report that pyrazine derivatives of amiloride reversibly inhibit odorant-evoked activity in lobster olfactory receptor neurons. The potency sequence is as follows--(IC50, mM): 5-(N,N-hexamethylene)amiloride (0.015) ~ 5-(N-methyl-N-isobutyl)amiloride (0.02) ~ 5-(N-ethyl-N-isopropyl)amiloride (0.03) > 5-(N,N-dimethyl)amiloride (0.48); 3',4'-dichlorobenzamil (0.4), phenamil (0.5), and amiloride itself (2) are ineffective. The same derivatives with the similar potency sequence also block a presumptive transient receptor potential (TRP) channel that is the likely downstream target of phosphoinositide signaling in these cells. Our results suggest that pyrazine derivatives of amiloride are useful probes to study more detailed mechanisms of chemosensory transduction in this system and possibly in other chemosensory systems in which TRP channels are the known or suspected downstream effector.

Keywords: inhibition; invertebrates; olfaction; phospholipid signaling; pyrazinecarboxamides; sensory systems.
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