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Amiloride Derivatives Are Effective Blockers of Insect Odorant Receptors

Amiloride Derivatives Are Effective Blockers of Insect Odorant Receptors

Katharina Röllecke, Markus Werner, Paul M Ziemba, Eva M Neuhaus, Hanns Hatt, Günter Gisselmann

Chem Senses. 2013 Mar;38(3):231-6.

PMID: 23329732

Abstract:

Heteromeric insect odorant receptors (ORs) form ligand-activated nonselective cation channels in recombinant expression systems. We performed a pharmacological characterization of Drosophila melanogaster and Bombyx mori ORs expressed in the Xenopus laevis oocyte expression system and characterized them using the 2-electrode voltage clamp. We identified amiloride derivatives as high-affinity blockers, which inhibit the ion current through the channel in a low micromolar range. For the heteromeric Drosophila Or47a + DmelOrco receptor, the potency sequence (IC(50)) is HMA [5-(N,N-hexamethylene)amiloride] (3.9 µM), MIA [5-(N-methyl-N-isobutyl)amiloride] (11.0 µM), and DMA [5-(N,N-dimethyl)amiloride] (113.3 µM). Amiloride itself is nearly ineffective. Other tested insect ORs (Drosophila Or49b + DmelOrco, B. mori BmorOr1 + BmorOrco) were blocked in a similar fashion suggesting that the amiloride derivatives were potential general blockers of all receptor combinations. Our results suggest that pyrazine derivatives of amiloride are useful probes to study the mechanism of chemosensory transduction in insects in more detail.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP96861653	5-(N-Methyl-N-isobutyl)amiloride		96861-65-3	Price

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