Abstract:
:Insect odorant receptors (ORs) function as heteromeric odorant-gated ion channels consisting of a conserved coreceptor, Orco, and an odorant-sensitive tuning subunit. Although some OR modulators have been identified, an extended library of pharmacological tools is currently lacking and would aid in furthering our understanding of insect OR complexes. We now demonstrate that amiloride and several derivatives, which have been extensively used as blockers for various ion channels and transporters, also block odorant-gated currents from 2 OR complexes from the malaria vector mosquito Anopheles gambiae. In addition, both heteromeric and homomeric ORs were susceptible to amiloride blockade when activated by VUAA1, an agonist that targets the Orco channel subunit. Amiloride derivatives therefore represent a valuable class of channel blockers that can be used to investigate the pharmacological and biophysical properties of insect OR function.
journal_name
Chem Sensesjournal_title
Chemical sensesauthors
Pask GM,Bobkov YV,Corey EA,Ache BW,Zwiebel LJdoi
10.1093/chemse/bjs100subject
Has Abstractpub_date
2013-03-01 00:00:00pages
221-9issue
3eissn
0379-864Xissn
1464-3553pii
bjs100journal_volume
38pub_type
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