Differential sensitivity of Ctenocephalides felis and Drosophila melanogaster nicotinic acetylcholine receptor α1 and α2 subunits in recombinant hybrid receptors to nicotinoids and neonicotinoid insecticides

Dederer, Helene; Werr, Margaret; Ilg, Thomas

doi:10.1016/j.ibmb.2010.09.012

Cited by 12 publications

(16 citation statements)

References 72 publications

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“…However, the H108L amino acid substation in the His108-type Dα1 subunit enhanced agonist efficacy of imidacloprid. Recently, it was reported that imidacloprid was a partial agonist with I max of 0.095 of that of ACh for the Dα1β2 nAChR, 24) which appears to contradict our earlier observation that imidacloprid induced a very small current amplitude in oocytes. 9) It is now possible to reconcile these apparently disparate findings by the fact that the recent study 24) employed the Dα1 subunit containing Leu108 and is consistent with findings presented here; imidacloprid showed higher efficacy on the hybrid receptor than the His108-type Dα1β2 nAChR.…”

Section: Discussioncontrasting

confidence: 94%

A single amino acid polymorphism in the Drosophila melanogaster Dα1 (ALS) subunit enhances neonicotinoid efficacy at Dα1-chicken β2 hybrid nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes

Ihara

Shimazu

Utsunomiya

et al. 2014

Bioscience, Biotechnology, and Biochemistry

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Section: Discussioncontrasting

confidence: 94%

A single amino acid polymorphism in the Drosophila melanogaster Dα1 (ALS) subunit enhances neonicotinoid efficacy at Dα1-chicken β2 hybrid nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes

Ihara

Shimazu

Utsunomiya

et al. 2014

Bioscience, Biotechnology, and Biochemistry

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“…gambiae Rdl with an IC 50 of 109 μM (Table ) whereas it acts as an agonist with EC 50 0.07 μM on the α1/β2 D. melanogaster / Gallus gallus nAChR hybrid expressed in X. laevis oocytes (Dederer et al . ). For deltamethrin, 50 μM was required to see an antagonistic effect on An.…”

Section: Discussionmentioning

confidence: 97%

The neonicotinoid imidacloprid, and the pyrethroid deltamethrin, are antagonists of the insect Rdl GABA receptor

Taylor-Wells

Brooke

Bermúdez

et al. 2015

Journal of Neurochemistry

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A mutation in the second transmembrane domain of the GABA receptor subunit, Rdl, is associated with resistance to insecticides such as dieldrin and fipronil. Molecular cloning of Rdl cDNA from a strain of the malaria mosquito, Anopheles gambiae, which is highly resistant to dieldrin revealed this mutation (A296G) as well as another mutation in the third transmembrane domain (T345M). Wild-type, A296G, T345M and A296G + T345M homomultimeric Rdl were expressed in Xenopus laevis oocytes and their sensitivities to fipronil, deltamethrin, 1,1,1-trichloro-2,2-bis(p-chlorophenyl) ethane (DDT), imidacloprid and spinosad were measured using twoelectrode voltage-clamp electrophysiology. Spinosad and DDT had no agonist or antagonist actions on Rdl. However, fipronil, deltamethrin and imidacloprid decreased GABAevoked currents. These antagonistic actions were either reduced or abolished with the A296G and the A296G + T345M mutations while T345M alone appeared to have no significant effect. In conclusion, this study identifies another mutation in the mosquito Rdl that is associated with insecticide resistance. While T345M itself does not affect insecticide sensitivity, it may serve to offset the structural impact of A296G. The present study also highlights Rdl as a potential secondary target for neonicotinoids and pyrethroids.

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“…Data taken from Dederer et al ., . The compound numbers in parentheses refer to the structures in Fig.…”

Section: Resultsmentioning

confidence: 99%

“…Neonicotinoids act as partial, full and super‐agonists of insect nAChRs and are broadly active and highly selective insecticides, that are also used against cyclorrhaphan flies, such as fruit flies or nuisance flies (Nurita and Abu Hassan, Raga & Eidi Sato, ). The nAChR subunits α1, α2, and possibly also α3 and α8/β2 are implicated as potential molecular targets in various insects (Matsuda et al ., ; Liu et al ., , , ; Gao et al ., ; Perry et al ., ; Yixi et al ., ; Li et al ., ; Dederer et al ., ), whereas spinosad appears to act on receptors containing nAChR subunit α6 (Perry et al ., ; Baxter et al ., ). While spinosad is an established blowfly insecticide (Levot et al ., ), no compound of the neonicotinoid class is yet registered on the market for use against L. cuprina .…”

Section: Introductionmentioning

confidence: 99%

Structure‐activity relationships of acetylcholine derivatives with Lucilia cuprina nicotinic acetylcholine receptor α1 and α2 subunits in chicken β2 subunit hybrid receptors in comparison with chicken nicotinic acetylcholine receptor α4/β2

Dederer

Berger

Meyer

et al. 2013

Insect Molecular Biology

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Insect nicotinic acetylcholine (ACh) receptors (nAChRs) are the targets of several insecticide classes. In the present study, we report the gene identification and cloning of nAChR α1 and α2 subunits (Lcα1 and Lcα2) from the sheep blowfly Lucilia cuprina. Xenopus oocytes voltage clamp experiments as hybrids with the chicken β2 nAChR (Ggβ2) subunit resulted in ACh-gated ion channels with distinct dose-response curves for Lcα1/Ggβ2 (effective concentration 50% [EC50 ] = 80 nM; nH = 1.05), and Lcα2/Ggβ2 (EC50 = 5.37 μM, nH = 1.46). The neonicotinoid imidacloprid was a potent agonist for the α-bungarotoxin-sensitive Lcα1/Ggβ2 (EC50 ∼ 20 nM), while the α-bungarotoxin-resistant Lcα2/Ggβ2 showed a 30-fold lower sensitivity to this insecticide (EC50 = 0.62 μM). Thirteen close derivatives of ACh were analysed in EC50 , Hill coefficient and maximum current (relative to ACh) determinations for Lcα1/Ggβ2 and Lcα2/Ggβ2 and the chicken Ggα4/Ggβ2 nAChRs, and comparisons relative to ACh allowed the definition of novel structure-activity and structure-selectivity relationships. In the case of N-ethyl-acetylcholine, the EC50 of the chicken Ggα4/Ggβ2 rose by a factor of 1000, while for both Lcα1/Ggβ2 and Lcα2/Ggβ2, potency remained unchanged. Further derivatives with insect nAChR selectivity potential were acetyl-α-methylcholine and trimethyl-(3-methoxy-3-oxopropyl)ammonium, followed by acetylhomocholine and trimethyl-(4-oxopentyl) ammonium. Our results may provide guidance for the identification or design of insect-specific nAChR agonists using structure-based or in silico methods.

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Differential sensitivity of Ctenocephalides felis and Drosophila melanogaster nicotinic acetylcholine receptor α1 and α2 subunits in recombinant hybrid receptors to nicotinoids and neonicotinoid insecticides

Cited by 12 publications

References 72 publications

A single amino acid polymorphism in the Drosophila melanogaster Dα1 (ALS) subunit enhances neonicotinoid efficacy at Dα1-chicken β2 hybrid nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes

A single amino acid polymorphism in the Drosophila melanogaster Dα1 (ALS) subunit enhances neonicotinoid efficacy at Dα1-chicken β2 hybrid nicotinic acetylcholine receptor expressed in Xenopus laevis oocytes

The neonicotinoid imidacloprid, and the pyrethroid deltamethrin, are antagonists of the insect Rdl GABA receptor

Structure‐activity relationships of acetylcholine derivatives with Lucilia cuprina nicotinic acetylcholine receptor α1 and α2 subunits in chicken β2 subunit hybrid receptors in comparison with chicken nicotinic acetylcholine receptor α4/β2

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