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Table 2 GABACl receptors response profiles to antagonists. IC50 in nM ± SEM obtained with a variety of compounds

From: The novel isoxazoline ectoparasiticide lotilaner (Credelio™): a non-competitive antagonist specific to invertebrates γ-aminobutyric acid-gated chloride channels (GABACls)

Receptor

Antagonist

IC50 (nM)

nH

N

DmS-GABA

Dieldrin

4170 ± 920

-0.45 ± 0.05

9

DmS-GABA

Fipronil

27.58 ± 1.71

-0.85 ± 0.04

8

DmS-GABA

Lotilaner

23.84 ± 1.87

-0.64 ± 0.03

16

DmS-GABA

AHC-2229544

959.47 ± 268.44

-0.30 ± 0.03

8

DmR2-GABA

Dieldrin

> 10,000

-0.15 ± 0.03

6

DmR2-GABA

Fipronil

230.32 ± 27.29

-0.57 ± 0.04

7

DmR2-GABA

Lotilaner

38.25 ± 3.75

-0.62 ± 0.04

7

Ls-GABA1

Fipronil

164.85 ± 11.80

-0.78 ± 0.04

12

Ls-GABA1

Lotilaner

52.40 ± 4.54

-0.75 ± 0.04

8

Rm-GABA

Fipronil

25.56 ± 2.25

-0.56 ± 0.03

6

Rm-GABA

Lotilaner

36.79 ± 4.39

-0.47 ± 0.03

8

Cl-GABAA α1β2γ2

Lotilaner

> 10,000

-0.09 ± 0.02

7

  1. Abbreviations: Dm, Drosophila melanogaster; Ls, Lepeophtheirus salmonis; Rm, Rhipicephalus microplus; Cl, Canis lupus familiaris. The Hill coefficient (nH) is indicated as well as the number of oocytes evaluated (N)