Inhibition of cortical glycine receptors by avermectin analogs
| Analog | % Inhibition of 300 μM Glycine | |
|---|---|---|
| L-676,893 | Avermectin A2a | 46.6 ± 7.8 |
| L-640,471 | Ivermectin | 97.4 ± 0.8 |
| L-676,863 | Abamectin (AVM B1a) | 99.5 ± 0.5 |
| L-669,437 | Nemadectin | 68.4 ± 5.3 |
| L-656,748 | 4"-Deoxy-4"-epi-methylamino AVM B1a | 86.4 ± 3.0 |
| L-676,897 | Avermectin B2a | 65.6 ± 7.1 |
| L-751,531 | 23-Oxo-AVM A2a | 65.3 ± 7.9 |
| L-697,960 | 13-Epi-O-MOM-AVM B2a aglycone | 34.0 ± 8.7 |
Data shown are mean ± S.E.M. of four determinations and represent the degree of inhibition of the peak glycine current after its third application in the presence of 1 μM avermectin. Experiments were carried out in the presence of 100 μM bicuculline.
AVM, avermectin; MOM, methoxymethyl.