Cross-resistance to an inhibitor of chitin synthesis, TH 60-40, in insecticide-resistant strains of the house fly

1974 ◽  
Vol 22 (6) ◽  
pp. 1145-1146 ◽  
Author(s):  
David C. Cerf ◽  
George P. Georghiou
Keyword(s):  
House Fly ◽  
Cross Resistance ◽  
Chitin Synthesis ◽  
Resistant Strains

Patterns of Cross Resistance to Insecticides in the House Fly in Japan

1983 ◽  
pp. 411-419 ◽  
Author(s):  
Akio Kudamatsu ◽  
Akifumi Hayashi ◽  
Rokuro Kano
Keyword(s):  
House Fly ◽  
Cross Resistance

scholarly journals Lead Optimization of Dehydroemetine for Repositioned Use in Malaria

2020 ◽  
Vol 64 (4) ◽  
Author(s):  
Priyanka Panwar ◽  
Kepa K. Burusco ◽  
Muna Abubaker ◽  
Holly Matthews ◽  
Andrey Gutnov ◽  
...  
Keyword(s):  
De Novo ◽  
Antimalarial Activity ◽  
Drug Repositioning ◽  
Multidrug Resistant ◽  
Cross Resistance ◽  
Synthetic Analogue ◽  
80S Ribosome ◽  
Content Type ◽  
Resistant Strains

ABSTRACT Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel antimalarial treatments. The antiamoebic compound emetine dihydrochloride has been identified as a potent in vitro inhibitor of the multidrug-resistant strain K1 of Plasmodium falciparum (50% inhibitory concentration [IC50], 47 nM ± 2.1 nM [mean ± standard deviation]). Dehydroemetine, a synthetic analogue of emetine dihydrochloride, has been reported to have less-cardiotoxic effects than emetine. The structures of two diastereomers of dehydroemetine were modeled on the published emetine binding site on the cryo-electron microscopy (cryo-EM) structure with PDB code 3J7A (P. falciparum 80S ribosome in complex with emetine), and it was found that (−)-R,S-dehydroemetine mimicked the bound pose of emetine more closely than did (−)-S,S-dehydroisoemetine. (−)-R,S-dehydroemetine (IC50 71.03 ± 6.1 nM) was also found to be highly potent against the multidrug-resistant K1 strain of P. falciparum compared with (−)-S,S-dehydroisoemetine (IC50, 2.07 ± 0.26 μM), which loses its potency due to the change of configuration at C-1′. In addition to its effect on the asexual erythrocytic stages of P. falciparum, the compound exhibited gametocidal properties with no cross-resistance against any of the multidrug-resistant strains tested. Drug interaction studies showed (−)-R,S-dehydroemetine to have synergistic antimalarial activity with atovaquone and proguanil. Emetine dihydrochloride and (−)-R,S-dehydroemetine failed to show any inhibition of the hERG potassium channel and displayed activity affecting the mitochondrial membrane potential, indicating a possible multimodal mechanism of action.

scholarly journals Cross-Resistance Studies of Cry1Ac-Resistant Strains of Helicoverpa armigera (Lepidoptera: Noctuidae) to Cry2Ab

2007 ◽  
Vol 100 (3) ◽  
pp. 909-915 ◽  
Author(s):  
Shudong Luo ◽  
Kongming Wu ◽  
Yan Tian ◽  
Gemei Liang ◽  
Xue Feng ◽  
...  
Keyword(s):  
Helicoverpa Armigera ◽  
Cross Resistance ◽  
Helicoverpa Armígera ◽  
Resistant Strains ◽  
Lepidoptera Noctuidae

Penetration of diazoxon and acetyl choline into the thoracic ganglia in susceptible and resistant houseflies and the effects of fixatives

1963 ◽  
Vol 54 (2) ◽  
pp. 189-197 ◽  
Author(s):  
K. A. Lord ◽  
Frances M. Molloy ◽  
C. Potter
Keyword(s):  
Nervous System ◽  
Cause Of Death ◽  
Musca Domestica ◽  
House Fly ◽  
Thoracic Ganglion ◽  
Acetyl Choline ◽  
Thoracic Ganglia ◽  
Nerve Sheath ◽  
Resistant Strains ◽  
Barrier To Entry

The nerve sheath of the thoracic ganglion of the house-fly (Musca domestica L.) is readily permeable to diazoxon but is impermeable to acetyl choline and acetyl thiocholine. Acetone and other lipoidal solvents, but not formaldehyde, were found to destroy the barrier to entry of the substrates, acetyl choline and acetyl thiocholine, and it is inferred that the barrier is lipoidal. At − 16°C., acetone does not destroy the cholinesterase of the ganglion.Cholinesterase associated with the ganglion could be divided into three regions which showed different inhibition characteristics: (a) ‘ superficial ’ enzyme outside the nerve sheath, inhibited by 3·3 × 10−8M diazoxon; (b) ‘ peripheral ’ enzyme in the cellular region of the ganglion, inhibited by 3·3 × 10−8M and 3·3 × 10−9M diazoxon; (c) ‘ central ’ enzyme in the synaptic area, inhibited by not less than 3·3 × 10−7M diazoxon. Using inhibition of cholinesterase as an indicator of penetration, no difference in permeability was found between the ganglia of the susceptible and resistant strains. No difference was found in the inhibition of cholinesterase by diazoxon in the ganglia of susceptible and resistant strains.It is concluded from this and previous work that if inhibition of cholinesterase of the nervous system is the cause of death there are no differences between the ganglia of the susceptible and resistant strains which affect resistance; and, furthermore, that inhibition of cholinesterase in the thoracic ganglion is unlikely to be the cause of death.

Cross Resistance to Rabon in the House Fly Pressured with Diazinon in the Field and in the Laboratory12

1972 ◽  
Vol 65 (1) ◽  
pp. 6-8 ◽  
Author(s):  
L. G. Pickens ◽  
R. W. Miller ◽  
Donald L. Bailey
Keyword(s):  
House Fly ◽  
Cross Resistance
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