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Carbamate Insecticides Target Human Melatonin Receptors
Marina Popovska-Gorevski1, Margarita L Dubocovich1, Rajendram V Rajnarayanan1
1Department of Pharmacology and Toxicology, Jacobs School of Medicine and Biomedical Sciences, University at Buffalo , Buffalo, New York 14221, United States.
Chemical Research in Toxicology
|December 28, 2016
Summary
Toxic carbamate insecticides carbaryl and carbofuran mimic melatonin, binding to melatonin receptors. This interaction may disrupt human health by interfering with crucial regulatory processes.
Area of Science:
- Pharmacoinformatics
- Toxicology
- Molecular Pharmacology
Background:
- Carbaryl and carbofuran are highly toxic insecticides linked to various diseases.
- Melatonin receptors (MT1 and MT2) play key roles in regulating physiological processes.
Purpose of the Study:
- To investigate if carbaryl and carbofuran interact with melatonin receptors.
- To elucidate the potential mechanism of action of these insecticides on human health.
Main Methods:
- Integrated pharmacoinformatics screening to identify structural similarities.
- In silico molecular modeling to predict binding to MT1 and MT2 receptors.
- In vitro radioligand binding assays using human MT1 and MT2 receptors.
Main Results:
- Carbaryl and carbofuran were identified as structural mimics of melatonin.
- Both insecticides showed higher affinity for the MT2 receptor compared to MT1.
- GTP assays indicated distinct interactions with MT1 (antagonist/inverse agonist) and MT2 (agonist) receptors.
Conclusions:
- Carbaryl and carbofuran directly bind to human melatonin receptors.
- This binding represents a potential novel mechanism for insecticide-induced health effects.
- Disruption of melatonin receptor signaling may impact homeostatic balance.
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