Pharmacological Actions of Carbamate Insecticides at Mammalian Melatonin Receptors.

ABSTRACT: Integrated in silico chemical clustering and melatonin receptor molecular modeling combined with in vitro 2-[¹²⁵I]-iodomelatonin competition binding were used to identify carbamate insecticides with affinity for human melatonin receptor 1 (hMT₁) and human melatonin receptor 2 (hMT₂). Saturation and kinetic binding studies with 2-[¹²⁵I]-iodomelatonin revealed lead carbamates (carbaryl, fenobucarb, bendiocarb, carbofuran) to be orthosteric ligands with antagonist apparent efficacy at hMT₁ and agonist apparent efficacy at hMT₂ Furthermore, using quantitative receptor autoradiography in coronal brain slices from C3H/HeN mice, carbaryl, fenobucarb, and bendiocarb competed for 2-[¹²⁵I]-iodomelatonin binding in the supra

SUBMITTER: Glatfelter GC 

PROVIDER: S-EPMC7841424 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature