September 2022 "The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran pests of cruciferous vegetables, and insights into regulation of its physiological processes contribute towards the development of new pesticides against it. Thus, we investigated the regulatory functions of its β-adrenergic-like octopamine receptor (PxOctβ3). The open reading frame (ORF) of PxOctβ3 was phylogenetically analyzed, and the levels of expression of the receptor mRNA were determined. This ORF was also cloned and expressed in HEK-293 cells. A series of octopamine receptor agonists and antagonists were tested against PxOctβ3. We showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative PCR showed that it was expressed at all developmental stages of P. xylostella. Octopamine activated PxOctβ3, resulting in increased levels of intracellular cAMP. Furthermore, the agonists naphazoline, clonidine, 2-phenethylamine, and amitraz activated the PxOctβ3 receptor, and naphazoline was the most effective. Only metoclopramide and mianserin had significant antagonistic effects on PxOctβ3, whereas yohimbine, phentolamine, and chlorpromazine lacked obvious antagonistic effects. The injection of double-stranded RNA in an RNA interference assay indicated that PxOctβ3 regulates development in P. xylostella. This study demonstrated the pharmacological properties and functions of PxOctβ3 in P. xylostella, thus, providing a theoretical basis for the design of pesticides that target octopamine receptors." Read more at the source #DrGPCR #GPCR #IndustryNews

can provide a comprehensive understanding of how drugs interact with different receptor regions and link Carlsson, J., Yoo, L., Gao, Z. G., Irwin, J. J., Shoichet, B. K., & Jacobson, K. A. (2010). D., Muñoz, L. L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L.

Here, we show that the gut IEL GLP-1 receptor (GLP-1R) is not required for enteroendocrine L cell GLP Such effects are mediated by the suppression of gut IEL effector functions linked to the dampening of These data reposition key roles of the L cell-gut IEL GLP-1R axis, revealing mechanisms linking GLP-1R

Authors Peter J P Croucher , Maya Ridinger , Pamela S Becker , Tara L Lin , Sandra L Silberman , Eunice

Contest Committee Sponsors GPCR Retreat Program < Back to schedule Cannabinoid compounds to augment L-DOPA

After exposure to 0.01-10 μg/L CPPDQ, obvious body accumulation of CPDDQ was detected. Meanwhile, exposure to CPPDQ (0.01-10 μg/L) decreased head thrash, body bend, and forward turn, and increased Nevertheless, only exposure to 10 μg/L CPPDQ induced neurodegeneration in GABAergic system. Exposure to CPPDQ (0.01-10 μg/L) further decreased expressions of daf-7 encoding TGF-β ligand, jnk-1 Additionally, among examined G protein-coupled receptor (GPCR) genes, exposure to CPPDQ (0.01-10 μg/L)