PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 chimeric ion channel agonist (EC50 values are 3.4 and 2.2 μM, respectively). Activates cortical neurons expressing PSAML141F,Y115F-5-HT3 chimeric ion channels and inhibits activity of neurons expressing PSAML141F-GlyR in vitro. Silences hypothalamic AGRP neurons transfected with PSAML141F-GlyR chimeric ion channels in mice in vivo, leading to suppression of feeding. Brain penetrant. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene.
Magnus et al (2011) Chemical and genetic engineering of selective ion channel-ligand interactions. Science 333 1292 PMID:21885782 |Cerritelli et al (2016) Activation of brainstem pro-opiomelanocortin neurons produces opioidergic analgesia, bradycardia and bradypnoea. PLoS One 11 e0153187 PMID:27077912