Trends in Pharmacological Sciences
Tips reviewMolecular characterization of endothelin receptors
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Clues to Glomerular Cell Chatter in Focal Segmental Glomerulosclerosis: Via Endothelin-1/ET<inf>A</inf>R
2021, Kidney International ReportsET<inf>A</inf> receptors are involved in the febrile response induced by high dose of bacterial endotoxin
2021, Journal of Thermal BiologyCitation Excerpt :These receptors have different selectivity to the ligand. ET-1 and ET-2 have greater affinity for the ETA receptor than ET-3, while the three ligands have similar affinity for the ETB receptor (Sakurai et al., 1992). ETA and ETB receptors share the same signaling pathway Gq/11 (Houde et al., 2016) although ETB receptors may also be associated with Gs and Gi, which promote activation or inhibition of adenylate cyclase, respectively, thus altering cyclic AMP levels (Davenport, 2002).
Endothelin and the heart in health and diseases
2019, PeptidesCitation Excerpt :The order of affinity of ETs for the first receptor type, designated ETA, is ET-1 > ET-2 > > ET-3. The second receptor type, designated ETB, shows equipotent affinity for all three ETs [41]. Exposure of cultured smooth muscle cells [42], Swiss 3T3 cells [43] and glomerular mesangial cells [44] to ET-1 for a long time causes a marked decrease in 125I-ET-1 binding sites, indicating an autologous down-regulation of ET receptors.
Neurobiology of opioid withdrawal: Role of the endothelin system
2016, Life SciencesCitation Excerpt :The biological responses of ET-1 are mediated via the activation of two distinct G protein coupled receptors (GPCRs): endothelin-A (ETA) [47] and endothelin-B (ETB) receptors [129]. While all three ETs have equal affinity for the ETB receptor, ET-3 has a lower affinity for the ETA receptor compared with either ET-1 or ET-2 [115]. The global distribution of ET and its binding sites in the brain suggests that, in addition to being a vasoactive agent, ET acts as an important regulatory neuropeptide in the CNS and affects many other biological functions [54,85,128].
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