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• W2023453199 abstract "1 The linear tetrapeptide radioligand, [125I]-PD151242 was used to characterize ETA receptors in human kidney which is an ETB-rich tissue. Saturation binding assays with [125I]-PD151242 revealed a single population of high affinity endothelin receptors: KD = 0.75 ± 0.07 nm and Bmax = 48.4 ± 1.6 fmol mg−1 protein (n = 3 individuals ± s.e.mean). Hill slopes were close to unity and a one site fit was preferred to a two site model. 2 ETA-receptor-selective ligands competed for [125I]-PD151242 binding with sub-nanomolar affinity: BQ123 KD = 0.43 ± 0.10 nm, Bmax = 46.6 ± 7.9 fmol mg−1 protein; FR139317, KD = 0.37 ± 0.06nM, Bmax = 39.5 ± 6.5 fmol mg−1 protein (n = 3 individuals ± s.e.mean). In each case, monophasic inhibition curves were obtained and a one site fit was preferred to a two site model. The ETB-selective agonist, BQ3020 at the highest concentration tested (10 μm) inhibited binding by only 50%. The non-selective RO462005 competed for the binding of [125I]-PD151242: KD = 1.31 ± 1.38 μm, Bmax = 33.0 ± 9.7 fmol mg−1 protein. Endothelin-2 and sarafotoxin S6B inhibited [125I]-PD151242 binding to renal tissue whereas ET-3 and sarafotoxin S6C were less effective. Non-endothelin and non-sarafotoxin peptides did not compete. 3 No degradation of [125I]-PD151242 was detected following incubation of the ligand with renal tissue under the conditions of the binding assay. 4 Polymerase chain reaction products corresponding to the expected size for mRNA encoding ETA and ETB receptor sub-types were detected in cortex and medulla in each of the five individuals examined. 5 Autoradiographical studies showed that ETA receptors visualised with [125I]-PD151242 were mainly localized to blood vessels including interlobular and arcuate arteries, arterioles and adjacent arcuate veins. ETB receptors localized with [125I]-BQ3020 were concentrated in the medulla and the density of binding to vessels was low. 6 These data suggest [125I]-PD151242 is selective for ETA receptors in human kidney and this sub-type is mainly localized to the renal vasculature. The results provide further evidence that the human vasculature mainly expresses the ETA receptor." @default.
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• W2023453199 date "1994-12-01" @default.
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• W2023453199 title "[125I]-PD151242: a selective ligand for endothelin ETA receptors in human kidney which localizes to renal vasculature" @default.
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• W2023453199 doi "https://doi.org/10.1111/j.1476-5381.1994.tb17140.x" @default.
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