Abstract
The properties of endothelin receptors on rat peritoneal macrophages were examined in in vitro receptor autoradiographic binding experiments and in a reverse transcription-polymerase chain reaction (RT-PCR) study. Dense and specific [ 125 I ]endothelin-1 binding sites were detected on the macrophages. [ 125 I ]Tyr 13–Suc–[Glu 9,Ala 11,15]–endothelin-1(8-21), IRL1620, a selective endothelin ET B receptor ligand, but not [ 125 I ]( N-[(hexahydro-1-azepinyl)carbonyl]) l-Leu(1-Me) d-Trp– d-Tyr, PD151242, a selective endothelin ET A receptor ligand, specifically bound to rat macrophages ( K d=0.75±0.19 nM, B max=7.77±2.50 fmol/mg). RT-PCR experiments also showed the expression of endothelin ET B receptor mRNA, but not endothelin ET A receptor mRNA, in these macrophages. These results indicate that rat peritoneal macrophages apparently express the endothelin ET B receptor but not the endothelin ET A receptor.
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