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Identification of endothelin receptors in normal and hyperplasic human prostate tissues

✍ Scribed by Le Brun, Gaëlle; Moldovan, Florina; Aubin, Philippe; Ropiquet, Frédéric; Cussenot, Olivier; Fiet, Jean

Publisher
John Wiley and Sons
Year
1996
Tongue
English
Weight
447 KB
Volume
28
Category
Article
ISSN
0270-4137

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✦ Synopsis

Specific endothelin-1 (ET1) binding sites have been demonstrated in membranes derived from normal (NP) and benign hyperplasic (BPH) human prostate using an lZ5I-ETl binding assay. '=I saturation experiments and Scatchard analysis demonstrated the existence of a homogeneous population of binding sites with high affinity (Kd,,,) and density ( B , , , ) , respectively, 106 2 15 pM and 1086 5 399 fmoYmg protein for NP (n = 5) and 168 ? 26 pM and 964 2 445 fmoYmg protein for BPH (n = 5). We demonstrated the presence of two subtypes of ETl receptors, ETA and ETB, by means of the following ET1 competitors: ET2, ET3, and BQ123 (which is selective for the ETA receptor), and IRL1620 and sarafotoxine c (S6c) (which are selective for the ETB receptor). The displacement CuTves allowed us to conclude that the large majority (85%) of the ETl receptors in normal and hyperplasic human prostate are of the A subtype.

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