Add time:08/07/2019         Source:sciencedirect.com

The pharmacological profile of N-(6-(2-(5-bromopyrimidine-2-yloxy)ethoxy)-5-(4-methylphenyl)pyrimidin-4-yl)-4-(2-hydroxy-1,1-dimethylethyl) benzensulfonamide sodium salt sesquihydrate (TA-0201), a new antagonist of endothelin receptors, was examined, using human recombinant and prostate endothelin receptors. In binding experiments with [125I]endothelin-1, TA-0201 showed extremely high affinity for recombinant endothelin ETA receptors (pKi=10.7), as compared with that for recombinant endothelin ETB receptors (pKi=7.8). Endothelin ETA and ETB receptors coexisted in human prostate with different proportions (endothelin ETA receptor: approximately 70%), which were distinguished by TA-0201 in the same manner as with recombinant receptors. Human prostate strips contracted in response to endothelin-1 and sorafotoxin S6c, but the maximum contraction induced by endothelin-1 was approximately three times greater than that induced by sarafotoxin S6c. The response to endothelin-1, but not to sarafotoxin S6c, was inhibited by TA-0201 and cyclo(d-Asp-Pro-d-Val-Leu-d-Trp) (BQ123) (endothelin ETA receptor antagonist) but not by BQ788 (endothelin ETB receptor antagonist). These results suggest that TA-0201 is a highly selective endothelin ETA receptor antagonist and will be useful for understanding the physiological and pathological roles of the endothelin ETA receptor in human prostate and other tissues.

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