Title : Pharmacologic characterization of the novel, orally available endothelin-A--selective antagonist SB 247083.

Pub. Date : 1998

PMID : 9595458






4 Functional Relationships(s)
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1 Competition radioligand binding with [125I]ET-1 at human cloned ETA and ETB receptors demonstrated ET-A selective affinity by SB 247083 (Ki 0.41 and 467 nM, respectively). Antimony endothelin receptor type A Homo sapiens
2 Competition radioligand binding with [125I]ET-1 at human cloned ETA and ETB receptors demonstrated ET-A selective affinity by SB 247083 (Ki 0.41 and 467 nM, respectively). Antimony endothelin receptor type B Homo sapiens
3 Competition radioligand binding with [125I]ET-1 at human cloned ETA and ETB receptors demonstrated ET-A selective affinity by SB 247083 (Ki 0.41 and 467 nM, respectively). Antimony endothelin receptor type A Homo sapiens
4 Therefore, the present study demonstrates that SB 247083, a unique chemical entity, represents a potent class of nonpeptide, orally active ETA-selective antagonists. Antimony endothelin receptor type A Homo sapiens