人血小板膜的血栓素A2/前列腺素H2受体与各种配体的pH依赖性结合。

pH-dependent binding of the TXA2/PGH2-receptor of human platelet membranes to various ligands.

作者信息

Theis J G, Dellweg H, Perzborn E, Gross R

机构信息

Institut für Herz/Kreislauf- und Artheroskleroseforschung, Bayer AG, Wuppertal, Germany.

出版信息

Agents Actions Suppl. 1992;37:222-7. doi: 10.1007/978-3-0348-7262-1_31.

DOI:10.1007/978-3-0348-7262-1_31

PMID:1385924

Abstract

[3H]-BAY U 3405 was used to characterize the pH-dependency of the binding of various ligands to the TXA2/PGH2-receptor of human platelet membranes. Maximum binding of [3H]-BAY U 3405 is achieved at pH 5.8. In inhibition studies the ligands Daltroban, CTA2, and U 46619 also show a higher affinity at pH 5.8 compared to pH 7.4. In contrast, the ligands I-PTA-OH and GR 32191 have a higher affinity at pH 7.4. No difference is seen with SQ 29548. The ligands I-PTA-OH, GR 32191, and SQ 29548 have a second protonable group in common, which is thought to be the reason for the different pH-dependent binding.

摘要

[3H]-BAY U 3405用于表征各种配体与人血小板膜TXA2/PGH2受体结合的pH依赖性。[3H]-BAY U 3405在pH 5.8时实现最大结合。在抑制研究中，与pH 7.4相比，配体达曲班、CTA2和U 46619在pH 5.8时也表现出更高的亲和力。相反，配体I-PTA-OH和GR 32191在pH 7.4时具有更高的亲和力。SQ 29548未见差异。配体I-PTA-OH、GR 32191和SQ 29548有一个共同的第二个可质子化基团，这被认为是pH依赖性结合差异的原因。