人类DP前列腺素类受体药理学和放射自显影法使用[(3)H] -BWA868C, DP receptor-selective拮抗剂放射性配体。
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谢里夫NA,威廉姆斯GW,戴维斯TL
人类DP前列腺素类受体药理学和放射自显影法使用[(3)H] -BWA868C, DP receptor-selective拮抗剂放射性配体。
Br J杂志。2000年11月,131 (6):1025 - 38。
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11082108 (在PubMed]
- 文摘
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1。一个强有力的和高度选择性DP前列腺素类受体拮抗剂放射性配体,[(3)H] -cyclohexyl-N-BWA868C (3-benzyl-5 - (6-carboxyhexyl) 1 -乙内酰脲(2-cyclohexyl-2-hydroxyethyl-amino), (((3) H) -BWA868C)),已经生成了受体结合和autoradiographic研究。2。特定的[(3)H] -BWA868C绑定人类血小板膜在23摄氏度,60分钟内达到平衡构成绑定总数的95%。协会(K(+ 1))和离解速率常数(K(1))的绑定是0.758 + / - -0.064分钟(1),更易与和0.0042 + / - -0.0002分钟(1),分别产生离解常数(K (D)) 5.66 + / 0。44 nM (n = 4)。3所示。特定[(3)H] -BWA868C绑定到DP与高亲和力受体(K (D) = 1.45 + / - -0.01 nM, n = 3)和有限的,饱和的结合位点(B (max) = 21.1 + / - -0.6 nmol g(1)湿重)。4所示。DP受体类前列腺素类(例如ZK118182, BW245C BWA868C, PGD(2)表现出高亲和力(摩尔)[(3)H] -BWA868C绑定,而前列腺素类选择性对EP、FP、IP和TP受体表现出低亲和力(微克)。 5. Specific DP receptor binding sites were autoradiographically localized on the ciliary epithelium/process, longitudinal and circular ciliary muscles, retinal choroid and iris in human eye sections using [(3)H]-BWA868C. While [(3)H]-PGD(2) yielded similar quantitative distribution of DP receptors as [(3)H]-BWA868C, the level of non-specific binding observed with [(3)H]-PGD(2) was significantly greater than that observed with [(3)H]-BWA868C. 6. It is concluded that [(3)H]-BWA868C is a high-affinity and very specific DP receptor radioligand capable of selectively labelling the DP receptor. [(3)H]-BWA868C may prove useful for future homogenate-based and autoradiographic studies on the DP receptor.