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本文引用的文献

1
A practical computer-based approach to the analysis of radioligand binding experiments.一种基于计算机的放射性配体结合实验分析实用方法。
Comput Programs Biomed. 1983 Aug-Oct;17(1-2):107-13. doi: 10.1016/0010-468x(83)90031-4.
2
Ligand: a versatile computerized approach for characterization of ligand-binding systems.配体：一种用于表征配体结合系统的通用计算机化方法。
Anal Biochem. 1980 Sep 1;107(1):220-39. doi: 10.1016/0003-2697(80)90515-1.
3
The effect of endothelin on noradrenergic transmission in rat and guinea-pig atria.内皮素对大鼠和豚鼠心房去甲肾上腺素能传递的影响。
Eur J Pharmacol. 1989 Sep 1;168(1):93-6. doi: 10.1016/0014-2999(89)90637-7.
4
Autoradiographical localization of binding sites for porcine [125I]endothelin-1 in humans, pigs, and rats: functional relevance in humans.
J Cardiovasc Pharmacol. 1989;13 Suppl 5:S166-70. doi: 10.1097/00005344-198900135-00045.
5
Endothelin induction of inositol phospholipid hydrolysis, sarcomere assembly, and cardiac gene expression in ventricular myocytes. A paracrine mechanism for myocardial cell hypertrophy.内皮素诱导心室肌细胞中肌醇磷脂水解、肌节组装及心脏基因表达。心肌细胞肥大的旁分泌机制。
J Biol Chem. 1990 Nov 25;265(33):20555-62.
6
[Ala1,3,11,15]endothelin-1 analogs with ETB agonistic activity.
Biochem Biophys Res Commun. 1991 Aug 30;179(1):286-92. doi: 10.1016/0006-291x(91)91367-l.
7
Molecular characterization of endothelin receptors.内皮素受体的分子特征
Trends Pharmacol Sci. 1992 Mar;13(3):103-8. doi: 10.1016/0165-6147(92)90038-8.
8
Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor.对ETA受体具有选择性的高效新型内皮素拮抗剂的生物学特性
Life Sci. 1992;50(4):247-55. doi: 10.1016/0024-3205(92)90331-i.
9
Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1.新型选择性配体BQ-123和[Ala1,3,11,15]ET-1揭示肺组织中内皮素受体亚型的不同分布
Biochem Biophys Res Commun. 1992 Jan 15;182(1):144-50. doi: 10.1016/s0006-291x(05)80123-8.

两种新型ETB选择性放射性配体[125I]-BQ3020和[125I]-[丙氨酸1,3,11,15]ET-1在人心脏中的特性研究

Characterization of two new ETB selective radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 in human heart.

作者信息

Molenaar P, Kuc R E, Davenport A P

机构信息

Clinical Pharmacology Unit, Addenbrooke's Hospital, Cambridge.

出版信息

Br J Pharmacol. 1992 Nov;107(3):637-9. doi: 10.1111/j.1476-5381.1992.tb14498.x.

DOI:10.1111/j.1476-5381.1992.tb14498.x
PMID:1472961
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1907740/
Abstract

Two new endothelin receptor radioligands, [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1, were characterized in tissue sections of human right atrium and left ventricle. Both radioligands had high affinity ([125I]-BQ3020 right atrium: KD = 0.145 +/- 0.037 nM, left ventricle: KD = 0.107 +/- 0.004 nM; [125I]-[Ala1,3,11,15]ET-1 right atrium: KD = 0.239 +/- 0.036 nM, left ventricle: KD = 0.199 +/- 0.027 nM). Competition binding experiments were performed in the left ventricle. The selective ETA receptor compound BQ123 competed with low affinity against [125I]-BQ3020 (KD = 28.7 +/- 2.7 microM) and [125I]-[Ala1,3,11,15]ET-1 (KD = 28.5 +/- 4.2 microM). The selective ETB receptor compound BQ3020 competed with high affinity against [125I]-BQ3020 (KD = 40.8 +/- 6.6 pM) and [125I]-[Ala1,3,11,15]ET-1 (KD = 0.276 +/- 0.099 nM). Another selective ETB receptor compound, [Ala1,3,11,15]ET-1 also competed with high affinity against [125I]-BQ3020 (KD = 0.663 +/- 0.120 nM) and [125I]-[Ala1,3,11,15]ET-1 (KD = 0.643 +/- 0.124 nM). These results indicate that [125I]-BQ3020 and [125I]-[Ala1,3,11,15]ET-1 are selective ETB receptor radioligands. [Ala1,3,11,15]ET-1 competed with the non-selective radioligand [125I]-ET-1 in left ventricle and revealed the presence of ETA and ETB receptors in the proportions of 76:24% respectively in the human left ventricle.

摘要

两种新的内皮素受体放射性配体，即[125I]-BQ3020和[125I]-[丙氨酸1,3,11,15]ET-1，在人右心房和左心室组织切片中进行了特性研究。两种放射性配体都具有高亲和力（[125I]-BQ3020在右心房：KD = 0.145±0.037 nM，在左心室：KD = 0.107±0.004 nM；[125I]-[丙氨酸1,3,11,15]ET-1在右心房：KD = 0.239±0.036 nM，在左心室：KD = 0.199±0.027 nM）。在左心室进行了竞争结合实验。选择性ETA受体化合物BQ123以低亲和力与[125I]-BQ3020（KD = 28.7±2.7 microM）和[125I]-[丙氨酸1,3,11,15]ET-1（KD = 28.5±4.2 microM）竞争。选择性ETB受体化合物BQ3020以高亲和力与[125I]-BQ3020（KD = 40.8±6.6 pM）和[125I]-[丙氨酸1,3,11,15]ET-1（KD = 0.276±0.099 nM）竞争。另一种选择性ETB受体化合物，[丙氨酸1,3,11,15]ET-1也以高亲和力与[125I]-BQ3020（KD = 0.663±0.120 nM）和[125I]-[丙氨酸1,3,11,15]ET-1（KD = 0.643±0.124 nM）竞争。这些结果表明，[125I]-BQ3020和[125I]-[丙氨酸1,3,11,15]ET-1是选择性ETB受体放射性配体。[丙氨酸1,3,11,15]ET-1在左心室与非选择性放射性配体[125I]-ET-1竞争，并揭示了人左心室中ETA和ETB受体的比例分别为76:24%。