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用[125I]-SB 207710标记仔猪右心房中的一小部分5-羟色胺4（5-HT4）受体：功能相关性

Labelling with [125I]-SB 207710 of a small 5-HT4 receptor population in piglet right atrium: functional relevance.

作者信息

Kaumann A J, Lynham J A, Brown A M

机构信息

Human Pharmacology Laboratory, Babraham Institute, Cambridge.

出版信息

Br J Pharmacol. 1995 Jul;115(6):933-6. doi: 10.1111/j.1476-5381.1995.tb15900.x.

DOI:10.1111/j.1476-5381.1995.tb15900.x
PMID:7582523
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1909015/
Abstract
  1. We investigated the affinity of SB 207710 for sinoatrial 5-HT4 receptors and the density of right atrial 5-HT4 receptors with [125I]-SB 207710 in right atria of new-born piglets. 2. SB 207710 (1-100 nM) antagonized the 5-HT-evoked tachycardia surmountably with a pKB of 9.8. 3. [125I]-SB 207710 (5-1500 pM) labelled a small population of saturable binding sites with a pKD of 10.1 and with 5-HT4 receptor characteristics. The density of atrial binding sites with 5-HT4 receptor characteristics was 174 and 22 times lower respectively than those of atrial beta 1- and beta 2-adrenoceptors, labelled with (-)-[125I]-cyanopindolol. 4. We suggest that the small 5-HT4 receptor population may in part explain why the maximal tachycardia caused by 5-HT is smaller than that caused by catecholamines.
摘要
  1. 我们在新生仔猪的右心房中，用[125I]-SB 207710研究了SB 207710对窦房结5-HT4受体的亲和力以及右心房5-HT4受体的密度。2. SB 207710（1 - 100 nM）可克服性拮抗5-羟色胺诱发的心动过速，其pKB为9.8。3. [125I]-SB 207710（5 - 1500 pM）标记了一小部分可饱和结合位点，其pKD为10.1，具有5-HT4受体特征。具有5-HT4受体特征的心房结合位点密度分别比用（-）-[125I]-氰吲哚洛尔标记的心房β1 - 和β2 - 肾上腺素能受体密度低174倍和22倍。4. 我们认为，少量的5-HT4受体群体可能部分解释了为什么5-羟色胺引起的最大心动过速小于儿茶酚胺引起的最大心动过速。

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Naunyn Schmiedebergs Arch Pharmacol. 1994 May;349(5):546-8. doi: 10.1007/BF00169146.
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Naunyn Schmiedebergs Arch Pharmacol. 1990 Nov;342(5):619-22. doi: 10.1007/BF00169055.
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