A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors
A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors
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DOI：
10.1016/s0014-2999(02)02048-4
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发表时间：
2002-08-16
影响因子：
5
通讯作者：
Williams, DL
中科院分区：
文献类型：
--
作者：
Lemaire, W;O'Brien, JA;Williams, DL
一种新的、有效的非肽类催产素受体拮抗剂（1-（1-（2-（2，2，2-三氟乙氧基）-4-（1-甲磺酰基-4-哌啶基氧基）苯乙酰基）-4-哌啶基）-3，4-二氢-2（1H）-喹啉酮）已被鉴定，可被[S-35]标记至高比活性。在结合研究中，与人加压素受体相比，该化合物对人催产素受体表现出亚纳摩尔亲和力和高度选择性（900-1800倍）。这种化合物似乎适合于研究人类和非人类灵长类动物组织中催产素受体的药理学，目前缺乏高选择性的工具。它也可能是有用的作为一个非标记的竞争对手或作为放射性配体在放射自显影研究催产素受体定位在这些组织。(C)2002 Elsevier Science B.V保留所有权利。
A novel, potent nonpeptide oxytocin receptor antagonist (1-(1-(2-(2,2,2-trifluoroethoxy)-4-(1-methylsulfonyl-4-piperidinyloxy) phenylacetyl)-4-piperidinyl)-3,4-dihydro-2(1H)-quinolinone) has been identified that can be labeled to high specific activity with [S-35]. In binding studies, this compound exhibits sub-nanomolar affinity and a high degree of selectivity (900-1800-fold) for human oxytocin receptors compared to human vasopressin receptors. This compound appears suitable for studying the pharmacology of oxytocin receptors in human and nonhuman primate tissues, for which there is currently a paucity of highly selective tools. It may also be useful as a nonlabeled competitor or as a radioligand in autoradiographic studies of oxytocin receptor localization in these tissues. (C) 2002 Elsevier Science B.V All rights reserved.