...
【24h】

Characterization of a new radioiodinated probe for the alpha2C adrenoceptor in the mouse brain.

机译:小鼠大脑中α2C肾上腺素受体的新型放射性碘探针的表征。

获取原文
获取原文并翻译 | 示例
           

摘要

[125I]17alpha-hydroxy-20alpha-yohimban-16beta-(N-4-p6 hydroxyphenethyl)carboxamide or [125I]rauwolscine-OHPC, a new radioiodinated probe derived from rauwolscine was synthesized and its binding characteristics investigated on sections of the mouse caudate putamen. [125I]rauwolscine-OHPC binding was saturable and revealed interaction with a single class of binding sites (KD= 0.171 nM, Bmax = 3082 pCi/mg of tissue). The kinetically derived affinity was in close agreement with the affinity evaluated by saturation experiments: k(-1)/k(+1)(0.0403 min(-1)/114 10(6) M(-1) min(-1))=0.35 nM. Competition studies revealed interaction with one single class of binding sites for each of the twelve compounds tested. The rank of potency suggested an interaction with alpha2 adrenoceptors (atipamezole > or = RX 821002 > yohimbine > (-)epinephrine). Moreover, the good affinity of [125I] rauwolscine-OHPC binding sites for spiroxatrine, yohimbine, WB 4101, the relatively good affinity for prazosin (Ki =37.4 nM) and the affinity ratio prazosin/oxymetazoline (37.4/43.4=0.86) were consistent with an alpha2C selective labelling of [125I]rauwolscine-OHPC. The distribution of [125I]rauwolscine-OHPC binding sites in mouse brain was characterized by autoradiography. The density of binding sites was high in the islands of Calleja, accumbens nucleus, caudate putamen and olfactory tubercles, moderate in the hippocampus, amygdala and anterodorsal nucleus of the thalamus. These findings demonstrated that [125I]rauwolscine-OHPC is a useful radioiodinated probe to label alpha2C adrenoceptors in mouse brain.
机译:[125I] 17alpha-hydroxy-20alpha-yohimban-16beta-(N-4-p6 hydroxyphenethyl)Carboxamide或[125I] rauwolscine-OHPC,合成了一种新的放射自碘化探针,来自劳乌斯卡因,其结合特性在小鼠尾状棘突上研究壳核。 [125I] rauwolscine-OHPC的结合是饱和的,并显示出与单类结合位点的相互作用(KD = 0.171 nM,Bmax = 3082 pCi / mg组织)。动力学得出的亲和力与饱和实验评估的亲和力非常一致:k(-1)/ k(+1)(0.0403 min(-1)/ 114 10(6)M(-1)min(-1) )= 0.35 nM。竞争研究表明,对于测试的十二种化合物中的每一种,其与一类单一的结合位点相互作用。效力等级表明与α2肾上腺素受体相互作用(阿替帕米唑>或= RX 821002>育亨宾>(-)肾上腺素)。此外,[125I]劳劳斯林-OHPC结合位点对螺索沙特林,育亨宾,WB 4101的亲和力良好,对哌唑嗪的亲和力相对较高(Ki = 37.4 nM),亲和力比为哌唑嗪/羟甲唑啉(37.4 / 43.4 = 0.86)。具有[125I] rauwolscine-OHPC的alpha2C选择性标记。通过放射自显影来表征[125I] rauwolscine-OHPC结合位点在小鼠脑中的分布。结合部位的密度在Calleja,伏隔核,尾状壳状核和嗅结节的岛中较高,在海马,杏仁核和丘脑的前房核中中等。这些发现表明,[125I] rauwolscine-OHPC是一种有用的放射性碘标记的探针,可标记小鼠脑中的α2C肾上腺素受体。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号