Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species

Evaluation of in vivo selective binding of [11C]doxepin to histamine H1 receptors in five animal species
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DOI:
10.1016/j.nucmedbio.2003.11.005
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发表时间:
2004-05-01
影响因子:
3.1
通讯作者:
Yanai, K
Yanai, K
中科院分区:
医学4区
文献类型:
--
作者:
Ishiwata, K;Kawamura, K;Yanai, K

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[C-11]doxepin已被用作放射配体,用于通过正电子发射断层扫描绘制人脑组胺H-1受体,其特异性结合在五种动物中进行了评估。在小鼠中,用冷多虑平和两种H-1受体拮抗剂治疗可以减少[C-11]多虑平的摄取,但用H-2/H-3拮抗剂治疗则没有。(+)-氯苯那敏(H-1拮抗剂)对小鼠、大鼠、家兔和猴的特异性结合在10-30%范围内,但在豚鼠中未检测到特异性结合。(C) 2004爱思唯尔公司版权所有。
The specific binding of [C-11]doxepin, which has been used as a radioligand for mapping histamine H-1 receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [C-11]doxepin uptake was reduced by treatment with cold doxepin and two H-1 receptor antagonists, but not with H-2/H-3 antagonists. The specific binding evaluated with treatment with (+)-chlorpheniramine (H-1 antagonist) was in the range of 10-30% in mouse, rat, rabbit, and monkey, but was not detected in guinea pig. (C) 2004 Elsevier Inc. All rights reserved.