Imaging of opioid receptors in the central nervous system.
Imaging of opioid receptors in the central nervous system.
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DOI：
10.1093/brain/awm255
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发表时间：
2008-05
期刊：
影响因子：
--
通讯作者：
Willoch F
中科院分区：
文献类型：
--
作者：
Henriksen G;Willoch F
通过正电子发射断层扫描（PET）进行的体内功能成像是提供中枢神经系统中μ-、κ和δ-阿片受体介导的信号传导的定量测量的唯一方法。在过去的二十年中，测量的变化，区域脑阿片样物质神经元激活介导的内源性产生的阿片肽，或外源性给药的阿片类药物，已进行了许多慢性疼痛的条件下，癫痫，以及兴奋剂和阿片类药物。尽管几种PET示踪剂已在临床上用于描述和定量阿片受体的变化，但调节阿片受体可用性变化的潜在机制仍不清楚。在介绍了与PET相关的阿片受体系统的一般信号传导机制后，对一些目前可用的PET示踪剂的药理学特性进行了严格的调查。临床研究进行了不同的PET配体也进行了审查和化合物依赖的结果进行了总结。展望总结与定制的示踪剂的属性，以促进选择性的地址动态变化的可用性的一个单一的子类，结合优化的量化框架是必要的，在体内阿片受体成像领域的进一步进展。
In vivo functional imaging by means of positron emission tomography (PET) is the sole method for providing a quantitative measurement of μ-, κ and δ-opioid receptor-mediated signalling in the central nervous system. During the last two decades, measurements of changes to the regional brain opioidergic neuronal activation—mediated by endogenously produced opioid peptides, or exogenously administered opioid drugs—have been conducted in numerous chronic pain conditions, in epilepsy, as well as by stimulant- and opioidergic drugs. Although several PET-tracers have been used clinically for depiction and quantification of the opioid receptors changes, the underlying mechanisms for regulation of changes to the availability of opioid receptors are still unclear. After a presentation of the general signalling mechanisms of the opioid receptor system relevant for PET, a critical survey of the pharmacological properties of some currently available PET-tracers is presented. Clinical studies performed with different PET ligands are also reviewed and the compound-dependent findings are summarized. An outlook is given concluding with the tailoring of tracer properties, in order to facilitate for a selective addressment of dynamic changes to the availability of a single subclass, in combination with an optimization of the quantification framework are essentials for further progress in the field of in vivo opioid receptor imaging.
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影响因子：
10.6
作者：
Bencherif, B;Wand, GS;Frost, JJ
通讯作者：
Frost, JJ
影响因子：
3.3
作者：
CHUNG, SK;COHEN, RS;PFAFF, DW
通讯作者：
PFAFF, DW
影响因子：
3.6
作者：
DEHAVENHUDKINS, DL;BROSTROM, PA;STERANKA, LR
通讯作者：
STERANKA, LR
影响因子：
14.5
作者：
BURN, DJ;RINNE, JO;BROOKS, DJ
通讯作者：
BROOKS, DJ
影响因子：
2.9
作者：
CONTRERAS, PC;TAM, L;RAFFERTY, MF
通讯作者：
RAFFERTY, MF