CONCURRENT DISSECTION AND INTRACAVAL RUPTURE OF AN ABDOMINAL AORTIC-ANEURYSM - CT FINDINGS
CONCURRENT DISSECTION AND INTRACAVAL RUPTURE OF AN ABDOMINAL AORTIC-ANEURYSM - CT FINDINGS
复制标题
DOI：
10.1097/00004728-198503000-00001
复制
发表时间：
1985-01-01
影响因子：
1.3
通讯作者：
SNYDER, SH
中科院分区：
文献类型：
--
作者：
FROST, JJ;WAGNER, HN;SNYDER, SH
卡芬太尼是一种有效的合成阿片类药物，可与.MU结合。阿片受体具有很高的亲和力(Ki=0.051 nM，37度)。c)。在大鼠大脑中，卡芬太尼对.MU的选择性分别是后者的90倍和250倍。阿片受体与增量相比较。还有.卡帕。分别是阿片受体。[11C]亚甲基与卡芬太尼的羧酸前体反应合成了碳-11-卡芬太尼。静脉注射碳-11-卡芬太尼。在人类和一只狒狒身上。用正电子发射断层扫描监测放射性在脑内的分布。在基底节和丘脑观察到较高的放射性浓度，在额叶和顶叶大脑皮层观察到中等浓度的放射性，在小脑和枕叶皮质观察到较低浓度的放射性；这一分布与用体外技术测量的阿片受体的已知区域密度相一致。阿片受体拮抗剂纳洛酮(1 mg/kg)可消除这种异质性分布。在注射后30-60分钟，纳洛酮对尾状核和丘脑内侧核结合的抑制率约为90%，因此，与非特异性结合部位相比，这种方法与阿片受体的特异性结合水平较高。在人体内测量阿片受体的能力使研究阿片受体被认为异常的各种神经和精神障碍以及研究阿片受体在中枢神经系统中的生理作用成为可能。
Carfentanil is a potent, synthetic opiate that binds to .mu. opiate receptors with very high affinity (KI = 0.051 nM, 37.degree. C). In rat brain, carfentanil is 90 and 250 times more selective for .mu. opiate receptors compared with .delta. and .kappa. opiate receptors, respectively. Carbon-11-carfentanil was synthesized by reacting [11C]methyliodide with the carboxylic acid precursor of carfentanil. Carbon-11-carefentanil was injected i.v. in man and a baboon. The distribution of the radioactivity in the brain was monitored using positron emission tomography. High concentrations of radioactivity were observed in the basal ganglia and thlamus, intermediate concentrations in the frontal and parietal cerebral cortex and low concentrations in the cerebellum and occipital cortex; this distribution corresponds to the known regional density of opiate receptors measuured using in vitro techniques. This heterogeneous distribution could be abolished by pretreatment with naloxone (1 mg/kg), an opiate antagonist. The percent inhibition of binding by naloxone is approximately 90% in the caudate nucleus and medial thalamus for 30-60 min after injection; therefore, this method is associated with a high level of specific binding to opiate receptors compared with nonspecific binding sites. The ability to measure opiate receptors in vivo in man makes it possible to study a variety of neurologic and psychiatric disorders in which opiate receptors are thought to be abnormal and to study physiologic role of opiate receptors in the CNS.