Nonadrenergic Binding of [3H]Atipamezole in Rat Lung
Nonadrenergic Binding of [3H]Atipamezole in Rat Lung
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[3H]阿替帕唑在大鼠肺中的非肾上腺素结合
DOI：
10.1111/j.1749-6632.1995.tb32391.x
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发表时间：
1995
影响因子：
5.2
通讯作者：
M. Scheinin
中科院分区：
文献类型：
--
作者：
B. Sjöholm;J. Savola;M. Scheinin
[~3H]咪唑生和[~3H]对氨基可乐定最初都被认为是α-肾上腺素能受体的选择性放射性配体。然而，它们随后也被证明广泛地与脑和其他组织中的非肾上腺素能咪唑啉结合部位结合。1-5个咪唑啉偏爱结合部位或受体可介导某些咪唑啉类药物的中枢降压和增压作用。这些非肾上腺素能结合部位也可能在实验性中风模型中介导神经保护作用。咪唑啉受体也可能参与血管的收缩，而其他光滑的人类血小板膜上有可能参与血小板聚集的非肾上腺素能对氨基可乐定结合部位。在抑郁症患者中，它们的密度可能增加。喜欢咪唑啉的受体被分为几个亚类，它们之间的相对亲和力不同。I-受体I~-主要与可乐定和对氨基可乐定结合，定位于质膜，组织分布有限。I型受体优先结合咪唑沙星，存在于多种组织和细胞中。根据酚妥拉明和氨基甲胺的结合亲和力，1，-受体可以进一步细分为I，和I，I，型。用人和兔肝脏的亚细胞组分研究表明，[~3H]咪唑氧生与I，I，受体结合的部位局限于线粒体部分。L5血小板膜上有I型结合部位。因此，与定位于质膜的-肾上腺素受体结合不同，与I2结合的[~3H]咪唑恶生似乎至少位于肝细胞和血小板胞内。
Both [3H] idazoxan and [3H] para-aminoclonidine were initially thought to be selective radioligands for a,-adrenoceptors. However, they were subsequently also shown to bind extensively to nonadrenergic imidazoline binding sites in brain and other tissues. 1-5 Imidazoline-preferring binding sites or receptors were proposed to mediate the central antihypertensive6 and in~ ulin-increasing~.~ actions of some imidazolines. These nonadrenergic binding sites may also mediate neuroprotective effects in an experimental stroke model.'Imidazoline receptors may also participate in the contraction of vascular and other smooth Human blood platelets have nonadrenergic para-aminoclonidine binding sites that ma be involved in platelet aggregation. 12 Their density may be increased in depression. Imidazoline-preferring receptors have been divided into several subclasses which differ from each other with respect to their relative affinities for 1igat1ds. I~ One, the I,-receptor, preferentially binds clonidine and para-aminoclonidine, is localized to plasma membranes, and has limited tissue distribution. I,-receptors preferentially bind idazoxan and are present in a number of tissues and cell types. 1,-receptors may be further subdivided into I, and I,, types by the binding affinities of, for example, phentolamine and amiloride.Studies with subcellular fractions from human and rabbit liver have demonstrated that [3H] idazoxan binding to I,, sites is localized to mitochondrial fractions. l5 Blood platelets have I,,-type binding sites in their internal membranes. l6 Therefore, in contrast to a,-adrenoceptor binding, which is localized to the plasma membrane,[3H] idazoxan binding to I2 sites appears to be located intracellularly at least in liver cells and blood platelets.
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负鼠肾脏和 OK 细胞系中 α-2C 肾上腺素能受体亚型的表征。
DOI：
--
发表时间：
1991
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Blaxall,HS;Murphy,TJ;Baker,JC;Ray,C;Bylund,DB
通讯作者：
Bylund,DB
Alpha-2A 和 alpha-2B 肾上腺素能受体亚型：在仅含有一种亚型的组织和细胞系中结合的拮抗剂。
DOI：
--
发表时间：
1988
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Bylund,DB;Ray-Prenger,C;Murphy,TJ
通讯作者：
Murphy,TJ
影响因子：
56.9
作者：
LI, G;REGUNATHAN, S;REIS, DJ
通讯作者：
REIS, DJ
不同于 α2-肾上腺素能受体的咪唑啉/胍接受位点的表征。
DOI：
--
发表时间：
1989
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Parini,A;Coupry,I;Graham,RM;Uzielli,I;Atlas,D;Lanier,SM
通讯作者：
Lanier,SM
地昔帕明降低抑郁症患者血小板中氚化对氨基可乐定的结合。
影响因子：
--
作者：
Piletz,JE;Halaris,A;Saran,A;Marler,MR
通讯作者：
Marler,MR