Pharmacology of high-affinity binding of [3H](+/-)2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) to bovine caudate nucleus tissue.
Pharmacology of high-affinity binding of [3H](+/-)2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) to bovine caudate nucleus tissue.
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[3H](/-)2-氨基-6,7-二羟基-1,2,3,4-四氢萘 (ADTN) 与牛尾状核组织高亲和力结合的药理学。
DOI：
10.1016/0006-2952(83)90391-x
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发表时间：
1983
影响因子：
5.8
通讯作者：
Neumeyer,JL
中科院分区：
文献类型：
--
作者：
Arana,GW;Baldessarini,RJ;Lamont,JS;Amlicke,D;Neumeyer,JL
利用小牛脑组织的亚细胞部分(P4)，提高了[3 H](±)2-氨基-6，7-二羟基-1，2，3，4-四氢萘([3 H]-ADTN)的高亲和力结合。在尾状核中发现了最高浓度的结合位点，这一点得到了广泛的评价。当使用含有抗氧化剂的无阳离子介质时，0.5 nM[~H]-ADTN的结合在25°和pH 7.5~8.0时最佳，并且具有82-87%的可置换性。在此条件下，缔合时间为20min，解离时间为38min。缔合-解离动力学和配体饱和等温线分析表明，其表观亲和力(Kd)为1-2 nM，最大结合量(Bmax)为422fmoles/mg蛋白质。这一过程被证明是可逆的，并与几种有效的多巴胺激动剂单相竞争，希尔常数为1。发现8个异构体对具有立体选择性。[H]-ADTN结合3，4-二羟基苯乙胺和10，11-二羟基阿朴吗啡具有很强的多巴胺激动剂作用，但不能与肾上腺素能儿茶酚胺或其他儿茶酚或多巴胺摄取的阻滞剂结合。多巴胺拮抗剂的竞争更弱，与其体内活性的一致性较差。用[3 H]-ADTN和[3 H]-(−)阿朴吗啡测试的5 0种药物的IC50值之间有密切的一致性(r和SLOPE>；0.9)，支持基于[3 H]阿朴吗啡先前研究的多巴胺激动剂结合部位的构效特征的印象。
High-affinity binding of [3 H](±) 2-amino-6, 7-dihydroxy-1, 2, 3, 4-tetrahydronaphthalene ([3 H]-ADTN) was improved by use of a subcellular fraction (P 4) of tissue obtained from calf brain. The highest concentration of binding sites was found in caudate nucleus which was evaluated extensively. Binding of 0.5 nM [3 H]-ADTN was optimal at 25° and pH 7.5 to 8.0 when a cation-free medium containing antioxidants was used and was 82–87% displaceable (“specific”). The T 1 2 for association was 20 min, and for dissociation 38 min, under these conditions. Analysis of association-dissociation kinetics and of ligand saturation isotherms revealed an apparent affinity (K d) of 1–2 nM and a binding maximum (B max) of 422 fmoles/mg protein. The process proved to be reversible by, and monophasically competitive with, several potent dopamine agonists, with Hill constants dose to unity. Stereoselectivity was found with eight isomer-pairs. Binding of [3 H]-ADTN was selective for 3, 4-dihydroxyphenethylamines and 10, 11-dihydroxyaporphines with potent dopamine-agonist actions, but not for adrenergic catecholamines or other catechols, or blockers of dopamine uptake. Dopamine antagonists competed more weakly and in poor correspondence with their in vivo activities. There was a close correspondence between IC 50 values obtained for fifty of the agents tested with both [3 H]-ADTN and [3 H]-(−) apomorphine (r and slope> 0.9), supporting impressions of the structure-activity characteristics of dopamine agonist binding sites based on prior studies with [3 H]-apomorphine.
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3H-ADTN 和 3H-阿朴吗啡与小牛脑多巴胺受体的结合类似。
影响因子：
5
作者：
P. Seeman;G. Woodruff;J. Poat
通讯作者：
J. Poat
红藻氨酸损伤后，(3H)-ADTN 与大鼠纹状体微粒体和突触膜部分结合的变化。
影响因子：
5.8
作者：
A. Davis;G. Woodruff;J. Poat;S. Freedman
通讯作者：
S. Freedman
[3H]ADTN 与大鼠纹状体膜的结合。
影响因子：
5.8
作者：
W. W. Templeton;G. Woodruff
通讯作者：
G. Woodruff
[3H]阿扑吗啡与牛脑组织结合的药理学。
影响因子：
5.8
作者：
Arana,GW;Baldessarini,RJ;Harding,M
通讯作者：
Harding,M
2-氨基-6,7-[3H]二羟基-1,2,3,4-四氢萘的纹状体与两个多巴胺能位点的结合，其特征在于对精神安定药的低亲和力和高亲和力
影响因子：
6.1
作者：
S. List;K. Wreggett;P. Seeman
通讯作者：
P. Seeman