Pharmacology of [3H]apomorphine binding to bovine brain tissue.
Pharmacology of [3H]apomorphine binding to bovine brain tissue.
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[3H]阿扑吗啡与牛脑组织结合的药理学。
DOI：
10.1016/0006-2952(81)90515-3
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发表时间：
1981
影响因子：
5.8
通讯作者：
Harding,M
中科院分区：
文献类型：
--
作者：
Arana,GW;Baldessarini,RJ;Harding,M
使用氨基-6，7-二羟基四氢萘（ADTN）作为空白，评价了[3 H]阿扑吗啡（APO）对牛尾状核“突触体下”膜部分的高亲和力（nM）和超过80%的多巴胺（DA）激动剂可置换结合的活性。具有10，11-邻苯二酚和小N-烷基基团的Aporphines是有效的抑制剂（IC 50< 25 nM），具有平行的抑制曲线（nh = 0.8至1.0）。对于苯乙胺，儿茶酚和胺部分是重要的结构要求; α或β取代显著降低效价。因此，肾上腺素和异丙肾上腺素较弱，而DA及其N-甲基化同系物较强;（−）去甲肾上腺素（NE）和氟代DA的效力居中，（+）NE、其他儿茶酚和羟基化苯乙胺几乎无活性;间酪胺虽然较弱，但活性高于对酪胺。其他DA激动剂[ADTN>麦角腈> N-正丙基-3-（3-羟基苯基）-哌啶（3-PPP）>溴隐亭]具有活性。抗精神病药竞争相对较弱，与体内活动不完美的对应。立体选择性被发现与几个阿朴啡，苯乙胺，和抗精神病药物。许多其他神经抑制剂，包括胺摄取抑制剂和肾上腺素能受体，无活性。这些特征有力地表明，载脂蛋白O与哺乳动物脑组织中的DA激动剂结合位点相互作用。
Activity against high-affinity (nM), and over 80 per cent dopamine (DA)-agonist-displaceable binding of [3 H] apomorphine (APO) to a “subsynaptosomal” membrane fraction of bovine caudate nucleus was evaluated using amino-6, 7-dihydroxytetralin (ADTN) as a blank. Aporphines with 10, 11-catechol and small N-alkyl groups were potent inhibitors (IC 50< 25 nM) with parallel inhibition curves (n h= 0.8 to 1.0). For phenethylamines, catechol and amine moieties were important structural requirements; α or β substitution markedly reduced potency. Thus, epinephrine and isoproterenol were weak while DA and its N-methylated congeners were potent;(−) norepinephrine (NE) and fluoro-DAs were intermediate in potency and (+) NE, other catechols and hydroxylated phenethylamines were virtually inactive; m-tyramine, while weak, was more active than p-tyramine. Other DA agonists [ADTN> lergotrile> N-n-propyl-3-(3-hydroxyphenyl)-piperidine (3-PPP)> bromocriptine] were active. Neuroleptics competed relatively weakly, with imperfect correspondence to in vivo activities. Stereoselectivity was found with several aporphines, phenethylamines, and antipsychotic drugs. Many other neuropharmacologically active agents, including inhibitors of amine uptake and adrenergic receptors, were inactive. These characteristics strongly suggest that APO interacts with a DA agonist binding site in mammalian brain tissue.
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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
阿扑吗啡：化学、药理学、生物化学。
影响因子：
--
作者：
F. Colpaert;W. V. van Bever;J. Leysen
通讯作者：
J. Leysen
Spiperone：抗精神病受体的首选配体。
影响因子：
5.8
作者：
J. Leysen;W. Gommeren;P. Laduron
通讯作者：
P. Laduron
苯氧苯扎明抑制多巴胺刺激的腺苷酸环化酶活性。
影响因子：
5
作者：
Kenneth G. Walton;Peter Liepmann;Ross J. Baldessarini
通讯作者：
Ross J. Baldessarini
去甲肾上腺素结合和儿茶酚胺受体的寻找
影响因子：
64.8
作者：
P. Cuatrecasas;G. Tell;V. Sica;I. Parikh;Kwen
通讯作者：
Kwen