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[3H]螺哌隆与[3H]多潘立酮在哺乳动物视网膜和尾状核匀浆中的结合比较。

Comparison of the binding of [3H]spiperone and [3H]domperidone in homogenates of mammalian retina and caudate nucleus.

作者信息

Watling K J, Iversen L L

出版信息

J Neurochem. 1981 Nov;37(5):1130-43. doi: 10.1111/j.1471-4159.1981.tb04663.x.

DOI:10.1111/j.1471-4159.1981.tb04663.x
PMID:7299392
Abstract

The specific binding of [3H]spiperone and [3H]domperidone, as defined by 1 microM-(+)butaclamol, was compared in homogenates of bovine retina and caudate nucleus. Scatchard analyses of saturation data for [3H]spiperone binding yielded dissociation constants (Kd) of 0.35 nM in the retina and 0.64 nM in the caudate nucleus. Comparison of the maximum number of binding sites (Bmax) present in each tissue indicated that the density of sites in bovine caudate nucleus (270 fmol/mg protein) was approximately three times higher than in bovine retina (92 fmol/mg protein). This difference was even more marked in guinea pig tissues, with a ratio of 7:1 between corpus striatum and retina. The pharmacological analysis of [3H]spiperone binding in both the bovine retina and caudate nucleus indicated an interaction with dopaminergic rather than serotonergic sites. However, inhibition curves obtained to dopaminergic agonists in the bovine retina were significantly steeper than those observed in the bovine caudate nucleus, as reflected in the greater Hill coefficients obtained for these agents in the retina. Furthermore, only a small amount of specific [3H]domperidone binding was observed in either the bovine caudate nucleus or the guinea pig striatum, whilst no specific [3H]domperidone binding was detectable in homogenates of either bovine or guinea pig retina. These data suggest that the retina possesses only a small population of dopaminergic D2 sites and that these binding sites may differ from those present in the caudate nucleus.

摘要

用1微摩尔(+)丁酰苯,对[3H]螺哌隆和[3H]多潘立酮的特异性结合进行了测定,并在牛视网膜和尾状核匀浆中进行了比较。对[3H]螺哌隆结合的饱和数据进行Scatchard分析,得出视网膜中的解离常数(Kd)为0.35纳摩尔,尾状核中为0.64纳摩尔。对每个组织中存在的最大结合位点数(Bmax)进行比较表明,牛尾状核中的位点密度(270飞摩尔/毫克蛋白)大约是牛视网膜(92飞摩尔/毫克蛋白)中的三倍。在豚鼠组织中这种差异更为明显,纹状体与视网膜的比例为7:1。对牛视网膜和尾状核中[3H]螺哌隆结合的药理学分析表明,其与多巴胺能而非5-羟色胺能位点相互作用。然而,在牛视网膜中获得的多巴胺能激动剂抑制曲线明显比在牛尾状核中观察到的更陡,这反映在视网膜中这些药物获得的更大的希尔系数上。此外,在牛尾状核或豚鼠纹状体中仅观察到少量特异性[3H]多潘立酮结合,而在牛或豚鼠视网膜匀浆中未检测到特异性[3H]多潘立酮结合。这些数据表明,视网膜仅拥有少量的多巴胺能D2位点,并且这些结合位点可能与尾状核中的不同。

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Comparison of the binding of [3H]spiperone and [3H]domperidone in homogenates of mammalian retina and caudate nucleus.[3H]螺哌隆与[3H]多潘立酮在哺乳动物视网膜和尾状核匀浆中的结合比较。
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引用本文的文献

1
Retinal dopamine D1 and D2 receptors: characterization by binding or pharmacological studies and physiological functions.视网膜多巴胺D1和D2受体:通过结合或药理学研究及生理功能进行表征。
Cell Mol Neurobiol. 1990 Sep;10(3):303-25. doi: 10.1007/BF00711177.
2
Selective effects of low doses of apomorphine on spatiotemporal contrast sensitivity in healthy volunteers: a double-blind placebo-controlled study.低剂量阿扑吗啡对健康志愿者时空对比敏感度的选择性影响:一项双盲安慰剂对照研究。
Br J Clin Pharmacol. 1991 Nov;32(5):551-6. doi: 10.1111/j.1365-2125.1991.tb03950.x.