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膜中肾上腺素能配体的脂溶性。在β-肾上腺素能结合系统中的直接评估。

Adrenergic ligand liposolubility in membranes. Direct assessment in a beta-adrenergic binding system.

作者信息

Dax E M, Partilla J S

出版信息

Mol Pharmacol. 1982 Jul;22(1):5-7.

PMID:6289075
Abstract

The binding of [3H]dihydroalprenolol to adipocyte membranes may be displaced not only from beta-adrenergic receptors but also nonstereospecifically from other membrane compartments by beta-adrenergic and other adrenergic agents. The EC50 of this nonstereospecific displaceable binding is directly related to the liposolubility (n-octanol:water partition coefficient) of the displacing ligand.

摘要

[3H]二氢烯丙洛尔与脂肪细胞膜的结合不仅可从β-肾上腺素能受体上被取代,还可被β-肾上腺素能药物和其他肾上腺素能药物非立体特异性地从其他膜区室上取代。这种非立体特异性可取代结合的半数有效浓度(EC50)与取代配体的脂溶性(正辛醇:水分配系数)直接相关。

相似文献

1
Adrenergic ligand liposolubility in membranes. Direct assessment in a beta-adrenergic binding system.膜中肾上腺素能配体的脂溶性。在β-肾上腺素能结合系统中的直接评估。
Mol Pharmacol. 1982 Jul;22(1):5-7.
2
Characteristics of beta-adrenergic-agonist binding to rat adipocyte membranes. Evidence that (+/-)-[3H]hydroxybenzylisoproterenol interacts selectively with the adipocyte beta-adrenergic receptors.β-肾上腺素能激动剂与大鼠脂肪细胞膜结合的特性。(±)-[³H]羟基苄基异丙肾上腺素与脂肪细胞β-肾上腺素能受体选择性相互作用的证据。
Biochim Biophys Acta. 1982 Mar 15;715(1):105-15. doi: 10.1016/0304-4165(82)90055-1.
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Characterization of the beta-adrenergic receptors of hamster white fat cells. Evidence against an important role for the alpha 2-receptor subtype in the adrenergic control of lipolysis.仓鼠白色脂肪细胞β-肾上腺素能受体的特性。反对α2-受体亚型在肾上腺素能对脂肪分解的控制中起重要作用的证据。
Biochim Biophys Acta. 1983 Jun 23;731(3):397-405. doi: 10.1016/0005-2736(83)90034-2.
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Reconstitution of beta-adrenergic receptors into phospholipid vesicles: restoration of [125I]iodohydroxybenzylpindolol binding to digitonin-solubilized receptors.将β-肾上腺素能受体重组到磷脂囊泡中:恢复[125I]碘羟基苄基吲哚洛尔与洋地黄皂苷增溶受体的结合。
J Cyclic Nucleotide Res. 1980;6(6):407-19.
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Beta-adrenergic receptors in early human placenta characterization of [3H]-dihydroalprenolol binding.早期人胎盘中β-肾上腺素能受体的[3H]-二氢阿普洛尔结合特性研究
Life Sci. 1983 Apr 4;32(14):1583-90. doi: 10.1016/0024-3205(83)90864-0.
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Quantitative resolution of beta-adrenergic receptor subtypes by selective ligand binding: application of a computerized model fitting technique.通过选择性配体结合对β-肾上腺素能受体亚型进行定量解析:一种计算机化模型拟合技术的应用
Mol Pharmacol. 1979 Jul;16(1):1-9.
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[3H-dihydroalprenolol binding to beta-adrenergic receptors in adipocyte membrane fractions of rats premedicated with estrogens].[3H-二氢烯丙洛尔与经雌激素预处理的大鼠脂肪细胞膜组分中β-肾上腺素能受体的结合]
Sb Lek. 1993;94(1):63-70.
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Rat adipocyte beta-adrenergic receptors: evidence in favour of the heterogeneity of agonist-binding sites and against negatively cooperation interactions.大鼠脂肪细胞β-肾上腺素能受体:支持激动剂结合位点异质性及反对负协同相互作用的证据。
FEBS Lett. 1979 Aug 15;104(2):431-6. doi: 10.1016/0014-5793(79)80868-6.
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Quantitation of beta adrenergic receptors in rat liver: confounding effect of displaceable but nonstereospecific antagonist binding.
J Recept Res. 1981;2(3):267-83. doi: 10.3109/10799898109038804.
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Differentiation between amine transport and beta-adrenergic receptor-mediated binding in cultured mammalian cells.培养的哺乳动物细胞中胺转运与β-肾上腺素能受体介导的结合之间的差异。
Mol Pharmacol. 1985 Oct;28(4):338-47.

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