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荷包牡丹碱不敏感的γ-氨基丁酸受体：（-）-巴氯芬与大鼠小脑膜结合的研究

Bicuculline-insensitive GABA receptors: studies on the binding of (-)-baclofen to rat cerebellar membranes.

作者信息

Drew C A, Johnston G A, Weatherby R P

出版信息

Neurosci Lett. 1984 Dec 21;52(3):317-21. doi: 10.1016/0304-3940(84)90181-2.

DOI:10.1016/0304-3940(84)90181-2
PMID:6097844
Abstract

The binding of 3H-baclofen to synaptic membranes prepared from rat cerebellum was studied. Consistent with pharmacological data that (-)-baclofen is the more active stereoisomer, studies on the binding of 3H-baclofen showed increased specific binding, a higher affinity Kd and a lower Bmax than equivalent studies using 3H-baclofen. Divalent metal ions (mercury, lead, calcium and zinc) inhibited the binding of 3H-baclofen. The effects of some conformationally restricted analogues of gamma-aminobutyric acid (GABA) on 3H-baclofen binding indicated that GABA interacts with (-)-baclofen-sensitive binding sites (GABAB) in extended rather than folded conformations, and that folded analogues of GABA may interact with a class of binding site (GABAc?) insensitive to (-)-baclofen and bicuculline.

摘要

研究了3H-巴氯芬与大鼠小脑制备的突触膜的结合。与药理学数据一致，即(-)-巴氯芬是活性更高的立体异构体，对3H-巴氯芬结合的研究表明，与使用3H-巴氯芬的等效研究相比，特异性结合增加，亲和力Kd更高，Bmax更低。二价金属离子（汞、铅、钙和锌）抑制3H-巴氯芬的结合。一些γ-氨基丁酸（GABA）构象受限类似物对3H-巴氯芬结合的影响表明，GABA以伸展而非折叠构象与(-)-巴氯芬敏感结合位点（GABAB）相互作用，并且GABA的折叠类似物可能与一类对(-)-巴氯芬和荷包牡丹碱不敏感的结合位点（GABAc？）相互作用。

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Bicuculline-insensitive GABA receptors: studies on the binding of (-)-baclofen to rat cerebellar membranes.荷包牡丹碱不敏感的γ-氨基丁酸受体：（-）-巴氯芬与大鼠小脑膜结合的研究
Neurosci Lett. 1984 Dec 21;52(3):317-21. doi: 10.1016/0304-3940(84)90181-2.
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Characteristics of GABAB receptor binding sites on rat whole brain synaptic membranes.大鼠全脑突触膜上GABAB受体结合位点的特征
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Life Sci. 1983 Feb 21;32(8):879-87. doi: 10.1016/0024-3205(83)90225-4.
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Autoradiographic localization of binding sites for the gamma-aminobutyric acid analogues 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP)isoguvacine and baclofen on cultured neurons of rat cerebellum and spinal cord.γ-氨基丁酸类似物4,5,6,7-四氢异恶唑并[5,4-c]吡啶-3-醇（THIP）、异鹅膏蕈氨酸和巴氯芬在大鼠小脑和脊髓培养神经元上结合位点的放射自显影定位。
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J Med Chem. 1991 Aug;34(8):2557-60. doi: 10.1021/jm00112a033.

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