Identification of α2‐Adrenergic Receptors in Chicken Pineal Gland Using [3H]Rauwolscine

Identification of α2‐Adrenergic Receptors in Chicken Pineal Gland Using [3H]Rauwolscine
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使用 [3H]Rauwolscine 鉴定鸡松果体中的 α2-肾上腺素能受体

DOI:
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发表时间:
1988
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影响因子:
--
通讯作者:
Carla Ray
Carla Ray
中科院分区:
--
文献类型:
--
作者:
D. Bylund;P. Rudeen;L. Petterborg;Carla Ray

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去甲肾上腺素诱导的鸟类松果体N-乙酰转移酶活性抑制似乎是由α2-肾上腺素能受体介导的。在本研究中,通过放射性配体结合直接鉴定了鸡松果体中的α2-肾上腺素能受体。使用[3 H]萝芙木碱(一种选择性α2-肾上腺素能受体拮抗剂)检查了1 - 6周龄鸡松果体的膜制备物,以表征结合位点。结果表明,在检查的时间跨度内,受体结合位点的亲和力(KD)或密度(Bmax)均无本体论变化。结合是可饱和的,具有高亲和力,平均KD为0.27 ± 0.01 nM,平均Bmax为242 ± 12 fmol/mg蛋白。这些结合位点的进一步表征表明,α2-肾上腺素能受体是α2A亚型,因为哌唑嗪和ARC-239以低亲和力结合,羟甲唑啉以高亲和力结合。
The norepinephrine‐induced inhibition of avian pineal N‐acetyltransferase activity appears to be mediated by α2‐‐adrenergic receptors. In this study, α2‐adrenergic receptors in the chicken pineal gland were directly identified by radioligand binding. Membrane preparations of pineal glands from chickens from 1 to 6 weeks of age were examined using [3H]rauwolscine, a selective α2‐adrenergic receptor antagonist, to characterize the binding sites. The results indicate no ontological change in either the affinity (KD) or density of receptor binding sites (Bmax) during the time span examined. The binding was saturable and of high affinity with a mean KD of 0.27 ± 0.01 nM and a mean Bmax of 242 ± 12 fmol/mg protein. Further characterization of these binding sites indicated that the α2‐adrenergic receptor is of the α2A subtype, since prazosin and ARC‐239 bound with low affinities and oxymetazoline bound with high affinity.
配体结合实验的抑制数据的图形呈现和分析。
DOI: 10.1016/0003-2697(86)90306-4
发表时间: 1986
影响因子: 2.9
作者:
Bylund,DB
通讯作者: Bylund,DB
DOI: --
发表时间: 1985
影响因子: 3.6
作者:
Turner,JT;Ray-Prenger,C;Bylund,DB
通讯作者: Bylund,DB