[3 h] rs - 15385 - 197,选择性和高亲和力为α2-adrenoceptors放射性配体:影响受体的分类。

文章的细节

引用

复制到剪贴板

麦金农AC,基尔帕特里克,肯尼BA, Spedding M,布朗厘米

[3 h] rs - 15385 - 197,选择性和高亲和力为α2-adrenoceptors放射性配体:影响受体的分类。

Br J杂志。1992年8月,106 (4):1011 - 8。

PubMed ID

1327384 (在PubMed

]

文摘

1。rs - 15385 - 197是最有效和选择性α2-adrenoceptor拮抗剂。我们使用rs - 15385 - 197 [3 h]定义α2-adrenoceptor亚型。绑定的rs - 15385 - 197 [3 h]鼠大脑皮层膜,老鼠新生儿肺和人类血小板是可逆的,饱和的高亲和力。饱和实验表明,[3 h] rs - 15385 - 197绑定到一个单一的人口的网站在所有3组织与高亲和力(0.08 - -0.14海里)。网站由[3 h]标记的密度rs - 15385 - 197是在大脑皮层(275 fmol mg-1蛋白质)比在新生儿肺(174 fmol mg-1蛋白质)和人类血小板(170 fmol mg-1蛋白质)。网站与[3 h]标记的密度rs - 15385 - 197标记的皮质明显大于[3 h]育亨宾(121 fmol mg-1蛋白质)。2。选择性α2-adrenoceptor拮抗剂,idazoxan,育亨宾,rauwolscine王寅26703流离失所的rs - 15385 - 197 [3 h]绑定到老鼠大脑皮层与山山坡上以简单的方式接近团结。这些拮抗剂的亲和力派生反对[3 h] rs - 15385 - 197类似于获得的位移值[3 h]育亨宾表明α2-adrenoceptor结合位点的性质。 3. alpha 2A-Adrenoceptor selective compounds, oxymetazoline and BRL 44409, showed high affinity for [3H]-RS-15385-197 binding in the human platelet and lower affinity in the neonate lung, while the alpha 2B-selective compounds, prazosin and imiloxan, showed high affinity for [3H]-RS-15385-197 binding in the neonate lung.This suggests that [3H]-RS-15385-197 labels both alpha2A- and alpha2B-adrenoceptor subtypes.4. Prazosin and methysergide inhibited the binding of [3H]-RS-15385-197 in the rat cerebral cortex in a simple manner consistent with an interaction at a single site. Although oxymetazoline inhibited [H]-RS- 15385-197 with a Hill slope significantly different from unity, the slope was increased to unity in the presence of Gpp(NH)p, suggesting an agonist-like interaction.5. The site labelled by [3H]-RS-15385-197 in the rat cortex shows high affinity for oxymetazoline and low affinity for prazosin which could be taken as evidence for classifying the site as an alpha2A-subtype.However, the affinities of yohimbine, rauwolscine and oxymetazoline at this site do not correspond to the population of sites in the human platelet. Yohimbine and rauwolscine were 20 fold selective for the platelet alph2A-subtype, whereas phentolamine was 2 fold and imiloxan was 10 fold selective for the cortex subtype. Indeed although the site showed some similarities with the alpha2A-subtype, the highest degree of homology was observed between this site and the rat submaxillary gland and the RG20 clone,tentatively called the alpha2D-adrenoceptor subtype. We propose that the alpha2-adrenoceptor in the rat cortex may therefore correspond to the putative alpha2D-subtype of the adrenoceptor.

beplay体育安全吗DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Oxymetazoline	Alpha-2A肾上腺素能受体	蛋白质	人类	是的	受体激动剂 部分激动剂	细节