Pharmacological characterization of presynaptic α2‐autoreceptors in rat submaxillary gland and heart atrium
Pharmacological characterization of presynaptic α2‐autoreceptors in rat submaxillary gland and heart atrium
复制标题
大鼠颌下腺和心房突触前α2-自身受体的药理学特征
DOI：
10.1111/j.1476-5381.1992.tb14494.x
复制
发表时间：
1992
影响因子：
7.3
通讯作者：
K. Starke
中科院分区：
文献类型：
--
作者：
N. Limberger;A. Trendelenburg;K. Starke
1在大鼠离体颌下腺和心房研究突触前α2-受体的药理学特性。将组织块与[3 H]-去甲肾上腺素预孵育，然后用含有地昔帕明的培养基灌注，并进行电刺激。在一系列实验中，测定了12种α-肾上腺素受体拮抗剂的PEC 30值，即，使氚的电诱发溢出增加30%的浓度的负对数。在另一个系列中，测定了9种α-肾上腺素受体拮抗剂对5-溴-6-（2-咪唑啉-2-基氨基）-喹喔啉（UK 14304）释放抑制作用的pKD值，以及3种拮抗剂对甲氧胺释放抑制作用的pKD值。2在颌下腺中，拮抗剂的pEC 30值与其对UK 14304的pKD值呈良好的相关性（r = 0.93）。心房也是如此（r = 0.92）。3在颌下腺中，3种拮抗剂对UK 14304的pKD值与其对甲氧胺的pKD值非常相似，最大差异为0.4。心房也是如此，最大差异为0.3。4颌下腺和心房的pEC_（30）值呈显著正相关（r = 0.81）。pKD值也是如此（r = 0.79）。然而，pEC 30和pKD值也表明两种组织之间存在一致差异。5可以得出结论，咪唑啉UK 14304（α2-选择性）、苯乙胺去甲肾上腺素和苯乙胺甲氧胺（α1-选择性）的作用位点仅为α2-肾上腺素受体。没有迹象表明突触前α1-肾上腺素受体或突触前咪唑啉受体介导的UK 14304的作用。颌下腺中的α2-自身受体群与心房中的不同。6与文献研究的比较表明，颌下腺自身受体与牛松果体中发现的α2D放射性配体结合位点非常相似，可能也与大鼠颌下腺相似。心房自身感受器也与该部位最一致，但一致性更有限;心房自身感受器可能代表与α2D部位相关但不同的类型，或不同类型的混合物。
1 The pharmacological properties of presynaptic α2‐autoreceptors were studied in rat isolated submaxillary glands and atria. Tissue pieces were preincubated with [3H]‐noradrenaline, then superfused with medium containing desipramine, and stimulated electrically. In one series of experiments, pEC30 values of 12 α‐adrenoceptor antagonists were determined, i.e., negative logarithms of concentrations that increased the electrically evoked overflow of tritium by 30%. In another series, pKD values of 9 α‐adrenoceptor antagonists against the release‐inhibiting effect of 5‐bromo‐6‐(2‐imidazolin‐2‐ylamino)‐quinoxaline (UK 14304), and of 3 antagonists against the release‐inhibiting effect of methoxamine, were determined. 2 In submaxillary glands, the pEC30 values of the antagonists correlated well with their pKD values against UK 14304 (r = 0.93). The same was true for atria (r = 0.92). 3 In submaxillary glands, the pKD values of 3 antagonists against UK 14304 were very similar to their pKD values against methoxamine, with a maximal difference of 0.4. The same was true for atria where the maximal difference was 0.3. 4 The pEC30 values obtained in submaxillary glands correlated significantly with those obtained in atria (r = 0.81). The same was true for the pKD values (r = 0.79). However, the pEC30 and pKD values also indicated consistent differences between the two tissues. 5 It is concluded that the sites of action of the imidazoline UK 14304 (α2‐selective), the phenylethylamine noradrenaline, and the phenylethylamine methoxamine (α1‐selective) are exclusively α2‐adrenoceptors. There is no indication for presynaptic α1‐adrenoceptors or for an effect of UK 14304 mediated by presynaptic imidazoline receptors. The α2‐autoreceptor population in the submaxillary gland differs from that in the atrium. 6 Comparison with studies from the literature indicates that the submaxillary autoreceptors are closely similar to the α2D radioligand binding site found in the bovine pineal gland and probably the rat submaxillary gland. The atrial autoreceptors also conform best to this site, but the agreement is more limited; the atrial autoreceptors may represent a type related to, but distinct from, the α2D site, or a mixture of different types.
登录
查看更多内容
负鼠肾脏和 OK 细胞系中 α-2C 肾上腺素能受体亚型的表征。
DOI：
--
发表时间：
1991
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Blaxall,HS;Murphy,TJ;Baker,JC;Ray,C;Bylund,DB
通讯作者：
Bylund,DB
Alpha-2A 和 alpha-2B 肾上腺素能受体亚型：在仅含有一种亚型的组织和细胞系中结合的拮抗剂。
DOI：
--
发表时间：
1988
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Bylund,DB;Ray-Prenger,C;Murphy,TJ
通讯作者：
Murphy,TJ
编码α2-肾上腺素能受体亚型的大鼠基因组克隆的分离。
DOI：
--
发表时间：
1991
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Lanier,SM;Downing,S;Duzic,E;Homcy,CJ
通讯作者：
Homcy,CJ
牛松果体中α2D-肾上腺素能受体的鉴定和表征。
影响因子：
3.6
作者：
Simonneaux,V;Ebadi,M;Bylund,DB
通讯作者：
Bylund,DB
嘌呤参与甲氧胺释放去甲肾上腺素的调节。
影响因子：
5
作者：
Shinozuka,K;Sedaa,KO;Bjur,RA;Westfall,DP
通讯作者：
Westfall,DP