大鼠颌下腺中α2 -肾上腺素能受体与α2A -和α2B -肾上腺素能受体亚型之间的差异。
Differences between the alpha 2-adrenoceptor in rat submaxillary gland and the alpha 2A-and alpha 2B-adrenoceptor subtypes.
作者信息
Michel A D, Loury D N, Whiting R L
机构信息
Institute of Pharmacology, Syntex Research, Palo Alto, CA 94303.
出版信息
Br J Pharmacol. 1989 Nov;98(3):890-7. doi: 10.1111/j.1476-5381.1989.tb14618.x.
Abstract
- The alpha 2-adrenoceptors of rat submaxillary gland, labelled with [3H]-rauwolscine, were characterized by use of a range of subtype selective ligands and were compared to rabbit spleen alpha 2A-adrenoceptors and rat kidney alpha 2B-adrenoceptors. 2. In rat submaxillary gland, [3H]-rauwolscine labelled an apparently homogeneous population of binding sites with relatively low affinity (Kd = 11.65 nM) compared to the affinity in rat kidney (Kd = 2.18 nM) and rabbit spleen (Kd = 4.64 nM). 3. In competition studies using 16 ligands the alpha 2-adrenoceptors in rat submaxillary gland appeared to differ from both the alpha 2A-adrenoceptor of rabbit spleen (r = 0.62) and also the alpha 2B-adrenoceptor of rat kidney (r = 0.28). 4. The affinity data obtained with benoxathian, imiloxan and WB 4101 indicated the presence of an alpha 2B-adrenoceptor in rat submaxillary gland. However, data for chlorpromaxine, oxymetazoline, spiroxatrine and xylometazoline indicated that submaxillary gland alpha 2-adrenoceptors were of the alpha 2A subtype. The affinity estimate for prazosin in rat submaxillary gland was intermediate between its affinity at the alpha 2A- and alpha 2B-adrenoceptors while affinity estimates for idazoxan and phentolamine in rat submaxillary gland were greater than those obtained at either the alpha 2A- or alpha 2B-adrenoceptor. 5. These data indicate that rat submaxillary gland alpha 2-adrenoceptors differ from the alpha 2A- and alpha 2B-adrenoceptors found in rabbit spleen and rat kidney, respectively.
摘要
- 用[3H] - 萝芙辛标记的大鼠颌下腺α2 - 肾上腺素能受体，通过一系列亚型选择性配体进行表征，并与兔脾α2A - 肾上腺素能受体和大鼠肾α2B - 肾上腺素能受体进行比较。2. 在大鼠颌下腺中，与大鼠肾（Kd = 2.18 nM）和兔脾（Kd = 4.64 nM）中的亲和力相比，[3H] - 萝芙辛标记了一群亲和力相对较低（Kd = 11.65 nM）的明显同质的结合位点。3. 在使用16种配体的竞争研究中，大鼠颌下腺中的α2 - 肾上腺素能受体似乎与兔脾的α2A - 肾上腺素能受体（r = 0.62）以及大鼠肾的α2B - 肾上腺素能受体（r = 0.28）均不同。4. 用贝诺噻嗪、咪洛昔生和WB 4101获得的亲和力数据表明大鼠颌下腺中存在α2B - 肾上腺素能受体。然而，氯丙嗪、羟甲唑啉、螺沙屈林和赛洛唑啉的数据表明颌下腺α2 - 肾上腺素能受体属于α2A亚型。大鼠颌下腺中哌唑嗪的亲和力估计值介于其在α2A - 和α2B - 肾上腺素能受体处的亲和力之间，而大鼠颌下腺中咪唑克生和酚妥拉明的亲和力估计值大于在α2A - 或α2B - 肾上腺素能受体处获得的值。5. 这些数据表明大鼠颌下腺α2 - 肾上腺素能受体分别与兔脾和大鼠肾中的α2A - 和α2B - 肾上腺素能受体不同。
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