Kawahara R S, Byington K H, Bylund D B
Eur J Pharmacol. 1985 Oct 29;117(1):43-50. doi: 10.1016/0014-2999(85)90470-4.
We have synthesized and characterized p-azidoclonidine (AZC) as a putative alpha 2-adrenoceptor photoaffinity label. [3H]AZC demonstrated high affinity (KD = 11.8 +/- 2.5 nM), saturability (Bmax = 171 +/- 21 fmol/mg protein), stereo-specificity, and rank order of potency expected of a specific alpha 2-receptor label when used as a reversible ligand in the rat cerebral cortex. The pharmacologic profile of AZC was similar to p-aminoclonidine (PAC), an established alpha 2-adrenoceptor partial agonist. Membranes covalently prelabeled with nonradioactive AZC showed a dose dependent decrease in the number of alpha 2-receptor sites subsequently detected by [3H]PAC and [3H]yohimbine. Specific covalent [3H]AZC binding to rat cerebral cortical alpha 2-receptors represented 35 +/- 7% of the total [3H]AZC bound. These data indicate that AZC is a selective alpha 2-adrenoceptor photoaffinity label which may be useful in the identification and purification of the alpha 2-Adrenoceptor.
我们已经合成并表征了对叠氮可乐定（AZC），它是一种假定的α2-肾上腺素能受体光亲和标记物。[3H]AZC在大鼠大脑皮层中用作可逆配体时，表现出高亲和力（KD = 11.8 +/- 2.5 nM）、可饱和性（Bmax = 171 +/- 21 fmol/mg蛋白质）、立体特异性以及特定α2受体标记物预期的效价顺序。AZC的药理学特征与已确立的α2-肾上腺素能受体部分激动剂对氨基可乐定（PAC）相似。用非放射性AZC共价预标记的膜显示，随后用[3H]PAC和[3H]育亨宾检测到的α2受体位点数量呈剂量依赖性减少。特异性共价[3H]AZC与大鼠大脑皮层α2受体的结合占总结合[3H]AZC的35 +/- 7%。这些数据表明AZC是一种选择性α2-肾上腺素能受体光亲和标记物，可能有助于α2-肾上腺素能受体的鉴定和纯化。
