Ernsberger P, U'Prichard D C
Life Sci. 1986 Apr 28;38(17):1557-63. doi: 10.1016/0024-3205(86)90494-7.
Reversible and irreversible interactions of the photoreactive clonidine analogue p-azidoclonidine (PAZC) with brain alpha 2-adrenergic receptors were examined. In the absence of light, PAZC displayed selective, high affinity, competitive interactions with sites labeled by the alpha 2-agonist 3H-p-aminoclonidine (3H-PAC). Reversible binding characteristics resembled those of other alpha 2-agonists. Preincubation of bovine frontal cortex membranes with 100 nM PAZC followed by ultraviolet irradiation and thorough washing decreased alpha 2-receptor density 42% relative to controls receiving irradiation alone. The loss of receptors could be prevented by inclusion of 500 nM phentolamine in the preincubation medium. Alpha 1- and beta-adrenergic receptors were relatively unaffected. PAZC is a potential photoaffinity ligand for the alpha 2-adrenergic receptor.
研究了光反应性可乐定类似物对叠氮可乐定（PAZC）与脑α2 -肾上腺素能受体的可逆和不可逆相互作用。在无光条件下，PAZC与α2 -激动剂3H -对氨基可乐定（3H - PAC）标记的位点表现出选择性、高亲和力的竞争性相互作用。其可逆结合特性类似于其他α2 -激动剂。用100 nM PAZC预孵育牛额叶皮质膜，然后进行紫外线照射并充分洗涤，相对于仅接受照射的对照组，α2 -受体密度降低了42%。预孵育培养基中加入500 nM酚妥拉明可防止受体丢失。α1 -和β -肾上腺素能受体相对未受影响。PAZC是一种潜在的α2 -肾上腺素能受体光亲和配体。
