McAdams R P, Waterfall J F
Naunyn Schmiedebergs Arch Pharmacol. 1986 Dec;334(4):430-5. doi: 10.1007/BF00569382.
Age-related changes in presynaptic alpha-2 and postsynaptic alpha-1 adrenoceptors have been determined using the rat isolated vas deferens and the thoracic aorta, respectively. The IC50 values of clonidine, B-HT 933 and UK 14,304 for inhibition of the electrically evoked contractions of the vas deferens were significantly higher in 50 week old rats when compared with rats of 5 weeks. Similarly, EC50 values for the contraction of the thoracic aorta by noradrenaline, methoxamine and phenylephrine were significantly increased in 50 week old rats compared with 5 week old rats. No age-related changes in the potency of the selective alpha-2 adrenoceptor antagonists yohimbine and Wy 26392 were detected in the vas deferens. Similarly, there were no age-related changes in the alpha-1 adrenoceptor antagonist potency of indoramin or prazosin on the aorta. The results of the present study suggest that the potency of both alpha-1 and alpha-2 adrenoceptor agonists, as measured by their respective EC and IC50 values decreases with increasing age.
分别使用大鼠离体输精管和胸主动脉,测定了突触前α₂和突触后α₁肾上腺素能受体的年龄相关变化。与5周龄大鼠相比,50周龄大鼠中可乐定、B-HT 933和UK 14,304抑制输精管电诱发收缩的IC₅₀值显著更高。同样,与5周龄大鼠相比,50周龄大鼠中去甲肾上腺素、甲氧明和去氧肾上腺素使胸主动脉收缩的EC₅₀值显著增加。在输精管中未检测到选择性α₂肾上腺素能拮抗剂育亨宾和Wy 26392的效价存在年龄相关变化。同样,吲哚拉明或哌唑嗪对主动脉的α₁肾上腺素能受体拮抗剂效价也没有年龄相关变化。本研究结果表明,通过各自的EC和IC₅₀值测量,α₁和α₂肾上腺素能受体激动剂的效价均随年龄增长而降低。