Matheny J L, Ahlquist R P
Arch Int Pharmacodyn Ther. 1975 Nov;218(1):4-10.
The adrenergic receptor responses of isolated strips of iris dilator muscle from rabbits were studied. An alpha agonist, norepinephrine and a beta agonist, isoprenaline, were used to assess adrenergic sensitivity before and after pretreatment of tissues with metabolic inhibitors at 22, 29 and 37 degrees C. The metabolic inhibitors used were iodoacetic acid and dinitrophenol. Temperature change altered adrenoceptor sensitivity in the same manner before and after metabolic inhibition. Iodoacetic acid (10.4 mug/ml) pretreatment increased both alpha and beta responses. Dinitrophenol (1.8 mug/ml) pretreatment increased alpha and decreased beta responsiveness. The results obtained indicate that some metabolic process altered by dinitrophenol may be involved in this adrenoceptor interconversion seen when temperature is changed. This supports the theory that local environment determines the drug sensitivity (alpha or beta) of a single adrenergic receptor.
对兔虹膜开大肌分离条带的肾上腺素能受体反应进行了研究。使用α激动剂去甲肾上腺素和β激动剂异丙肾上腺素，在22、29和37摄氏度下用代谢抑制剂预处理组织前后，评估肾上腺素能敏感性。所用的代谢抑制剂为碘乙酸和二硝基苯酚。温度变化在代谢抑制前后以相同方式改变肾上腺素能受体敏感性。碘乙酸（10.4微克/毫升）预处理增加了α和β反应。二硝基苯酚（1.8微克/毫升）预处理增加了α反应并降低了β反应性。所得结果表明，二硝基苯酚改变的某些代谢过程可能参与了温度变化时所见的这种肾上腺素能受体相互转化。这支持了局部环境决定单个肾上腺素能受体的药物敏感性（α或β）的理论。
