Stone E A, U'Prichard D C
Eur J Pharmacol. 1981 Oct 22;75(2-3):159-61. doi: 10.1016/0014-2999(81)90078-9.
The binding of [3H]dihydroalprenolol to beta-adrenergic receptors in the rat brainstem was studied. Propranolol inhibited dihydroalprenolol binding to a greater extent than did isoproterenol or epinephrine. Scatchard plots obtained with propranolol were biphasic whereas those obtained with isoproterenol and epinephrine were monophasic. The results indicate that in the brainstem propranolol displaces dihydroalprenolol from sites other than beta-adrenergic receptors. Nonspecific binding of dihydroalprenolol in this tissue therefore cannot be assayed using propranolol but should be measured with isoproterenol or epinephrine.
研究了[3H]二氢心得舒与大鼠脑干中β-肾上腺素能受体的结合情况。普萘洛尔比异丙肾上腺素或肾上腺素更能抑制二氢心得舒的结合。用普萘洛尔得到的Scatchard图呈双相,而异丙肾上腺素和肾上腺素得到的图呈单相。结果表明,在脑干中普萘洛尔从β-肾上腺素能受体以外的位点置换二氢心得舒。因此,该组织中二氢心得舒的非特异性结合不能用普萘洛尔测定,而应用异丙肾上腺素或肾上腺素测定。