Lew R, Summers R J
Eur J Pharmacol. 1987 Aug 4;140(1):1-11. doi: 10.1016/0014-2999(87)90627-3.
The distribution of beta-adrenoceptors in slide-mounted dog kidney sections was determined using the radioligand (-)-[125I]cyanopindolol ((-)-[125I]CYP) and autoradiography. Using conditions designed to prevent (-)-[125I]CYP binding to non-beta-adrenoceptor sites, biochemical studies revealed that (-)-[125I]CYP binding equilibrated within 150 min (K1 = 3.2 X 10(8) M-1 min-1), was saturable (KD = 30.72 +/- 2.96 pM; Bmax = 0.57 +/- 0.03 fmol/section, n = 4) and stereoselective with respect to the stereoisomers of propranolol and pindolol. Delineation of beta-adrenoceptor subtypes with the selective beta 1-adrenoceptor antagonist betaxolol and beta 2-adrenoceptor antagonist ICI 118,551 demonstrated that the proportions of beta 1-: beta 2-adrenoceptors was between 1:6 and 1:11. Autoradiographic studies showed that beta 1-adrenoceptors were localized on the juxtaglomerular apparatus and glomeruli, while beta 2-adrenoceptors were localized on medullary rays. The distribution of beta-adrenoceptors with respect to renal function in the dog kidney is discussed.
使用放射性配体(-)-[125I]氰基吲哚洛尔((-)-[125I]CYP)和放射自显影法,测定了犬肾切片中β-肾上腺素能受体的分布。在设计用于防止(-)-[125I]CYP与非β-肾上腺素能受体位点结合的条件下,生化研究表明,(-)-[125I]CYP结合在150分钟内达到平衡(K1 = 3.2×10(8)M-1 min-1),具有饱和性(KD = 30.72±2.96 pM;Bmax = 0.57±0.03 fmol/切片,n = 4),并且对普萘洛尔和吲哚洛尔的立体异构体具有立体选择性。用选择性β1-肾上腺素能受体拮抗剂倍他洛尔和β2-肾上腺素能受体拮抗剂ICI 118,551对β-肾上腺素能受体亚型进行的描述表明,β1-:β2-肾上腺素能受体的比例在1:6至1:11之间。放射自显影研究表明,β1-肾上腺素能受体定位于近球小体和肾小球,而β2-肾上腺素能受体定位于髓放线。本文讨论了犬肾中β-肾上腺素能受体相对于肾功能的分布情况。