Mansier P, Chevalier B, Barnett D B, Swynghedauw B
Unité INSERM U 127, Hôpital Lariboisière, Paris, France.
Pflugers Arch. 1993 Aug;424(3-4):354-60. doi: 10.1007/BF00384363.
The beta adrenergic (beta AR) and muscarinic (MR) receptors have been quantitated in parallel, using 125I-pindolol and 3H-quinuclidinylbenzilate, in a model of compensatory left ventricular (LV) hypertrophy (LVH), which developed in rats 4-6 weeks after an abdominal aortic stenosis. Since aortic banding resulted in a pronounced LVH of 62%, the results were expressed both in terms of density (fmol/mg protein) and quantity (fmol per LV). In addition, competition curves using either a specific beta 1-antagonist or isoproterenol or carbachol allowed the determination of the two beta AR subtypes and of the low and high affinity sites (defined by the inhibitory constant Ki) for both beta 1AR and MR. In LVH, receptor density decreased for each of total beta AR, beta 1AR subtype, high affinity (Ki 6-8 nM) beta 1AR sites (from 26 +/- 2 to 19 +/- 3 fmol/mg protein, P < 0.05), total MR and high affinity (Ki 12 nM) MR sites (from 63 +/- 6 to 40 +/- 4 fmol/mg protein, P < 0.001). The beta AR and MR densities dropped in parallel so that the MR/beta AR ratio remained unchanged. In sharp contrast (because the LVs were bigger) the quantities of total beta AR, beta 1AR subtype, beta 1AR high affinity sites, total MR and MR high affinity sites per LV were unmodified.(ABSTRACT TRUNCATED AT 250 WORDS)
在腹主动脉缩窄4 - 6周后大鼠所形成的代偿性左心室肥厚（LVH）模型中，使用125I - 吲哚洛尔和3H - 喹核醇基苯甲酸酯对β肾上腺素能（βAR）和毒蕈碱（MR）受体进行了平行定量。由于主动脉缩窄导致左心室显著肥厚达62%，结果以密度（fmol/mg蛋白质）和数量（每左心室fmol）表示。此外，使用特异性β1拮抗剂、异丙肾上腺素或卡巴胆碱的竞争曲线可确定两种βAR亚型以及β1AR和MR的低亲和力和高亲和力位点（由抑制常数Ki定义）。在左心室肥厚中，总βAR、β1AR亚型、高亲和力（Ki 6 - 8 nM）β1AR位点（从26±2降至19±3 fmol/mg蛋白质，P < 0.05）、总MR和高亲和力（Ki 12 nM）MR位点（从63±6降至40±4 fmol/mg蛋白质，P < 0.001）的受体密度均降低。βAR和MR密度平行下降，因此MR/βAR比值保持不变。形成鲜明对比的是（因为左心室更大），每左心室的总βAR、β1AR亚型、β1AR高亲和力位点、总MR和MR高亲和力位点的数量未改变。（摘要截短于250字）
