Sharma V K, Banerjee S P
J Biol Chem. 1977 Nov 10;252(21):7444-6.
The effects of thyroid status on muscarinic cholinergic receptors in the rat myocardium were investigated. The potent muscarinic antagonist [3H]quinuclidinyl benzilate was used to identify muscarinic cholinergic receptors in rat heart particulate fractions from control, hypothyroid, and hyperthyroid rats. Thyroidectomy increased specific [3H]quinuclidinyl benzilate binding to heart particulate fractions by about 60% as compared to euthyroid rat cardiac preparations. Administration of triiodothyronine to euthyroid rats decreased specific binding to muscarinic cholinergic receptors by about 20%. Scatchard analysis revealed that the cardiac particulate fraction from thyroidectomized rats contained 134 fmol of [3H]quinuclidinyl benzilate binding sites per mg of protein, as compared with 85 fmol/mg of protein found in the heart preparation of thyroidectomized rats chrinically treated with triiodothyronine. The equilibrium dissociation constant for the interaction of receptors with quinuclidinyl benzilate was the same (1 nM) in the heart particulate fractions derived from these two groups of rats. The results of this study demonstrate that thyroid hormone can regulate the number of cardiac muscarinic cholinergic receptors. Thus, the parasympathetic nervous system may participate in the cardiovascular abnormalities in different thyroid states.
研究了甲状腺状态对大鼠心肌毒蕈碱胆碱能受体的影响。使用强效毒蕈碱拮抗剂[3H]喹核醇基苯甲酸酯来鉴定来自对照、甲状腺功能减退和甲状腺功能亢进大鼠的大鼠心脏微粒体部分中的毒蕈碱胆碱能受体。与甲状腺功能正常的大鼠心脏制剂相比,甲状腺切除术使心脏微粒体部分对[3H]喹核醇基苯甲酸酯的特异性结合增加了约60%。给甲状腺功能正常的大鼠注射三碘甲状腺原氨酸使毒蕈碱胆碱能受体的特异性结合减少了约20%。Scatchard分析显示,甲状腺切除大鼠的心脏微粒体部分每毫克蛋白质含有134 fmol的[3H]喹核醇基苯甲酸酯结合位点,而在长期用三碘甲状腺原氨酸治疗的甲状腺切除大鼠的心脏制剂中发现每毫克蛋白质含有85 fmol。这两组大鼠心脏微粒体部分中受体与喹核醇基苯甲酸酯相互作用的平衡解离常数相同(1 nM)。本研究结果表明,甲状腺激素可调节心脏毒蕈碱胆碱能受体的数量。因此,副交感神经系统可能参与不同甲状腺状态下的心血管异常。