THE BETA-ADRENERGIC-RECEPTOR IN HUMAN-LYMPHOCYTES - SUBCLASSIFICATION BY THE USE OF A NEW RADIO-LIGAND, (+/-)-IODOCYANOPINDOLOL-125
THE BETA-ADRENERGIC-RECEPTOR IN HUMAN-LYMPHOCYTES - SUBCLASSIFICATION BY THE USE OF A NEW RADIO-LIGAND, (+/-)-IODOCYANOPINDOLOL-125
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DOI：
10.1016/0024-3205(81)90490-2
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发表时间：
1981-01-01
期刊：
影响因子：
6.1
通讯作者：
WEBER, F
中科院分区：
文献类型：
--
作者：
BRODDE, OE;ENGEL, G;WEBER, F
本文报道了一种对β-肾上腺素能受体具有高亲和力和特异性的新型放射性配体--(.+-.)-125Iodocyanopindolol(ICYP)用于鉴定和鉴定人淋巴细胞的β-肾上腺素能受体。ICYP与1.56+-的结合是饱和的。0.2fmolICYP以最大占有率和高亲和力(Kd=57.+-)与/106细胞特异性结合。7.1 PM，N=4)。酚妥拉明(10~(-4)M)或5-羟色胺(10~(-5)M)对ICYP的结合无明显影响。β1-选择性(心得安，美托洛尔)和β2-选择性(IPS 339，zinterol)肾上腺素能药物通过伪Scatchard图(Hofstee图)抑制结合的分析得到了线性图，表明人淋巴细胞中存在均一的β-肾上腺素能受体群体。由此得到的心得安(16.8微米)、美托洛尔(4.11微米)、津替洛尔(0.08微米)和IPS339(0.002微米)的Kd值表明，人淋巴细胞中存在的β-肾上腺素能受体属于β2-亚型。根据其低的非特异性结合和对β-肾上腺素能受体的高度特异性，ICYP似乎是长期研究人淋巴细胞β-肾上腺素能受体调节的理想配体。
(.+-.)-125Iodocyanopindolol (ICYP), a new radio-ligand with high affinity and specificity to .beta.-adrenoceptors was used to identify and characterize .beta.-adrenergic receptors in human lymphocytes. Binding of ICYP was saturable with 1.56 .+-. 0.2 fmol ICYP specifically bound/106 cells at maximal occupancy of the sites and of high affinity (KD = 57 .+-. 7.1 pM, N = 4). In contrast to 125Iodohydroxybenzylpindolol, ICYP-binding was not affected by phentolamine (up to 10-4 M) or serotonin (up to 10-5 M). Analysis of inhibition of binding via a pseudo-Scatchard-plot (Hofstee-plot) by .beta.1-selective (practolol, metoprolol) and .beta.2-selective (IPS 339, zinterol) adrenergic drugs resulted in linear plots suggesting the existence of a homogeneous population of .beta.-adrenergic receptors in human lymphocytes. The resulting KD values for practolol (16.8 .mu.M), metoprolol (4.11 .mu.M), zinterol (0.08 .mu.M) and IPS 339 (0.002 .mu.M) suggest that the .beta.-adrenergic receptor present in human lymphocytes is of the .beta.2-subtype. According to its low non-specific binding and its high specificity to .beta.-adrenergic receptors, ICYP appears to be an ideal ligand for long-term studies on the regulation of .beta.-adrenergic receptors of human lymphocytes.