Ek B, Jodal M, Lundgren O
Acta Physiol Scand. 1987 Mar;129(3):353-60. doi: 10.1111/j.1748-1716.1987.tb08078.x.
In order to localize beta-adrenoceptors 125I-(-)pindolol (IPIN) was used in binding to sections from cat colon. The binding characteristics for IPIN to beta-adrenoceptors on colon sections were estimated by demonstrating reversible binding in the presence of isoprenaline and by steroselective binding to the isomers of propranolol. The binding of IPIN to both beta 1- and beta 2-adrenoceptors was shown by biphasic displacement curves in the presence of the selective beta-adrenoceptor compounds betaxolol, ICI 118.551 and procaterol. The colon sections were found to contain proportions of beta 1-adrenoceptors (30-50%) and beta 2-adrenoceptors (50-70%). In the autoradiographic studies, 100% of the developed grains after exposure of IPIN to the photographic emulsion were displaced by 50 microM of isoprenaline. By microscopic counting at autoradiographic grains, 30-40% of the grains were found in the circular smooth muscle, while 60-70% of the grains were found in the longitudinal smooth muscle. A concentration of 2 nM ICI 118.551 completely displaced all grains in the circular smooth muscle and partly displaced those found in the longitudinal smooth muscle. A high concentration of ICI 118.551 (1 microM) displaced all grains above background from the smooth muscle. It is concluded that the circular smooth muscle only contains beta 2-adrenoceptors, while longitudinal smooth muscle may contain a proportion of beta 1-adrenoceptors. Whether such a location of beta adrenoceptors can be related to the beta 1-adrenoceptor-mediated inhibition of colon motility can not be clarified from these studies.(ABSTRACT TRUNCATED AT 250 WORDS)
为了定位β-肾上腺素能受体,使用125I-(-)吲哚洛尔(IPIN)与猫结肠切片进行结合实验。通过在异丙肾上腺素存在下证明可逆结合以及对普萘洛尔异构体的立体选择性结合,来评估IPIN与结肠切片上β-肾上腺素能受体的结合特性。在选择性β-肾上腺素能受体化合物倍他洛尔、ICI 118.551和丙卡特罗存在的情况下,双相置换曲线表明IPIN与β1和β2肾上腺素能受体均有结合。发现结肠切片中含有一定比例的β1肾上腺素能受体(30 - 50%)和β2肾上腺素能受体(50 - 70%)。在放射自显影研究中,将IPIN暴露于感光乳剂后,100%的显影颗粒可被50微摩尔的异丙肾上腺素置换。通过对放射自显影颗粒进行显微镜计数,发现30 - 40%的颗粒位于环形平滑肌中,而60 - 70%的颗粒位于纵行平滑肌中。2纳摩尔的ICI 118.551可完全置换环形平滑肌中的所有颗粒,并部分置换纵行平滑肌中的颗粒。高浓度的ICI 118.551(1微摩尔)可置换平滑肌中高于背景的所有颗粒。结论是环形平滑肌仅含有β2肾上腺素能受体,而纵行平滑肌可能含有一定比例的β1肾上腺素能受体。这些研究无法阐明β肾上腺素能受体的这种定位是否与β1肾上腺素能受体介导的结肠运动抑制有关。(摘要截短于250字)