Silberring J, Lason W, Przewłocka B, Przewłocki R
Neuropeptides. 1986 Nov-Dec;8(4):367-76. doi: 10.1016/0143-4179(86)90008-9.
3H-Guanidinoethylmercaptosuccinic acid (3H-GEMSA) a very selective inhibitor of enkephalin convertase, binds to the crude rat spinal cord homogenates saturably, reversibly and with high affinity. Scatchard analysis revealed two classes of binding sites with KD: 4.5 nM and 215 nM. A plot of dissociation experiment was nonlinear with the T1/2: 2 min and 6 min, respectively. 3H-GEMSA binding sites are evenly distributed throughout the rat spinal cord and their high density might suggest a physiological significance of enkephalin convertase in that tissue.
3H-胍基乙基巯基琥珀酸(3H-GEMSA)是脑啡肽转换酶的一种非常有选择性的抑制剂,它以饱和、可逆且高亲和力的方式与大鼠脊髓粗匀浆结合。Scatchard分析显示有两类结合位点,解离常数(KD)分别为4.5 nM和215 nM。解离实验的曲线是非线性的,半衰期(T1/2)分别为2分钟和6分钟。3H-GEMSA结合位点在大鼠脊髓中分布均匀,其高密度可能表明脑啡肽转换酶在该组织中具有生理意义。