Gabizon R, Yetinson T, Schuldiner S
J Biol Chem. 1982 Dec 25;257(24):15145-50.
We have synthesized a new derivative of 5-hydroxytryptamine, a substrate of the biogenic amine transporter in bovine chromaffin granules. This new compound, 4-azido,3-nitrophenyl-azo-(5-hydroxytryptamine), is a competitive, reversible, and specific inhibitor of the biogenic amine transporter in the dark (Ki = 2 microM)., Upon illumination, the inactivation of the transporter becomes irreversible and follows an apparent first order rate kinetics (KINAC = 4 microM). The transporter can be protected if other substrates are present during illumination. When [3H]4-azido,3-nitrophenyl-azo-(5-hydroxytryptamine) is used, preferential labeling of one polypeptide (Mr approximately 45,000) is observed in the light, provided no other substrates of the transporter are present during illumination. We have tentatively identified this polypeptide as the transporter itself or one of its subunits.
我们合成了一种5-羟色胺的新衍生物，它是牛嗜铬颗粒中生物胺转运体的底物。这种新化合物，4-叠氮基-3-硝基苯基偶氮-(5-羟色胺)，是黑暗中生物胺转运体的竞争性、可逆性和特异性抑制剂（Ki = 2 microM）。光照后，转运体的失活变得不可逆，并遵循明显的一级速率动力学（KINAC = 4 microM）。如果在光照期间存在其他底物，则转运体可以得到保护。当使用[3H]4-叠氮基-3-硝基苯基偶氮-(5-羟色胺)时，在光照下观察到一种多肽（Mr约为45,000）的优先标记，前提是光照期间不存在转运体的其他底物。我们初步鉴定该多肽为转运体本身或其亚基之一。
