Glover V, Medvedev A, Sandler M
Department of Paediatrics, Queen Charlotte's and Chelsea Hospital, London, UK.
Life Sci. 1995;57(22):2073-9. doi: 10.1016/0024-3205(95)02189-p.
Isatin (indole-2,3-dione) is an endogenous compound with anxiogenic properties. In the brain, highest levels (0.1 microgram/g) have been found in the rat hippocampus. In the present study, we show that isatin has little effect on a wide range of neurotransmitter and hormonal receptors but that it acts as an inhibitor of atrial natriuretic peptide (ANP) binding, with an IC50 of 4x 10(-7) M. It also inhibits ANP-activated particulate guanylate cyclase from rat kidney, heart and brain membranes in dose-dependent fashion, varying also with ANP concentration. These findings suggest that isatin is a new endogenous regulator of mammalian ANP activity, with potential implications for the control of both anxiety and natriuresis.
异吲哚酮（吲哚-2,3-二酮）是一种具有致焦虑特性的内源性化合物。在大脑中，已发现大鼠海马体中的含量最高（0.1微克/克）。在本研究中，我们表明异吲哚酮对多种神经递质和激素受体影响很小，但它可作为心房利钠肽（ANP）结合的抑制剂，IC50为4×10⁻⁷M。它还以剂量依赖的方式抑制大鼠肾脏、心脏和脑膜中ANP激活的颗粒型鸟苷酸环化酶，且随ANP浓度而变化。这些发现表明异吲哚酮是哺乳动物ANP活性的一种新的内源性调节剂，对焦虑和利钠作用的控制可能具有潜在意义。
