Ostrowitzki S, Rao M L, Rédei J, Andres A H
Psychiatrische Klinik, Rheinische Friedrich-Wilhelms-Universität, Bonn, Federal Republic of Germany.
J Neural Transm Gen Sect. 1993;93(1):27-35. doi: 10.1007/BF01244935.
Changes in the central and peripheral serotonergic receptor activity have been reported to be involved in depression and suicidality. To elucidate the interdependence between central and peripheral receptor sites and their regulation by serotonin, we estimated intra-individual serotonin2 receptor binding characteristics in porcine cortex synaptosomes and in platelet membranes using 3H-LSD as ligand and ketanserin as competitor and quantified the relevant serotonin concentrations. A positive correlation between the apparent half maximal saturation concentration, KD, of the receptor in cortex synaptosomes and platelet membranes (r = 0.65, p = 0.0046, n = 18), and between the apparent maximal binding capacity, Bmax, of the receptor in cortex synaptosomes and platelets (r = 0.52, p = 0.027, n = 18) was observed. The blood serotonin concentrations correlated negatively with the maximal binding capacity, Bmax, in platelets (r = -0.77, p = 0.0002, n = 18). These results suggest that the binding characteristics of the central and peripheral serotonin2 receptor are similar, and that the platelet receptor activity may be regulated by blood levels of serotonin.
据报道,中枢和外周血清素能受体活性的变化与抑郁症和自杀行为有关。为了阐明中枢和外周受体位点之间的相互依存关系以及它们受血清素的调节,我们使用3H-LSD作为配体、酮色林作为竞争剂,估计了猪皮质突触体和血小板膜中个体内血清素2受体的结合特性,并对相关血清素浓度进行了定量。观察到皮质突触体和血小板膜中受体的表观半数最大饱和浓度KD之间呈正相关(r = 0.65,p = 0.0046,n = 18),以及皮质突触体和血小板中受体的表观最大结合容量Bmax之间呈正相关(r = 0.52,p = 0.027,n = 18)。血液血清素浓度与血小板中的最大结合容量Bmax呈负相关(r = -0.77,p = 0.0002,n = 18)。这些结果表明,中枢和外周血清素2受体的结合特性相似,并且血小板受体活性可能受血清素血液水平的调节。