Lawrence J A, Poulin P, Lawrence D, Lederis K
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Calgary, Alta., Canada.
Brain Res. 1988 Apr 19;446(2):212-8. doi: 10.1016/0006-8993(88)90879-7.
Arginine-vasopressin (AVP) has been implicated as a putative central neurotransmitter or neuromodulator in some brain functions. This study demonstrates binding of [3H]AVP to rat brain homogenates that is pH and temperature dependent, is saturable (Kd = 0.77 nM, Bmax = 0.374 pmol/mg) and reversible. A number of AVP analogues competitively displaced the [3H]AVP binding, indicating that central AVP binding sites may have a resemblance to the peripheral (V1) AVP vasopressor receptor. Homogenate binding occurred predominantly in the microsomal fraction (P3) of the hypothalamus while in the hippocampus and septum binding was predominantly in the synaptosomal fraction (P2). Autoradiographic methods showed displaceable [3H]AVP binding in the lateral septum, amygdala, supraoptic, paraventricular and suprachiasmatic nuclei of the hypothalamus supporting the results of homogenate binding in preparations of these regions.
精氨酸加压素(AVP)被认为是某些脑功能中一种假定的中枢神经递质或神经调节剂。本研究表明,[3H]AVP与大鼠脑匀浆的结合具有pH和温度依赖性,具有饱和性(Kd = 0.77 nM,Bmax = 0.374 pmol/mg)且可逆。许多AVP类似物竞争性地取代了[3H]AVP的结合,表明中枢AVP结合位点可能与外周(V1)AVP血管升压素受体相似。匀浆结合主要发生在下丘脑的微粒体部分(P3),而在海马体和隔区,结合主要发生在突触体部分(P2)。放射自显影方法显示,在下丘脑的外侧隔区、杏仁核、视上核、室旁核和视交叉上核中存在可置换的[3H]AVP结合,这支持了这些区域制剂中匀浆结合的结果。