3H]thienyl-phencyclidine ([3H]TCP) binds to two different sites in rat brain. Localization by autoradiographic and biochemical techniques |
| |
| Authors: | J Vignon A Privat I Chaudieu A Thierry J M Kamenka R Chicheportiche |
| |
| Institution: | 1. Ecole Nationale Supe´rieure de Chimie, 24075 Montpellier France;2. U 249 Institut de Biologie, 34060 Montpellier Cedex France;1. Neuroscience Research Center, Neuropharmacology Institute, Kerman University of Medical Sciences, Kerman, Iran;2. Department of Anatomical Sciences, Afzalipour Medical Faculty, Kerman University of Medical Sciences, Kerman, Iran;1. Department of Psychology, California State University, San Bernardino, CA, USA;2. Department of Psychology, University of Nebraska-Lincoln, Lincoln, NE, USA;1. Department of Physiology, Faculty of Medicine, Demiroglu Bilim University, Istanbul, Turkey;2. Kocaeli University, Faculty of Medicine, Department of Pharmacology, Kocaeli, Turkey;3. Marmara University, Faculty of Pharmacy, Department of Pharmacology and Psychopharmacology Research Unit, Istanbul, Turkey;4. Department of Electrical and Electronics Engineering, İzmir Bakircay University, İzmir, Turkey;5. Kocaeli University, Faculty of Medicine, Department of Physiology, Kocaeli, Turkey |
| |
| Abstract: | A high affinity 3H]thienyl-phencyclidine (3H]TCP) binding and its similarity to that of 3H]phencyclidine (3H]PCP) have been demonstrated on whole rat brain homogenates. We now describe the regional distribution of the 3H]TCP binding sites in the rat brain with fixed sections and frozen slide-mounted sections visualized by autoradiography and with homogenates of 12 regions by direct binding experiments. The 3 techniques give a similar pattern for the 3H]TCP binding distribution and the biochemical study reveals that two distinct binding sites for 3H]TCP exist: one of high affinity (5-10 nM) in the forebrain, which should be responsible for the psychotropic effects and a second one of lower affinity (50-80 nM) in the hindbrain and the spinal cord, which should be involved in the extrapyramidal behavior induced by PCP and congeneers. Competition experiments have shown that muscarinic compounds interact only with the hindbrain receptor possibly in two different sites, although morphine interacts with a very low affinity with the forebrain's high affinity receptor. Results obtained with SKF-10,047 (N-allylnormetazocine) seem to indicate that TCP and sigma-receptors are different. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
