caa a22 4500 465763111 CHVBK 20180323111904.0 cr unu---uuuuu 170327e19900301xx s 000 0 eng 10.1007/BF02896925 doi (NATIONALLICENCE)springer-10.1007/BF02896925 Effects of membrane fluidity on [3H]TCP binding to PCP receptors [Elektronische Daten] [Frank DePietro, James Byrd] Phencyclidine (PCP) binds with high affinity to the ion channel associated with the NMDA receptor. The binding of the PCP receptor-specific ligand TCP is greatly reduced at temperatures between 2°C and 6°C, at which the plasma membrane is in a rigid state. However, membrane rigidity alone does not appear to cause the reduced TCP binding, since the membrane fluidizing agent A2C did not increase TCP binding at 4°C; instead, it decreased binding at 21°C. This inhibitory effect of A2C on TCP binding was dose dependent and was highly correlated with A2C-induced increases in membrane fluidity. The IC50 of A2C inhibition was 8.9 mM, with a pseudo-Hill coefficient of −0.24. Scatchard analysis demonstrated that this effect was the result of an increase in the apparentK d of [3H]TCP for the PCP receptor, with no effect on theB max. These results suggest that the function of the NMDA-PCP receptor complex is impaired by increases in membrane fluidity. These findings may be pharmacologically relevant in understanding the mechanism of action of such agents as general anesthetics and ethanol, which cause increases in plasma membrane fluidity. Birkhäuser, 1990 DePietro Frank Developmental Neurobiology Program, Center for Neuroscience, Department of Psychiatry, University of Pittsburgh, Room E-1226, WPIC, 3811 O'Hara Street, 15213, Pittsburgh, PA, USA aut Byrd James Developmental Neurobiology Program, Center for Neuroscience, Department of Psychiatry, University of Pittsburgh, Room E-1226, WPIC, 3811 O'Hara Street, 15213, Pittsburgh, PA, USA aut Journal of Molecular Neuroscience Humana Press 2/1(1990-03-01), 45-52 0895-8696 2:1<45 1990 2 12031 https://doi.org/10.1007/BF02896925 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02896925 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- DePietro Frank Developmental Neurobiology Program, Center for Neuroscience, Department of Psychiatry, University of Pittsburgh, Room E-1226, WPIC, 3811 O'Hara Street, 15213, Pittsburgh, PA, USA aut NATIONALLICENCE 700 1- Byrd James Developmental Neurobiology Program, Center for Neuroscience, Department of Psychiatry, University of Pittsburgh, Room E-1226, WPIC, 3811 O'Hara Street, 15213, Pittsburgh, PA, USA aut NATIONALLICENCE 773 0- Journal of Molecular Neuroscience Humana Press 2/1(1990-03-01), 45-52 0895-8696 2:1<45 1990 2 12031 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer