caa a22 4500 465739245 CHVBK 20180323111804.0 cr unu---uuuuu 170327e19900401xx s 000 0 eng 10.1007/BF02243998 doi (NATIONALLICENCE)springer-10.1007/BF02243998 [3H] sertraline binding to rat brain membranes [Elektronische Daten] [B. Koe, L. Lebel, W. Welch] Tritiated sertraline, a radiolabeled form of a potent and selective inhibitor of serotonin uptake, was found to bind with high affinity to rat whole brain membranes. Characterization studies showed that [3H] sertraline binding occurred at a single site with the following parameters:K d 0.57 nM,B max 821 fmol/mg protein,n h 1.06. This binding was reversible; the dissociation constant calculated from kinetic measurements (K d 0.81 nM) agreed with that determined by saturation binding experiments. [3H] Sertraline binding in the presence of serotonin, paroxetine, fluoxetine or imipramine suggested competitive inhibition of binding (large increase inK d with little change inB max). The rank order of potency of inhibition of [3H] sertraline binding was similar to that of inhibition of serotonin uptake for known uptake inhibitors and the 1-amino-4-phenyltetralin uptake blockers. A marked decrease in ex vivo [3H] sertraline binding in the brain of rats 7 days after treatment withp-chloroamphetamine was consistent with the loss of serotonin uptake sites induced by this agent. The results of our study indicated that [3H] sertraline labels serotonin uptake sites in rat brain. Springer-Verlag, 1990 [3H] Sertraline binding nationallicence Serotonin uptake nationallicence Uptake blockers nationallicence 1-Amino-4-phenyltetralins nationallicence Koe B. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut Lebel L. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut Welch W. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut Psychopharmacology Springer-Verlag 100/4(1990-04-01), 470-476 0033-3158 100:4<470 1990 100 213 https://doi.org/10.1007/BF02243998 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02243998 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Koe B. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut NATIONALLICENCE 700 1- Lebel L. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut NATIONALLICENCE 700 1- Welch W. Central Research Division, Pfizer Inc., 06340, Groton, CT, USA aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 100/4(1990-04-01), 470-476 0033-3158 100:4<470 1990 100 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer