PMID: 9182242Feb 1, 1996Paper

Alkylation of [3H]8-OH-DPAT binding sites in rat cerebral cortex and hippocampus

Neurochemical Research
E K NénonénéT A Reader

Abstract

The binding of tritiated 8-hydroxy-2-(di-n-propyl-amino)tetralin, or [3H]8-OH-DPAT, to membranes from rat cerebral cortex and hippocampus could be inhibited by serotonin (5-HT) and buspirone, and by the 5-HT antagonists propranolol, NAN-190, pindolol, pindobind-5-HT(1A), WAY1OO135, spiperone and ritanserin. All competition curves, except for ritanserin, best fitted a two-site model. In vitro treatment of the membranes with N-ethylmaleimide (NEM), to alkylate sulfhydryl groups, caused dose-dependent decreases of binding; the inhibition curves were biphasic, and the effects irreversible. Reduction of disulfide bonds with L-dithiothreitol (L-DTT) also decreased binding, but in a monophasic way; these effects were fully reversible in cortex, but only partially reversible in hippocampus. In the latter region, but not in cerebral cortex, previous occupancy by [(3)H]8-OH-DPAT partially protected binding from the effects of both L-DTT and NEM, suggesting that the thiol groups in the receptor recognition site(s) of this brain region are readily accessible. The binding characteristics were examined with the aid of saturation curves, carried out with increasing concentrations, up to 140 nM, of [(3)H]8-OH-DPAT. The saturation data were sug...Continue Reading

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Citations

Mar 10, 2000·European Journal of Pharmacology·R H Alper, D L Nelson
May 23, 2013·Toxicology·Teresa L GarrettJames B Lucot
Sep 27, 2005·European Journal of Pharmacology·Yuji Odagaki, Ryoichi Toyoshima
Mar 13, 2001·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·A ScandroglioF Borsini
Dec 1, 1999·Biological Psychiatry·W C DrevetsC Mathis
Mar 30, 2001·Journal of Psychopharmacology·H Sánchez, D N Velázquez-Martínez

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