title: EMD 57445, the selective sigma receptor ligand, has no effect on the 5-hydroxytryptamine system.
abstract: The behavioral and biochemical effects of EMD 57445, a selective sigma receptor ligand with potential antipsychotic activity, on the 5-hydroxytryptamine (5-HT) system were studied in rats and mice. The drug influence was investigated in three behavioral tests: 8-OH-DPAT (5-HT1A agonist)-induced behavioral syndrome in rats, m-chlorophenylpiperazine (m-CPP, 5-HT1B agonist)-induced hypothermia in mice and L-5-hydroxytryptophan (L-5-HTP)-induced head twitches (5-HT2A stimulation) in rats. EMD 57445 did not show any activity in all three behavioral models. In biochemical studies, no changes in the 5-HT and 5-HIAA levels in rat brain cortex, nucleus accumbens, striatum, hypothalamus and hippocampus were found. The results indicate that EMD 57445 does not interact with 5-HT (5-HT1A, 5-HT1B, 5-HT2A) receptor subpopulations and does not affect 5-HT metabolism.
authors.affiliation: Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.
authors.forename: G
authors.initials: G
authors.lastname: Skuza
authors.forename: Z
authors.initials: Z
authors.lastname: Rogóz
authors.forename: K
authors.initials: K
authors.lastname: Gołembiowska
mesh_terms: D006916:5-Hydroxytryptophan / Q000633:toxicity; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects / Q000502:physiology; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006897:Hydroxyindoleacetic Acid / Q000378:metabolism; D007035:Hypothermia / Q000139:chemically induced; D008024:Ligands; D008297:Male; D051379:Mice; D010080:Oxazoles / Q000378:metabolism / Q000494:pharmacology*; D010879:Piperazines / Q000633:toxicity; D010880:Piperidines / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000187:drug effects*; D017480:Receptors, sigma / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D017366:Serotonin Receptor Agonists / Q000494:pharmacology
chemical_list: D014150:Antipsychotic Agents; D008024:Ligands; D010080:Oxazoles; D010879:Piperazines; D010880:Piperidines; D011985:Receptors, Serotonin; D017480:Receptors, sigma; D017366:Serotonin Receptor Agonists; C103849:panamesine; D012701:Serotonin; D006897:Hydroxyindoleacetic Acid; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D006916:5-Hydroxytryptophan; C015068:1-(3-chlorophenyl)piperazine