title: EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT1A receptor agonistic properties.
abstract: The 5-HT1A receptor agonist 8-hydroxy-(di-n-propylamino)tetralin (8-OH-DPAT; 0.55 mg/kg s.c.) and the 5-HT (5-hydroxytryptamine, serotonin) reuptake inhibitor/5-HT1A receptor ligand 5-[4-[4-(5-cyano-3-indolyl)-butyl]-1-piperazinyl]-benzofuran-2-carbox ami de (EMD 68843; 55 mg/kg p.o.) inhibited ultrasonic vocalization in rats, an effect which was antagonized by the 5-HT1A receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]-ethyl]-N-(2-pyridyl)- cyclohexancarboxamide (WAY 100635; 1.0 mg/kg s.c.). 8-OH-DPAT decreased body temperature in rats, an effect which was also antagonized by WAY 100635, whereas EMD 68843 neither affected body temperature by itself nor interacted with 8-OH-DPAT or WAY 100635. The selective 5-HT reuptake inhibitor fluoxetine (100 mg/kg p.o.) had no effect on ultrasonic vocalization or body temperature. Therefore EMD 68843 is suggested to be a 5-HT1A receptor agonist selective for presynaptic 5-HT1A receptors.
authors.affiliation: Merck KGaA, Department of CNS-Research, CNS-Pharmacology, Darmstadt, Germany.
authors.forename: G D
authors.initials: GD
authors.lastname: Bartoszyk
authors.forename: R
authors.initials: R
authors.lastname: Hegenbart
authors.forename: H
authors.initials: H
authors.lastname: Ziegler
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001572:Benzofurans / Q000494:pharmacology*; D001831:Body Temperature / Q000187:drug effects; D005473:Fluoxetine / Q000494:pharmacology; D007211:Indoles / Q000494:pharmacology*; D008297:Male; D010879:Piperazines / Q000494:pharmacology; D017729:Presynaptic Terminals / Q000187:drug effects*; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000187:drug effects*; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology*; D000069503:Vilazodone Hydrochloride
chemical_list: D001572:Benzofurans; D005473:Fluoxetine; D007211:Indoles; D010879:Piperazines; D011725:Pyridines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D017366:Serotonin Receptor Agonists; D017367:Selective Serotonin Reuptake Inhibitors; D000069503:Vilazodone Hydrochloride; C090413:N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide