title: Synthesis and binding properties of novel selective 5-HT3 receptor ligands.
abstract: This work reports on the synthesis and affinities for the 5-HT(3) versus the 5-HT(4) receptor of new piperazinyl-substituted thienopyrimidine derivatives 20-45 with a view to identify potent and selective ligands for the 5-HT(3) receptor. Some of the new compounds show good affinity for the 5-HT(3) receptor and, notably, do not display any affinity for the 5-HT(4) receptor. 4-(4-Methyl-1-piperazinyl)-2-methylthio-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine 31 exhibits the highest affinity for the 5-HT(3) receptor (Ki = 33 nM) and behaves as noncompetitive antagonist.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Catania, viale A. Doria 6, 95125 Catania, Italy. mmodica@mbox.unict.it
authors.forename: Maria
authors.initials: M
authors.lastname: Modica
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Romeo
authors.forename: Luisa
authors.initials: L
authors.lastname: Materia
authors.forename: Filippo
authors.initials: F
authors.lastname: Russo
authors.forename: Alfredo
authors.initials: A
authors.lastname: Cagnotto
authors.forename: Tiziana
authors.initials: T
authors.lastname: Mennini
authors.forename: Róbert
authors.initials: R
authors.lastname: Gáspár
authors.forename: George
authors.initials: G
authors.lastname: Falkay
authors.forename: Ferenc
authors.initials: F
authors.lastname: Fülöp
mesh_terms: D000818:Animals; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D011485:Protein Binding; D051381:Rats; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism*; D018490:Serotonin Agents / Q000138:chemical synthesis* / Q000378:metabolism*; D013055:Spectrophotometry, Infrared
chemical_list: D008024:Ligands; D044406:Receptors, Serotonin, 5-HT3; D018490:Serotonin Agents