© Copyright 2009-2018 - Dipartimento di Scienze del Farmaco - Università di Catania - Città Universitaria Ed. 2 - Viale Andrea Doria, 6 - 95125 - Catania (Italy)
Ricerca >> Gruppi di Ricerca >> Gruppi della Sezione Chimica Farmaceutica >> Scheda pubblicazione
(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective sigma ligands with antagonist properties |
||||||
Abstract | A series of (+)-cis-N-normetazocine derivatives has been described, and their affinities for sigma1, sigma2, and phencyclidine (PCP) sites and opioid, muscarinic (M2), dopamine (D2), and serotonin (5-HT2) receptors were evaluated. The effect of the N-substitution with a substituted ethylamino spacer was investigated. Compounds 8c-11c displayed high affinities for sigma1 sites and for opioid receptors. Substitution of the second basic nitrogen either with alkyl or cycloalkyl substituents give compounds (1a-6a) with high affinity and selectivity for sigma1 binding sites. Compounds 1a-5a were further characterized in vivo, and their agonist/antagonist activity was evaluated. In mouse, compound 1a and 2a as well as haloperidol suppressed in a dose-related manner the stereotyped behavior induced by (+)-SKF 10,047. Compounds 3a-5a and (+)-pentazocine do not affect the stereotyped behavior induced by ip injection of (+)-SKF 10,047. Therefore, from this series of compounds we identified potent and selective sigma1 ligands which might prove useful to unveil the functional role of sigma1 sites | |||||
Autori |
|
|||||
Altri Autori | Cacciaguerra S. Spampanato Santi |
NEWS
19/Apr/16
Esito colloquio per conferimento Assegno di Ricerca CHIM 09 Esito colloquio A.R. ssd CHIM/09 |
11/Apr/16
BALLE DI SCIENZA http://www.ballediscienza-catania.it |
24/Mar/16
ATTIVITA' DI SUPPORTO ALLA DIDATTICA (vedi calendari) Fisica (CdLM CTF) Anatomia Umana (CdLM Farmacia) Fisica (CdLM Farmacia) Microbiologia (CdLM Farmacia) Fisiologia (CdL SFA) Fisica (CdL SFA) Microbiologia (CdL SFA) Informatica (CdL SFA)
|