(+)-cis-N-ethyleneamino-N-normetazocine derivatives. Novel and selective σ ligands with antagonist properties

G Ronsisvalle, A Marrazzo, O Prezzavento…

Index: Ronsisvalle; Marrazzo; Prezzavento; Pasquinucci; Vittorio; Pittala; Pappalardo; Cacciaguerra; Spampinato Journal of medicinal chemistry, 1998 , vol. 41, # 10 p. 1574 - 1580

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Citation Number: 9

Abstract

A series of (+)-cis-N-normetazocine derivatives has been described, and their affinities for σ1, σ2, 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 σ1 sites and for opioid receptors. Substitution of the second basic nitrogen either with ...