The morphine-like properties of a series of aminoalkyl- and cycloalkylamino-naphtalenic derivatives of 17-methyl-17-azaequilenine were studied in rats trained to discriminate morphine (5.6 mg/kg IP) from vehicle in a two-lever operant behavioral procedure reinforced by water access. It was found that one of the compounds tested (i.e., A8; 1-ethyl-1-hydroxy-1-[2-(6-hydroxynaphthyl)]-2-methyl-3-dimethylaminopropane) fully generalized for the-morphine stimulus. The discriminative effects of 8s were stereospecific, as indicated by the fact that (+)-(1R,2R)-A8 was three rimes more potent than the racemic compound and that the (-)-(1S,2S) enantiomer was completely inactive. (+)-(1R,2R)-A8 generalization for the morphine cue was inhibited by naloxone. None of the other five derivatives examined generalized for the morphine stimulus. In conclusion, the naphthalenic structure is a source of compounds with stereospecific and naloxone-reversible morphine-like properties. (C) 2000 Elsevier Science Inc.

Stereoselective morphine-like discriminative properties of a new alkylaminonaphthalenic derivative / Sabina, Fraioli; Antonilli, Letizia; Nencini, Paolo. - In: PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR. - ISSN 0091-3057. - STAMPA. - 66:1(2000), pp. 199-204. ((Intervento presentato al convegno 4th International Pharmacology Biochemistry and Behavior tenutosi a MORZINE, FRANCE nel JAN 10, 2000 [10.1016/s0091-3057(00)00202-1].

Stereoselective morphine-like discriminative properties of a new alkylaminonaphthalenic derivative

ANTONILLI, Letizia;NENCINI, Paolo
2000

Abstract

The morphine-like properties of a series of aminoalkyl- and cycloalkylamino-naphtalenic derivatives of 17-methyl-17-azaequilenine were studied in rats trained to discriminate morphine (5.6 mg/kg IP) from vehicle in a two-lever operant behavioral procedure reinforced by water access. It was found that one of the compounds tested (i.e., A8; 1-ethyl-1-hydroxy-1-[2-(6-hydroxynaphthyl)]-2-methyl-3-dimethylaminopropane) fully generalized for the-morphine stimulus. The discriminative effects of 8s were stereospecific, as indicated by the fact that (+)-(1R,2R)-A8 was three rimes more potent than the racemic compound and that the (-)-(1S,2S) enantiomer was completely inactive. (+)-(1R,2R)-A8 generalization for the morphine cue was inhibited by naloxone. None of the other five derivatives examined generalized for the morphine stimulus. In conclusion, the naphthalenic structure is a source of compounds with stereospecific and naloxone-reversible morphine-like properties. (C) 2000 Elsevier Science Inc.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11573/255175
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