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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Stereoselective morphine-like discriminative properties of a new alkylaminonaphthalenic derivative.
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Stereoselective morphine-like discriminative properties of a new alkylaminonaphthalenic derivative.

机译：一种新的烷基氨基萘衍生物的立体选择性吗啡样鉴别性能。

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摘要

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 A8 were stereospecific, as indicated by the fact that (+)-(1R,2R)-A8 was three times 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.
机译：在经过训练的双杠杆操作行为程序中，研究了将吗啡（5.6 mg / kg IP）与载体区分开的大鼠，研究了一系列17-甲基-17-氮杂喹啉的氨基烷基-和环烷基氨基-萘甲酸衍生物的类吗啡性质。通过水。发现所测试的化合物之一（即，A8; 1-乙基-1-羟基-1- [2-（6-羟基萘基）]-2-甲基-3-二甲基氨基丙烷）对吗啡刺激完全泛化。 A8的区分作用是立体特异性的，这一事实表明，（+）-（1R，2R）-A8的效力是外消旋化合物的三倍，并且（-）-（1S，2S）对映异构体是完全无活性的。纳洛酮抑制了吗啡提示的（+）-（1R，2R）-A8泛化。所检查的其他五种衍生物均未对吗啡刺激产生一般性影响。总之，萘结构是具有立体特异性和纳洛酮可逆的吗啡样性质的化合物的来源。

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