当前位置： SCI文献检索 > PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY期刊下所有文献 > U-50,488, a selective kappa opioid agonist: comparison to other reputed kappa agonists.

U-50,488, a selective kappa opioid agonist: comparison to other reputed kappa agonists.

Abstract：

:1. U-50,488 is a structurally novel, non-mu opioid. In the present experiments it was compared to the reputed kappa opioid agonists, ketazocine, ethylketocyclazocine and bremazocine as regards analgesic cross tolerance to morphine and U-50,488, antagonism of analgesia by naloxone and MR-2266 (in vivo pA2 determination), and narcotic antagonist properties (antagonism of morphine analgesia and precipitation of abstinence in morphine-dependent mice). 2. The analgesic mechanism of bremazocine was similar to that of U-50,488 but the former compound had, in addition, considerable mu-antagonist activity. The analgesic mechanisms of the ketazocines were less selective; both shared both mu and kappa agonist properties. U-50, 488, however, had no such mu agonist or antagonist effects and thus is a more selective kappa agonist. 3. This compound and its congeners may prove useful in the elucidation of the functions of kappa receptors in the central nervous system.

journal_name

Prog Neuropsychopharmacol Biol Psychiatry

journal_title

Progress in neuro-psychopharmacology & biological psychiatry

authors

Von Voigtlander PF,Lewis RA

doi

10.1016/s0278-5846(82)80130-9

subject

Has Abstract

pub_date

1982-01-01 00:00:00

pages

467-70

issue

4-6

eissn

0278-5846

issn

1878-4216

pii

S0278-5846(82)80130-9

journal_volume

6

pub_type

杂志文章

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