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1.
РЖ ВИНИТИ 34 (BI48) 95.09-04Т1.332

   

    Opioid thermal antinociception in rhesus monkeys: Receptor mechanisms and temperature dependency [Text] / E. A. Walker [et al.] // J. Pharmacol. and Exp. Ther. - 1993. - Vol. 267, N 1. - P280-285 . - ISSN 0022-3565
Перевод заглавия: Опиоидная термическая антиноцицепция у обезьян-резусов: рецепторные механизмы и температурная зависимость
Аннотация: The antinociceptive effects of the opioid agonists etonitazene (I), and alfentanil (II), as well as the agonist/antagonists nalbuphine (III), [(1)-'бета'-2'-hydroxy-2,9-dimethyl-5-phenyl-6,7-benzomorphan (GPA 1657)] and profadol were studied in the warm water (48'ГРАДУС' and 55'ГРАДУС'C) tail-withdrawal assay in rhesus monkeys. A II, I, and III appear to produce antinociception through a mu opioid receptor. II and I appeared to have high efficacy at mu receptors as both compounds were fully effective at low and high water temperatures and quadazocine antagonized these effects equivalently. III appeared to have low efficacy properties at mu receptors, in that it was ineffective at the higher water temperature but blocked II antinociceptive effects at this temperature. In addition, quadazocine also potently antagonized the antinociceptive effects of III at the lower water temperature. GPA 1657 and profadol blocked II antinociceptive effects in 55'ГРАДУС'C water suggesting some antagonist effects at mu opioid receptors. However, GPA 1657 and profadol appeared to have additional antinociceptive effects at other opioid and nonopioid receptors. Each of these actions of GPA 1657 and profadol were limited by nonopioid convulsant effects at high doses. These studies suggest agonists may be differentiated based on antinociceptive effectiveness, receptor selectivity and intrinsic efficacy in the rhesus monkey tail-withdrawal procedure. США, Wayne State Univ., Detroit, MI 48202. Библ. 42
ГРНТИ  
ВИНИТИ 341.45.21.15.57.15.15
Рубрики: ОПИОИДЫ
ЭТОНИТАЗЕН

АЛФЕНТАНИЛ

НАЛБУФИН

ПРОФАДОЛ

ТЕСТ ОТДЕРГИВАНИЯ ХВОСТА

ПОГРУЖЕНИЕ В ГОРЯЧУЮ ВОДУ

АНТИНОЦИЦЕПЦИЯ

ОБЕЗЬЯНЫ


Доп.точки доступа:
Walker, E.A.; Butelman, E.R.; DeCosta, B.R.; Woods, J.H.


2.
РЖ ВИНИТИ 34 (BI24) 95.11-04М3.171

   

    Opioid thermal antinociception in rhesus monkeys: Receptor mechanisms and temperature dependency [Text] / E. A. Walker [et al.] // J. Pharmacol. and Exp. Ther. - 1993. - Vol. 267, N 1. - P280-285 . - ISSN 0022-3565
Перевод заглавия: Опиоидная термическая антиноцицепция у обезьян-резусов: рецепторные механизмы и температурная зависимость
Аннотация: The antinociceptive effects of the opioid agonists etonitazene (I), and alfentanil (II), as well as the agonist/antagonists nalbuphine (III), [(1)-'бета'-2'-hydroxy-2,9-dimethyl-5-phenyl-6,7-benzomorphan (GPA 1657)] and profadol were studied in the warm water (48'ГРАДУС' and 55'ГРАДУС'C) tail-withdrawal assay in rhesus monkeys. A II, I, and III appear to produce antinociception through a mu opioid receptor. II and I appeared to have high efficacy at mu receptors as both compounds were fully effective at low and high water temperatures and quadazocine antagonized these effects equivalently. III appeared to have low efficacy properties at mu receptors, in that it was ineffective at the higher water temperature but blocked II antinociceptive effects at this temperature. In addition, quadazocine also potently antagonized the antinociceptive effects of III at the lower water temperature. GPA 1657 and profadol blocked II antinociceptive effects in 55'ГРАДУС'C water suggesting some antagonist effects at mu opioid receptors. However, GPA 1657 and profadol appeared to have additional antinociceptive effects at other opioid and nonopioid receptors. Each of these actions of GPA 1657 and profadol were limited by nonopioid convulsant effects at high doses. These studies suggest agonists may be differentiated based on antinociceptive effectiveness, receptor selectivity and intrinsic efficacy in the rhesus monkey tail-withdrawal procedure. США, Wayne State Univ., Detroit, MI 48202. Библ. 42
ГРНТИ  
ВИНИТИ 341.39.15.29
Рубрики: ОПИОИДЫ
ЭТОНИТАЗЕН

АЛФЕНТАНИЛ

НАЛБУФИН

ПРОФАДОЛ

ТЕСТ ОТДЕРГИВАНИЯ ХВОСТА

ПОГРУЖЕНИЕ В ГОРЯЧУЮ ВОДУ

АНТИНОЦИЦЕПЦИЯ

ОБЕЗЬЯНЫ


Доп.точки доступа:
Walker, E.A.; Butelman, E.R.; DeCosta, B.R.; Woods, J.H.


 




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