Abstract：
:In the present study the antagonism of fentanyl pharmacodynamics was studied in the mouse and the receptor populations mediating the analgesic and lethal effects of fentanyl were examined. Both 1 and 8 days following implantation (s.c.) of a 15 mg naltrexone pellet there was a significant shift to the right of the fentanyl dose-response curves for analgesia and lethality. The analgesia dose-response curves were shifted significantly more (80- to 264-fold) than the lethality curves (13- to 16-fold) in the presence of naltrexone. In addition, acute naloxone (0.1 mg/kg s.c.), antagonized fentanyl analgesia more than lethality. Consequently, the relative safety ratio of fentanyl (LD50/ED50) was decreased in the presence of opioid antagonists. Pretreatment with naloxonazine (35 mg/kg s.c.) 24 h prior to testing effectively inhibited fentanyl-induced analgesia, but not fentanyl-induced lethality. However, pretreatment with beta-funaltrexamine (beta-FNA) (20 mg/kg, s.c.) 24 h prior to testing inhibited both fentanyl-induced analgesia and lethality. Implantation (s.c.) of a 75 mg morphine pellet for 72 h resulted in cross-tolerance to both fentanyl analgesia and lethality. However, the degree of the cross-tolerance was 1.8-fold for analgesia and 4.5-fold for lethality. Displacement studies of [3H]naltrexone by fentanyl in mouse brain homogenate indicated two populations of binding sites. Taken together, the pharmacodynamic studies and the binding studies suggest that fentanyl exerts its analgesic and lethal effects through different receptor populations.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Jang Y,Yoburn BCdoi
10.1016/0014-2999(91)90512-okeywords:
subject
Has Abstractpub_date
1991-05-17 00:00:00pages
135-41issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(91)90512-Ojournal_volume
197pub_type
杂志文章abstract：:Sex and stress hormones coordinate experience and behaviour with physiological regulations. In the brain the sex hormones act to promote the repertoire of affiliative and reproductive behaviours. Stress hormones target in particular brain circuits underlying emotional arousal and cognition. To exert these actions the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.10.017
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abstract：:The administration of radioactive angiotensin I to the retrogradely perfused feline adrenal gland caused a brisk discharge of catecholamines. Recovery of the labelled decapeptide and metabolites in the adrenal effluent fluid was complete in 5 min. Radioimmunoassay of this perfusate revealed that most of the peptide re...
journal_title：European journal of pharmacology
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doi：10.1016/0014-2999(76)90207-7
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abstract：:Experiments were conducted to explore the effects of Neuropeptide FF acting at spinal and supraspinal sites in models of chronic inflammatory or neuropathic pain and of acute pain. Neuropeptide FF was administered intrathecally (i.t.; 10.0, 25.0 and 50.0 nmol) or intracerebroventricularly (i.c.v.; 10.0, 12.5 and 15.0 ...
journal_title：European journal of pharmacology
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abstract：:Adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), adenosine, adenine and inosine were injected intradermally into the backs of human volunteers. ATP, ADP and AMP evoked weal and flare responses in the skin in a dose dependent manner. The rank order of potency was ATP greater tha...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90110-2
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abstract：:Effects of nicotine, and nicotine+vitamin E on glutathione reductase (Glutathione: NADP(+) oxidoreductase, EC 1.8.1.7) activity in the muscle, heart, lungs, testicles, kidney, stomach, brain and liver tissues were investigated in vivo and also in vitro. The groups were: nicotine [0.5 mg/kg/day, intraperitoneal (i.p.)]...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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abstract：:Germacrone is one of the main bioactive components in the traditional Chinese medicine Rhizoma curcuma. In this study, the anti-proliferative effect of germacrone on the human hepatoma cell lines and the molecular mechanism underlying the cytotoxicity of germacrone were investigated. Treatment of human hepatoma cell l...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00742-1
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journal_title：European journal of pharmacology
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doi：10.1016/j.ejphar.2004.09.056
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90364-2
更新日期：1981-04-09 00:00:00
abstract：:Possible changes in noradrenergic function were investigated in rat frontal cerebral cortex after acute treatment (1, 2 h) with the GABAB agonist, baclofen. A single i.p. injection of d,l-baclofen 10 mg/kg both reduced noradrenaline (NA) biosynthesis in vivo (31%) and the endogenous concentration of normetanephrine (N...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90369-2
更新日期：1991-05-02 00:00:00
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journal_title：European journal of pharmacology
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更新日期：1998-02-26 00:00:00
abstract：:Lycopene, a natural carotenoid, has potential chemopreventive effects in many cancers. This study aimed to examine the effects of lycopene on regulating the inflammation and apoptosis of N-nitrosomethylbenzylamine(NMBzA) induced esophageal cancer in F344 rats. After the rats were fed normal diets containing different ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90002-9
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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abstract：:Pentoxifylline (PTX), a non-specific inhibitor of cAMP phosphodiesterases, is commonly used for treatment of peripheral vascular disorders although its direct action on endothelial cells is not well described. The aim of this study was to determine the influence of PTX on tubule formation and mRNA expression for angio...
journal_title：European journal of pharmacology
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更新日期：2018-05-15 00:00:00
abstract：:In this study, the anti-inflammatory effects of flavonoids isolated from the roots of Glycyrrhiza uralensis (Leguminosae), namely, isoliquiritin (the glycoside of isoliquirigenin) and isoliquiritigenin (the aglycone of isoliquiritin) were evaluated on lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Isoliquirit...
journal_title：European journal of pharmacology
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