Abnormal opioid system have been identified in addictive behavior and activity of the opioid system has also shown a strong link with the nutritional balance. A significant increase in endorphin levels was noticed after exercise, proportional to the duration and intensity of this activity. One brain imaging study showed an increase in opioid activity in athletes after endurance training. However , a decrease in opioid tone related to receptor desensitization in the brain has been raised in the sport and it is possible to feel like , the subject must perform physical exercise more frequently . Consequently, in order to deepen the hypothesis of addiction in high-level sport , the brain opioid activity should be assessed pre- training compared to a group of sedentary control subjects .
Preliminary results of a previous study the investigators are conducting on anorexia nervosa (AN ) show abnormalities that appear to be involved in self addiction anorexia nervosa and the regulation of gonadal function. However, the relation of cause and effect between these anomalies and undernutrition remains to be determined . Given the addictive component in the endurance sport and the variability of the nutritional status of its practitioners , evaluation of brain activity in these subjects could provide additional answers.

开始日期2014-09-15

申办/合作机构

Centre Hospitalier Universitaire de Saint-Etienne

100 项与 Diprenorphine 相关的临床结果

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100 项与 Diprenorphine 相关的转化医学

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100 项与 Diprenorphine 相关的专利（医药）

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534

项与 Diprenorphine 相关的文献（医药）

2025-11-01·NEUROPHARMACOLOGY

Comparison of ventilatory depression by carfentanil, fentanyl, and heroin, and reversal by opioid receptor antagonists in rats

Article

作者: France, Charles P ; Flynn, Shawn M

Fentanyl and its analogs continue to drive the overdose crisis in the United States. It is unclear whether there are unique properties of fentanyls that increase the risk of opioid overdose compared with other opioid receptor agonists (e.g., heroin). This study compared the ventilatory depressant effects of the opioid receptor agonists heroin, fentanyl, and carfentanil, and reversal of those effects by opioid receptor antagonists. This study used whole-body plethysmography in rats to determine the ventilatory depressant effects of heroin (178-1780 μg/kg), fentanyl (5.6-56 μg/kg), and carfentanil (0.56-5.6 μg/kg) when administered alone and in mixtures, to compare the profile of effects across drugs and determine whether there are significant interactions between the drugs when co-administered. The potencies of the opioid receptor antagonists naloxone and diprenorphine to reverse opioid-induced ventilatory depression were compared across opioid agonists. All three agonists reduced minute volume with carfentanil being ∼50- and 100-fold more potent than fentanyl and heroin, respectively. The profile of effects on ventilation did not differ across agonists and no significant drug-drug interactions were detected. Naloxone and diprenorphine dose-dependently reversed the ventilatory depressant effects of each opioid agonist. Both antagonists were less potent at reversing the effects of carfentanil compared with reversing a functionally equivalent dose of heroin. These findings suggest that fentanyl might not produce unique effects on breathing that increase risk of overdose. That naloxone and diprenorphine were less potent to reverse the effects of carfentanil compared with an equivalent dose of heroin is consistent with existing literature and emphasizes the need for continued evaluation of potential differences in pharmacological properties across opioid receptor agonists.

2025-04-24·JOURNAL OF MEDICINAL CHEMISTRY

Fentanyl–Antibody Interaction as a Novel Strategy against Opiates and Opioids Abuse

Review

作者: Ribaudo, Giovanni ; Gianoncelli, Alessandra ; Taccani, Andrea Achille

While naloxone remains the antidote for opioid overdoses, more efficient tools are required to effectively combat this growing crisis. Vaccines and antibodies targeting substances of abuse appear to be a novel and promising approach to tackling the fentanyl and opioid epidemic. After an initial in-depth rundown on the pharmacodynamics of the substances involved from a structural and mechanistic standpoint, and a brief overview of pharmacological approaches used in clinical settings for managing overdoses and opioid addiction, this Perspective will be mainly focused on these innovative strategies, based on the development of antibodies binding and sequestering substances of abuse and on their generation in vivo through vaccines. The most promising approaches will be examined, from production techniques to their potential clinical applications, analyzing the structures and mechanisms of antibody-substance interactions and comparing these with receptor binding processes.

2025-03-03·CHEMBIOCHEM

Unsymmetric Triazine‐Based Triglucoside Detergents for Membrane Protein Stability

Article

作者: Ehsan, Muhammad ; Ghani, Lubna ; Lan, Baoliang ; Chae, Pil Seok ; Liu, Xiangyu ; Katsube, Satoshi ; Poulsen, Ida H. ; Arslan, Muhammad ; Zhang, Xiang ; Loland, Claus J. ; Byrne, Bernadette ; Guan, Lan

Abstract:

Membrane proteins play a crucial role in a variety of biological processes and are key targets for pharmaceutical development. Structural studies of membrane proteins provide molecular insights into the mechanisms of these processes and are essential for effective drug discovery. Historically, these studies have relied on solubilization of the target protein using detergents, but conventional detergents often fail to maintain the stability of challenging membrane proteins. To address this issue, there is a need to develop novel detergents with enhanced protein stabilization properties. In this study, we synthesized unsymmetric variants of recently reported tris(hydroxymethyl)aminomethane(TRIS)‐linker‐bearing triazine‐based triglucosides (TTGs) by incorporating two different alkyl chains (long and short) into the detergent structure. When tested with model membrane proteins, including a G protein‐coupled receptor, TTG‐8,12 demonstrated superior efficacy in stabilizing membrane proteins compared to the original TTGs and the gold standard detergents DDM/LMNG. These results suggest that detergent unsymmetry is an important concept for improving detergent performance and unsymmetric detergents such as TTG‐8,12 hold significant potential for advancing membrane protein structural studies.

100 项与 Diprenorphine 相关的药物交易

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