Brain PET imaging using 11C-flumazenil and 11C-buprenorphine does not support the hypothesis of a mutual interaction between buprenorphine and benzodiazepines at the neuroreceptor level DOI
Sylvain Auvity, Dominique Vodovar, Sébastien Goutal

et al.

Journal of Cerebral Blood Flow & Metabolism, Journal Year: 2023, Volume and Issue: 44(3), P. 449 - 458

Published: Dec. 14, 2023

Among opioids, buprenorphine presents a favorable safety profile with limited risk of respiratory depression. However, fatalities have been reported when is combined to benzodiazepine. Potentiation interaction opioid receptors (ORs) benzodiazepines, and/or vice versa, hypothesized explain this drug-drug (DDI). The mutual DDI between and benzodiazepines was investigated at the neuroreceptor level in nonhuman primates (n = 4 individuals) using brain PET imaging kinetic modelling. binding potential (BP ND ) benzodiazepine receptor (BzR) assessed 11 C-flumazenil before after administration (0.2 mg, i.v.). Moreover, kinetics were same individuals C-buprenorphine diazepam (10 Outcome parameters compared two-way ANOVA. Buprenorphine did not impact plasma nor C-flumazenil. BP unchanged following exposure, any region (p > 0.05). Similarly, or C-buprenorphine. volume distribution ( V T To conclude, our findings do support neuropharmacokinetic neuroreceptor-related mechanism buprenorphine/benzodiazepine interaction.

Language: Английский

Endogenous opiates and behavior: 2023 DOI
Richard J. Bodnar

Peptides, Journal Year: 2024, Volume and Issue: 179, P. 171268 - 171268

Published: June 28, 2024

Language: Английский

Citations

4
Selective Mu-Opioid Receptor Imaging Using 18F-Labeled Carfentanils DOI
So Jeong Lee,

Torben D. Pearson,

Maëva Dhaynaut

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 7, 2025

Carfentanil, a highly potent synthetic opioid, paradoxically serves as crucial positron emission tomography (PET) imaging tool in neurobiological studies of the mu-opioid receptor (MOR) system when labeled with carbon-11 ([11C]CFN). However, its clinical research use is hindered by extreme potency and limited availability short-lived (t1/2 = 20.4 min). We present fluorine-18-labeled fluorocarfentanils ([18F]FCFNs), which can be produced at higher molar activity, allowing for lower mass doses benefiting from longer half-life fluorine-18 109.8 min), facilitating broader accessibility. Using copper-mediated radiofluorination, we synthesized small [18F]FCFN library conducted preclinical evaluations. Two candidates, o-18F-1 p-18F-2, showed optimal brain uptake, favorable pharmacokinetics, high MOR-specific binding. Selectivity was confirmed through vitro binding assays vivo PET scans. These [18F]FCFNs are promising accessible human MOR imaging.

Language: Английский

Citations

0
Decreased opioid receptor availability and impaired neurometabolic coupling as signatures of morphine tolerance in male rats: A positron emission tomography study DOI Open Access

Amélie Soyer,

Sarah Leterrier, Sébastien Goutal

et al.

Biomedicine & Pharmacotherapy, Journal Year: 2025, Volume and Issue: 183, P. 117848 - 117848

Published: Jan. 16, 2025

Language: Английский

Citations

0
Brain PET imaging using 11C-flumazenil and 11C-buprenorphine does not support the hypothesis of a mutual interaction between buprenorphine and benzodiazepines at the neuroreceptor level DOI
Sylvain Auvity, Dominique Vodovar, Sébastien Goutal

et al.

Journal of Cerebral Blood Flow & Metabolism, Journal Year: 2023, Volume and Issue: 44(3), P. 449 - 458

Published: Dec. 14, 2023

Among opioids, buprenorphine presents a favorable safety profile with limited risk of respiratory depression. However, fatalities have been reported when is combined to benzodiazepine. Potentiation interaction opioid receptors (ORs) benzodiazepines, and/or vice versa, hypothesized explain this drug-drug (DDI). The mutual DDI between and benzodiazepines was investigated at the neuroreceptor level in nonhuman primates (n = 4 individuals) using brain PET imaging kinetic modelling. binding potential (BP ND ) benzodiazepine receptor (BzR) assessed 11 C-flumazenil before after administration (0.2 mg, i.v.). Moreover, kinetics were same individuals C-buprenorphine diazepam (10 Outcome parameters compared two-way ANOVA. Buprenorphine did not impact plasma nor C-flumazenil. BP unchanged following exposure, any region (p > 0.05). Similarly, or C-buprenorphine. volume distribution ( V T To conclude, our findings do support neuropharmacokinetic neuroreceptor-related mechanism buprenorphine/benzodiazepine interaction.

Language: Английский

Citations

1