Comparison of Five Benzodiazepine-Receptor Agonists on Buprenorphine-Induced μ-Opioid Receptor Regulation
-
- Poisnel Géraldine
- CEA-DSV-I<sup>2</sup>BM-CI-NAPS-LDMTEP UMR, Université de Caen, France
-
- Dhilly Martine
- CEA-DSV-I<sup>2</sup>BM-CI-NAPS-LDMTEP UMR, Université de Caen, France
-
- Boisselier Reynald Le
- Drug Dependence Evaluation Center, University Hospital Center of Caen, France
-
- Barre Louisa
- CEA-DSV-I<sup>2</sup>BM-CI-NAPS-LDMTEP UMR, Université de Caen, France
-
- Debruyne Danièle
- CEA-DSV-I<sup>2</sup>BM-CI-NAPS-LDMTEP UMR, Université de Caen, France
書誌事項
- タイトル別名
-
- Comparison of five benzodiazepine receptor agonists on buprenorphine induced m opioid receptor regulation
この論文をさがす
抄録
In this study, we compared the effects of five short-, medium-, or long-acting benzodiazepine-receptor agonists (BZDs) [alprazolam (APZ), clonazepam (CLZ), flunitrazepam (FLZ), loprazolam (LPZ), zolpidem (ZLP)], at two distinct doses, 0.2 and 2 mg/kg, on the cell surface regulation of μ-opioid receptor induced by 0.15 mg/kg buprenorphine (BPN) in specific regions of the rat brain. Using 0.312 – 5 nM [3H]-DAMGO concentrations and Scatchard plot analysis, Bmax (maximal receptor density) and Kd (dissociation constant) were determined at different brain regions of interest (amygdala, cortex, hippocampus, hypothalamus, thalamus). Acute BPN induced an expected down-regulation and addition of each of the BZDs to BPN induced less down-regulation than did BPN alone, sometimes while altering affinity. Some significant differences in the intensity of these effects were observed between BZDs. FLZ that is widely abused and enlarges BPN toxicity appeared the most potent to increase μ-cell surface receptor density at the lowest dose of 0.2 mg/kg. Besides, LPZ for which the effect on μ-opioid–receptor regulation appeared lower is considered to have a low risk of dependence in the epidemiological data banks. CLZ and ZLP (2 mg/kg) induced the strongest modification on μ-opioid–receptor density, but a substantial decrease in affinity could minimize the functional consequences. The reported changes were maximal in the amygdala, hippocampus, and thalamus. Among people using BPN and BZDs, the effects described here are likely to influence addictive behaviors and induce toxic effects that could be quantitatively different due to the quality of the BZD.<br>
収録刊行物
-
- Journal of Pharmacological Sciences
-
Journal of Pharmacological Sciences 110 (1), 36-46, 2009
公益社団法人 日本薬理学会
- Tweet
詳細情報 詳細情報について
-
- CRID
- 1390001205179531648
-
- NII論文ID
- 10025736509
-
- NII書誌ID
- AA11806667
-
- ISSN
- 13478648
- 13478613
-
- NDL書誌ID
- 10225661
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可