| 产品描述: | Org 27569是cannabinoid CB1 receptor变构调节剂,通过增强激动剂亲和力而诱导CB1受体状态改变,且降低逆向激动剂的亲和力。A CB1 receptor allosteric modulator. |
| 体内研究: |
ORG 27569 (3.2 和 5.6 mg/kg,腹腔注射) 显著减弱可卡因相关线索诱导的恢复、可卡因启动诱导的恢复、甲基苯丙胺相关线索诱导的恢复和甲基苯丙胺启动诱导的大鼠恢复。Org27569 (30 mg/kg,ip) 产生独立于 CB1 的食欲减退作用,并且不影响 anandamide (AEA) 的辨别刺激作用。与载体相比,Org27569 (脑室内注射 100 μg) 不影响全身给药 CP55,940 的药理作用。 |
| 参考文献: |
1. Jing L, et al. Effects of the cannabinoid CB? receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in rats. Drug Alcohol Depend. 2014 Oct 1;143:251-6. 2. Fay JF, et al. A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569. J Biol Chem. 2012 Jul 30. 3. Gamage TF, et al. In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569. Behav Pharmacol. 2014 Apr;25(2):182-5. 4. Price MR, et al. Allosteric modulation of the cannabinoid CB1 receptor. Mol Pharmacol. 2005 Nov;68(5):1484-95. 5. Baillie GL, et al. CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Mol Pharmacol. 2013 Feb;83(2):322-38. |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.439 ml |
12.197 ml |
24.393 ml |
| 5 mM |
0.488 ml |
2.439 ml |
4.879 ml |
| 10 mM |
0.244 ml |
1.22 ml |
2.439 ml |
| 50 mM |
0.049 ml |
0.244 ml |
0.488 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |