| 产品描述: | JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. |
| 靶点: |
Opioid Receptor;JAK |
| 体内研究: |
JDTic (2.5-16 mg/kg, s.c.) dose-dependently blocks the antinociceptive response of nicotine in the tail-flick test but has no effect in the hot-plate assay or body temperature assessments at any dose tested in the mice injected with nicotine. JDTic (3 mg/kg, i.p.) is capable of reversing anxiety-like behavior in the rat model of hangover anxiety. JDTic (10 mg/kg, i.p.) decreases alcohol self-administration, suppresses cue-induced reinstatement of alcohol seeking, and specifically blocks the effects of a KOR agonist at the 2 h pretreatment time point. JDTic (30 mg/kg, i.g.) significantly blockes U50,488-induced diuresis immediately in rats |
| 参考文献: |
1. Jackson KJ, et al. Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse. Psychopharmacology (Berl). 2010 Jun;210(2):285-94. 2. Schank JR, et al. The kappa opioid receptor antagonist JDTic attenuates alcohol seeking and withdrawal anxiety. Addict Biol. 2012 May;17(3):634-47. doi: 10.1111/j.1369-1600.2012.00455.x. 3. Beardsley PM, et al. Effectiveness of analogs of the kappa opioid receptor antagonist (3R)-7-hydroxy-N-((1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic) to reduce U50,488-induced diuresis and stress-induced cocaine reinstatement in rats. Psychopharmacology (Berl). 2010 Jun;210(2):189-98. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.857 ml |
9.284 ml |
18.568 ml |
| 5 mM |
0.371 ml |
1.857 ml |
3.714 ml |
| 10 mM |
0.186 ml |
0.928 ml |
1.857 ml |
| 50 mM |
0.037 ml |
0.186 ml |
0.371 ml |
|
| 注意: |
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