| 体内研究: |
In a rat model of postoperative pain, Thioflosulide (L-745337) (40-80 μg, intrathecal) coadministered with intrathecal morphine (0.5 nmol) increases the withdrawal thresholds in a dose-dependent manner. Adding 80 μg Thioflosulide (L-745337) to 1 nmol morphine produces an antiallodynic effect greater than that of morphine at twice the dose. Thioflosulide (L-745337) (0-30 mg/kg, s.c.) combined with intrathecal morphine results in the same antiallodynic response as morphine alone. Thioflosulide (L-745337) shows anti-inflammatory activity, with the effective-dose of 0.4 mg/kg, and the maximal anti-inflammation dose of 5 mg/kg in arthritic rats. |
| 参考文献: |
1. Kroin JS, et al. Cyclooxygenase-2 inhibition potentiates morphine antinociception at the spinal level in a postoperative pain model. Reg Anesth Pain Med. 2002 Sep-Oct;27(5):451-5. 2. Turull N, et al. Effect of the COX-2 selective inhibitor l-745,337 on inflammation and organ prostaglandin E2 (PGE2) levels in adjuvant arthritic rats. Inflammation. 2000 Dec;24(6):533-45. 3. Li CS, et al. Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. J Med Chem. 1995 Dec 8;38(25):4897-905. |
| 溶解性: |
DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.707 ml |
13.535 ml |
27.07 ml |
| 5 mM |
0.541 ml |
2.707 ml |
5.414 ml |
| 10 mM |
0.271 ml |
1.354 ml |
2.707 ml |
| 50 mM |
0.054 ml |
0.271 ml |
0.541 ml |
|
| 注意: |
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