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Ketorolac (RS37619) hemicalcium is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorola chemicalcium is also a DDX3 inhibitor that can be used for cancer research[1][4]. | [in vivo]
Ketorolac (RS37619) (0.4% ketorolac tromethamine ophthalmic solution) shows powerful ocular anti-inflammatory activities in rabbits[1].
Ketorolac (4 mg/kg/day, p.o.; 2 weeks) has no detrimental effect in the volume fraction of bone trabeculae formed inside the alveolar socket in rats[2].
Ketorolac (60 μg; intrathecal injection; once) attenuates the damage caused by spinal cord ischemia in rats[3].
Ketorolac salt (20 and 30 mg/kg; i.p.; two times in a week for 3 weeks) reduces oral carcinogenesis in mice[4]. | Animal Model: | New Zealand White rabbits (2.0–2.7 kg), LPS endotoxin-induced ocular inflammation[1] | | Dosage: | 50 μL ketorolac tromethamine ophthalmic solution 0.4% | | Administration: | In eyes, twice, 2 hours and 1 hour before LPS challenge | | Result: | Resulted in a nearly complete inhibition (98.7%) of LPS endotoxin-induced increases in FITC (fluorescein isothiocyanate)-dextran in the anterior chamber, and resulted in a nearly complete inhibition (97.5%) of LPS endotoxin-induced increases in aqueous PGE2 concentrations in the aqueous humor. |
| Animal Model: | Male Wistar rats (400–450 g), spinal cord ischemia model[3] | | Dosage: | 30 and 60 μg
| | Administration: | Intrathecal injection, 1 h before the ischemia induction for once | | Result: | Significantly reduced the motor disturbances and improved the survival rate at 60 μg. |
| Animal Model: | BALB/c mice, oral carcinogenesis model[4] | | Dosage: | 20 mg/kg and 30 mg/kg | | Administration: | IP injection, two times in a week for 3 weeks | | Result: | Decreased tumor burden, reduced expression of DDX3 and anti-apoptotic proteins (Bcl-2 and Mcl-1).
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| [References]
[1] Waterbury LD, et al. Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects of ketorolac tromethamine and bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40. DOI:10.1185/030079906X112471
[2] Fracon RN, et al. Treatment with paracetamol, ketorolac or etoricoxib did not hinder alveolar bone healing: a histometric study in rats. J Appl Oral Sci. 2010 Dec;18(6):630-4. DOI:10.1590/s1678-77572010000600016
[3] Hsieh YC, et al. Intrathecal ketorolac pretreatment reduced spinal cord ischemic injury in rats. Anesth Analg. 2005 Apr;100(4):1134-9. DOI:10.1213/01.ANE.0000146962.91038.15
[4] Samal SK, et al. Ketorolac salt is a newly discovered DDX3 inhibitor to treat oral cancer. Sci Rep. 2015 Apr 28;5:9982. DOI:10.1038/srep09982 |
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