Diclofenac
From Proteopedia
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Diclofenac has a relatively high lipid solubility, making it one of the few NSAIDs that are able to enter the brain by crossing the blood-brain barrier. In the brain, too, it is thought to exert its effect through inhibition of COX-2.<ref name="a44">PMID:25078485</ref> In addition, it may have effects inside the spinal cord.<ref name="a45">PMID:27014880</ref>. | Diclofenac has a relatively high lipid solubility, making it one of the few NSAIDs that are able to enter the brain by crossing the blood-brain barrier. In the brain, too, it is thought to exert its effect through inhibition of COX-2.<ref name="a44">PMID:25078485</ref> In addition, it may have effects inside the spinal cord.<ref name="a45">PMID:27014880</ref>. | ||
| - | It also may inhibit [[phospholipase A2]] as part of its mechanism of action. These additional actions may explain its high potency – it is the most potent NSAID on a broad basis.<ref name="a46">PMID:3085490</ref> <scene name='97/974935/Cv/2'>Crystal structure of the complex formed between phospholipase A2 and diclofenac</scene> ([[2b17]]). | + | It also may inhibit [[phospholipase A2]] as part of its mechanism of action. These additional actions may explain its high potency – it is the most potent NSAID on a broad basis.<ref name="a46">PMID:3085490</ref> <scene name='97/974935/Cv/2'>Crystal structure of the complex formed between phospholipase A2 and diclofenac</scene> ([[2b17]]). <scene name='97/974935/Binding_site/1'>Diclofenac binding site</scene>. |
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 13:26, 3 July 2023
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References
- ↑ Mitchell JA, Akarasereenont P, Thiemermann C, Flower RJ, Vane JR. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7. PMID:8265610 doi:10.1073/pnas.90.24.11693
- ↑ Dastidar SG, Ganguly K, Chaudhuri K, Chakrabarty AN. The anti-bacterial action of diclofenac shown by inhibition of DNA synthesis. Int J Antimicrob Agents. 2000 Apr;14(3):249-51. PMID:10773497 doi:10.1016/s0924-8579(99)00159-4
- ↑ Sandri A. [Diclofenac: update on tolerableness and spinal anti-inflammatory action]. Minerva Med. 2014 Aug;105(4):313-8 PMID:25078485
- ↑ Sandri A. Spinal antinflammatory action of Diclofenac. Minerva Med. 2016 Jun;107(3):167-72. Epub 2016 Mar 25 PMID:27014880
- ↑ Scholer DW, Ku EC, Boettcher I, Schweizer A. Pharmacology of diclofenac sodium. Am J Med. 1986 Apr 28;80(4B):34-8. PMID:3085490 doi:10.1016/0002-9343(86)90077-x
