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The case for the de...
The case for the development of novel analgesic agents targeting both fatty acid amide hydrolase and either cyclooxygenase or TRPV1
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- Fowler, Christopher J (författare)
- Umeå universitet,Farmakologi
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- Naidu, P S (författare)
- Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA, USA
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- Lichtman, A (författare)
- Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA, USA
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- Onnis, V (författare)
- Department of Toxicology, Unit of Medicinal Chemistry, University of Cagliari, Cagliari, Italy
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(creator_code:org_t)
- John Wiley & Sons, 2009
- 2009
- Engelska.
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Ingår i: British Journal of Pharmacology. - : John Wiley & Sons. - 0007-1188 .- 1476-5381. ; 156:3, s. 412-419
- Relaterad länk:
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https://europepmc.or...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- Although the dominant approach to drug development is the design of compounds selective for a given target, compounds targeting more than one biological process may have superior efficacy, or alternatively a better safety profile than standard selective compounds. Here, this possibility has been explored with respect to the endocannabinoid system and pain. Compounds inhibiting the enzyme fatty acid amide hydrolase (FAAH), by increasing local endocannabinoid tone, produce potentially useful effects in models of inflammatory and possibly neuropathic pain. Local increases in levels of the endocannabinoid anandamide potentiate the actions of cyclooxygenase inhibitors, raising the possibility that compounds inhibiting both FAAH and cyclooxygenase can be as effective as non-steroidal anti-inflammatory drugs but with a reduced cyclooxygenase inhibitory 'load'. An ibuprofen analogue active in models of visceral pain and with FAAH and cyclooxygenase inhibitory properties has been identified. Another approach, built in to the experimental analgesic compound N-arachidonoylserotonin, is the combination of FAAH inhibitory and transient receptor potential vanilloid type 1 antagonist properties. Although finding the right balance of actions upon the two targets is a key to success, it is hoped that dual-action compounds of the types illustrated in this review will prove to be useful analgesic drugs.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- endocannabinoid
- anandamide
- fatty acid amide hydrolase
- cyclooxygenase
- non-steroidal anti-inflammatory drugs
- transient receptor potential vanilloid type 1
- inflammatory pain
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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