8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid,2-[3-[2-(furanylmethyl)thio]-1-oxopropyl]hydrazide (SC-51322): A potent PGE2 antagonist and analgesic
✍ Scribed by E.Ann Hallinan; Awilda Stapelfeld; Michael A. Savage; Melvin Reichman
- Book ID
- 103982797
- Publisher
- Elsevier Science
- Year
- 1994
- Tongue
- English
- Weight
- 306 KB
- Volume
- 4
- Category
- Article
- ISSN
- 0960-894X
No coin nor oath required. For personal study only.
✦ Synopsis
Prostaglandin E2 (PGE2). a product of arachidonic acid metabolism, is one mediator of the nociceptive process. PGE2 has been shown to elicit pain and hyperalgesia in humans and to potentiate the action of bradykinin in the transmission of pain.1 Ferreira and Vane have postulated that the alleviation of pain with NSAIDs (non-steroidal antiinflammatory drugs) occur6 by the inhibition of cyclooxygenase's action on arachidonic acid.2 In particular, the inhibition of cyclooxygenase prevents the formation of PGE2. Sanner and others have observed that SC-19229 (1) is a fimctional antagonist of PGEz-elicited contractions in select tissues in vitro;3 while Hammond et al. have shown that antagonists of PGEz such as SC-19220 and pinadoline (2) are analgesic.4 The rationale of our analgesia program is