Abstract |
CGP 28237 (5-methylsulphonylamino-6-phenoxy-1-indanone) belongs to a series of structurally novel indanones. The compound is a weak acid (pK = 6.98), but it does not contain a carboxylic group. CGP 28237 exhibits potent anti-inflammatory activity in developing and established adjuvant arthritis in rats (ED40 approximately 0.5 mg/kg p.o.) and good activity in carrageenin oedema (ED40 approximately 3 mg/kg p.o.). It inhibits yeast-induced fever in rats with ED50 values of 1, 2 and 10 mg/kg p.o. at 1, 3 and 5 hours after drug administration. The antinociceptive activity in mice ( phenyl-p-benzoquinone writhing) and rats ( acetic-acid writhing) is weak. CGP 28237 has been shown to be non-ulcerogenic in rats under acute and chronic test conditions: it does not cause mucosal lesions in the stomach at 2 X 400 mg/kg p.o., it does not enhance gastro-intestinal blood loss during 10 days' oral treatment with 400 mg/kg p.o., and it did not induce gastro-intestinal lesions in a 4-week toxicity study up to 1000 mg/kg p.o. Although CGP 28237 is not a cyclooxygenase inhibitor in bovine seminal vesicle microsomes, it inhibits prostaglandin synthesis in zymosan-stimulated murine macrophages (IC50 approximately 3 X 10(-6) mol/l) and protects rabbits against arachidonic acid-induced lung embolism with 10 mg/kg p.o. CGP 28237 may represent a novel anti-inflammatory drug with excellent gastro-intestinal tolerability.
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Authors | I Böttcher, A Schweizer, M Glatt, H Werner |
Journal | Drugs under experimental and clinical research
(Drugs Exp Clin Res)
Vol. 13
Issue 5
Pg. 237-45
( 1987)
ISSN: 0378-6501 [Print] Switzerland |
PMID | 3500026
(Publication Type: Journal Article)
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Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Arachidonic Acids
- Indans
- Indenes
- 5-methylsulfonylamino-6-phenoxy-1-indanone
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Topics |
- Animals
- Anti-Inflammatory Agents, Non-Steroidal
(pharmacology, therapeutic use)
- Arachidonic Acids
(metabolism)
- Arthritis, Experimental
(drug therapy)
- Drug Tolerance
- Edema
(drug therapy)
- Female
- Fever
(drug therapy)
- Indans
(pharmacology, therapeutic use)
- Indenes
(pharmacology)
- Male
- Mice
- Mice, Inbred Strains
- Occult Blood
- Pulmonary Embolism
(drug therapy)
- Rabbits
- Rats
- Rats, Inbred Lew
- Rats, Inbred Strains
- Stomach Ulcer
(chemically induced)
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