Literature DB >> 7340463

Reduction of aspirin-induced ulcers by a new imidazoline anti-inflammatory agent.

M P Holsapple, A Chun, R W Lagally, D E Nichols, G K Yim.   

Abstract

We have previously described the anti-inflammatory and low ulcerogenic actions of the formamidine pesticide, chlordimeform (CDM). In this study, the related basic compound, CDMI [2-(2-methyl-4-chlorophenylamino)-2-imidazoline], also demonstrated potent anti-edema (vs. carrageenin) and low ulcerogenic activity. A nonulcerogenic i.p. dose of CDMI reduced aspirin (ASA)-induced ulcers [lesion index (L.I.): 25.8 for ASA alond vs. 5.3 for ASA + i.p. CDMI]; prevented stress-induced ulcers in mice; and decreased acid secretion (by 90% in the Shay rat preparation). A mildly ulcerogenic oral dose (0.6 mmol/kg) of CDMI prevented stress ulcers, but did not reduce ASA ulcers. A nonulcerogenic oral dose (0.15 mmol/kg) of CDMI did reduce ASA ulcers (L.I.: 24.5 for ASA alone vs. 14.7 for ASA + oral CDMI). Thus, CDMI is a unique anti-inflammatory agent with additional anti-secretory and ulcer-reducing actions.

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Year:  1981        PMID: 7340463     DOI: 10.1007/bf01978795

Source DB:  PubMed          Journal:  Agents Actions        ISSN: 0065-4299


  14 in total

1.  Carrageenin-induced edema in hind paw of the rat as an assay for antiiflammatory drugs.

Authors:  C A WINTER; E A RISLEY; G W NUSS
Journal:  Proc Soc Exp Biol Med       Date:  1962-12

Review 2.  The role of acid in the pathogenesis of aspirin-induced gastrointestinal erosions and hemorrhage.

Authors:  A R Cooke
Journal:  Am J Dig Dis       Date:  1973-03

3.  Investigation of the carrageenin-induced rat paw edema assay and correlation between anti-inflammatory activity and gastric hemorrhage production in the rat.

Authors:  D T Walz; M J Di Martino; C L Griffin; A Misher
Journal:  Arch Int Pharmacodyn Ther       Date:  1970-06

4.  Effect of prostaglandin E1 on gastric secretion and ulcer formation in the rat.

Authors:  A Robert; J E Nezamis; J P Phillips
Journal:  Gastroenterology       Date:  1968-10       Impact factor: 22.682

5.  Prostaglandin synthesis inhibited by formamidine pesticides.

Authors:  G K Yim; M P Holsapple; W R Pfister; R M Hollingworth
Journal:  Life Sci       Date:  1978-12-18       Impact factor: 5.037

6.  Decreased gastrointestinal ulcerogenicity of chlordimeform, a basic anti-inflammatory agent.

Authors:  M P Holsapple; G K Yim
Journal:  Toxicol Appl Pharmacol       Date:  1981-06-15       Impact factor: 4.219

7.  Reversible depression of electrically-induced contractions of guinea pig longitudinal muscle by a reversible inhibitor of prostaglandin synthetase.

Authors:  M P Holsapple; D E Blake; G K Yim
Journal:  Prostaglandins Med       Date:  1979-10

8.  Dissociation constants of clonidine and structurally related imidazolidines.

Authors:  P B Timmermans; P A van Zwieten
Journal:  Arzneimittelforschung       Date:  1978

9.  The effects of metiamide on gastric secretion and stress ulceration in rats.

Authors:  S Dai; C W Ogle; C H Lo
Journal:  Eur J Pharmacol       Date:  1975 Sep-Oct       Impact factor: 4.432

Review 10.  Chemistry, biological activity, and uses of formamidine pesticides.

Authors:  R M Hollingworth
Journal:  Environ Health Perspect       Date:  1976-04       Impact factor: 9.031

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