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

Holsapple, Michael P.; Blake, Donald E.; Yiml, George K.W.

doi:10.1016/0161-4630(79)90083-1

Cited by 3 publications

(2 citation statements)

References 9 publications

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“…Moreover, at the high concentrations required (10 -4-10 -3 M), CDM also reduces ACh-induced contractions of the guinea pig ileum [2]; spontaneous contractions of the isolated rabbit heart [14]; and even K+-induced contractions of the frog rectus abdominus muscle [15]. Moreover, at the high concentrations required (10 -4-10 -3 M), CDM also reduces ACh-induced contractions of the guinea pig ileum [2]; spontaneous contractions of the isolated rabbit heart [14]; and even K+-induced contractions of the frog rectus abdominus muscle [15].…”

Section: Drug Effects On Acute Inflammatiormentioning

confidence: 89%

Pharmacological modulation of edema mediated by prostaglandin, serotonin and histamine

1980

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Previous studies demonstrated that the formamidine pesticide chlordimeform (CDM) reversibly inhibited prostaglandin biosynthesis and prevented the late (PG-mediated) phase of carrageenin-induced hind paw edema. This study emphasizes antagonism by CDM of the early (5HT and histamine-mediated) phase of carrageenin edema. CDM and cyproheptadine both antagonized paw edema induced by albumin (5HT and histamine-mediated) and by the direct injection of 5HT and histamine, whereas aspirin and the PG antagonist, SC-19220, were ineffective. As expected, cyproheptadine selectively reduced the early phase, whereas aspirin and SC-19220 selectively reduced the late phase of carrageenin-induced edema. These results are thus consistent with earlier studies demonstrating PG mediation of the late phase of carrageenin edema, and 5HT and histamine mediation of albumin edema and the early phase of carrageenin edema. In addition, they indicate that CDM possesses multiple acute anti-inflammatory actions not exhibited by aspirin, by SC-19220 or by cyproheptadine alone.

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Section: Drug Effects On Acute Inflammatiormentioning

confidence: 89%

Pharmacological modulation of edema mediated by prostaglandin, serotonin and histamine

1980

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“…Formamidines were proposed to be prostaglandin synthetase inhibitors based on studies in isolated guinea pig ileum, which show aspirin-like actions with depression of electrically induced responses, reversible by prostaglandin E1 but not by naloxone. , According to this, Yim et al evaluated the antipyretic and anti-inflammatory activities of amitraz given intraperitoneally to rats at 5 to 80 mg/kg doses compared with two known inhibitors of prostaglandin synthesis, aspirin (20 to 320 mg/kg) and indomethacin (0.25 to 2 mg/kg). The results show that amitraz behaves as an antipyretic and anti-inflammatory agent.…”

Section: Mechanisms Of Amitraz Toxicitymentioning

confidence: 99%

Molecular Mechanisms of Amitraz Mammalian Toxicity: A Comprehensive Review of Existing Data

Pino

Moyano-Cires

Anadón

et al. 2015

Chem. Res. Toxicol.

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Amitraz is a formamidine pesticide widely used as an insecticide and acaricide. Amitraz poisoning cases in humans and animals are still being described to date, which is a cause of concern for health authorities. Amitraz was reported not to pose unreasonable risks or adverse effects to humans or the environment unlike the other commercialized member of the formamidine family, chlordimeform, which was removed from the market because of carcinogenic effects in animal studies. Amitraz was classified as a nonquantifiable "Suggestive Evidence of Carcinogenicity" and not genotoxic, but recently, it has been reported that it could induce genotoxic effects. Moreover, ever since the previously published evaluations made by the Environmental Protection Agency (EPA) and the Joint Meeting of Pesticide Residues (JMPR) there have been new reported data on amitraz toxicity related to genotoxicity, oxidative stress, cell death, immunotoxicty, endocrine disruption, and developmental toxicity which indicate that the risk of this compound could be underestimated. Furthermore, there is missing information about the dose-response relationship for some mechanisms and toxic effects described for amitraz and its metabolites, the mechanism of action by which several toxic effects are produced, and amitraz pharmacokinetics on different species. According to this, the new information reported should be taken into account, and more studies should be performed to fill in the gaps of missing information for a complete hazard identification and therefore an exhaustive risk assessment of amitraz. This review is aimed at updating the current knowledge on molecular mechanisms of amitraz mammalian toxicity, pointing out the missing information, providing some possible explanation of the mechanism by which some toxic effects observed are produced, and suggesting future direction of its research. To our knowledge, this is the first review on the molecular mechanisms of amitraz toxicity.

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

et al. 1981

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

Cited by 3 publications

References 9 publications

Pharmacological modulation of edema mediated by prostaglandin, serotonin and histamine

Pharmacological modulation of edema mediated by prostaglandin, serotonin and histamine

Molecular Mechanisms of Amitraz Mammalian Toxicity: A Comprehensive Review of Existing Data

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

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