The Effects of Non‐steroidal Anti‐inflammatory Drugs on Cholinergic and Histamine‐induced Contractions of Guinea‐pig Isolated Ileum

Famaey, Jean Pierre; Fontaine, Jeanine; Reuse, Joannes

doi:10.1111/j.1476-5381.1977.tb07737.x

Cited by 30 publications

(8 citation statements)

References 25 publications

(42 reference statements)

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“…The aspirin-like drugs have non-specific inhibitory actions on smooth muscle responsiveness to spasmogens (Northover, 1967;Manku & Horrobin, 1976;Famaey, Fontaine & Reuse, 1977), and diphloretin phosphate, although a potent inhibitor of prostaglandin breakdown, has also been shown to inhibit These experiments provide evidence that sulphasalazine at micromolar concentrations inhibits prostaglandin inactivation in cell-free tissue homogenates prepared from a wide range of species and organs and that the drug has the same effect in the intact lung, both in vitro and in the anaesthetized rat. These in vitro properties are not shared by its principal colonic metabolites sulphapyridine and 5-aminosalicylic acid.…”

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confidence: 75%

Effects of Sulphasalazine and Its Metabolites on Prostaglandin Synthesis, Inactivation and Actions on Smooth Muscle

Hoult

Moore

1980

British J Pharmacology

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6 Prostaglandin biosynthesis from arachidonic acid was measured in microsomal preparations from four sources by bioassay and radiochemical methods. Indomethacin was a potent inhibitor (ID50 0.8 to 4.1 pM) but sulphasalazine and its methyl analogue were very weak inhibitors (ID50 1500 to > 5000 gM), 5-aminosalicylic acid was weaker still and sulphapyridine inactive. 7 Sulphasalazine at 50 gM did not affect the actions of prostaglandins on five smooth muscle preparations; at 500 gM there was a rapidly reversible and probably non-specific antagonism of responses to low doses of prostaglandins.8 The specificity and selectivity of the interaction of sulphasalazine and its metabolites with the formation, breakdown and actions of prostaglandins are discussed. IntroductdonWe have shown recently that sulphasalazine is a to inhibit prostaglandin breakdown were achieved in potent inhibitor of prostaglandin inactivation in cellcolon (but not in lung or kidney) after treating rats free homogenates but is only a feeble inhibitor of chronically with oral doses comparable to those used prostaglandin biosynthesis from arachidonic acid clinically in the treatment of ulcerative colitis (Moore,

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confidence: 75%

Effects of Sulphasalazine and Its Metabolites on Prostaglandin Synthesis, Inactivation and Actions on Smooth Muscle

Hoult

Moore

1980

British J Pharmacology

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“…Partial mediation by cholinergic nerves of the histamineinduced contraction has also been observed in some external muscles of the mammalian gut (Bertaccini, 1982). The release of prostaglandin-like substances by histamine and the modification of the histamine-induced contraction by cyclo-oxygenase inhibitors have already been observed in the guinea-pig tracheal (Grodzinska et al, 1975;Orehek et al, 1975) and ileal smooth muscle (Famaey et al, 1977). Also in the present preparations, we have shown that the arachidonic acid (0.2-3 gM)-induced contraction was fully prevented by indomethacin or aspirin at the concentration used here Kamikawa et al, 1985a).…”

Section: Discussionmentioning

confidence: 98%

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Fujinuma

Kamikawa

Shimo

1985

British J Pharmacology

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1 To characterize the histamine receptors in the muscularis mucosae, the isotonic responsiveness of the isolated muscularis mucosae of the guinea-pig oesophagus to histamine receptor agonists and antagonists was examined in vitro. 2 Histamine (0.1-100 M) produced a concentration-dependent contraction of the muscularis mucosae (EC50 = 1.6 ± 0.2 LM). The contractions were rapid in onset, sustained, reversible by washing and the preparation did not show tachyphylaxis. 3 2-Methylhistamine (2-MH), 2-pyridylethylamine (PEA) and 4-methylhistamine (4-MH) produced similar sustained contractions of the muscularis mucosae. The order of sensitivity was histamine > 2-MH > PEA> 4-MH. Impromidine (10-300 LM) and dimaprit (10-300 gM) caused no response in this tissue. 4 The contractile responses to histamine, 2-MH, and PEA were competitively antagonized by diphenhydramine, and the pA2 values were almost the same (approximately 8.1). Cimetidine (I 00 gM)could not modify the contractile response to these agonists. 5 The contractile response to histamine was slightly inhibited by tetrodotoxin (0.3 JM), atropine (1 LM), indomethacin (0.1-3 jAM) or aspirin (30-300 jM), and the EC50 value was increased about [2][3][4][5][6] times by these drugs. 6 When the preparation was incubated in Tyrode solution containing various calcium concentrations (0, 0.45, 0.9 and 1.8 mM), the concentration-response curve to histamine was shifted to the right and downward; the effect was inversely dependent on the calcium concentration, and in a calcium-free medium the response to histamine was abolished. Verapamil (1-10 M) partially inhibited the contractile response to histamine. 7 The present results indicate that the contraction of the guinea-pig oesophageal muscularis mucosae to histamine is mediated mainly by a direct action on the smooth muscle and partly by indirect actions via the stimulation of either endogenous prostaglandin biosynthesis or intramural cholinergic nerves. The histamine receptors responsible for contractions of this tissue are probably mainly of the H,-subtype with H2-receptors having a negligible role.

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“…These results suggested that the inhibitory action on the cholinergic nervous system was involved in these ameliorative effects [4], [5]. Subsequently, when the actions of ZSR and compounds 1 and 2 on BaCl 2 -induced hyperperistalsis of the small intestine were evaluated in vivo to investigate whether these substances directly suppress peristalsis of the small intestine.…”

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confidence: 98%

Component ofZingiber officinalethat Improves the Enhancement of Small Intestinal Transport

Hashimoto

Satoh²,

Murata³

et al. 2002

Planta med

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The Effects of Non‐steroidal Anti‐inflammatory Drugs on Cholinergic and Histamine‐induced Contractions of Guinea‐pig Isolated Ileum

Cited by 30 publications

References 25 publications

Effects of Sulphasalazine and Its Metabolites on Prostaglandin Synthesis, Inactivation and Actions on Smooth Muscle

Effects of Sulphasalazine and Its Metabolites on Prostaglandin Synthesis, Inactivation and Actions on Smooth Muscle

Pharmacological characterization of the histamine receptor in the isolated muscularis mucosae of the guinea‐pig oesophagus

Component ofZingiber officinalethat Improves the Enhancement of Small Intestinal Transport

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