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. 1991 Jan;102(1):179–185. doi: 10.1111/j.1476-5381.1991.tb12150.x

Effects of histamine H1-, H2- and H3-receptor selective drugs on the mechanical activity of guinea-pig small and large intestine.

R Leurs 1, M M Brozius 1, M J Smit 1, A Bast 1, H Timmerman 1
PMCID: PMC1917885  PMID: 1646056

Abstract

1. In this study we have evaluated the possible contribution of acetylcholine release in histamine-induced contractions of guinea-pig large and small intestinal smooth muscle. Moreover, the presence of the histamine receptor types involved in smooth muscle relaxations and inhibition of electrically-induced twitches was studied by use of several selective agents. 2. Histamine-induced contractions appeared to be a pure H1-receptor-mediated effect. Responses were not attenuated by the presence of 0.1 microM atropine and were competitively and stereoselectively inhibited by the two enantiomers of chlorpheniramine with pA2 values of 6.73 +/- 0.08, 7.30 +/- 0.06, 6.93 +/- 0.03 and 7.19 +/- 0.04 for the L-isomer and 8.63 +/- 0.09, 8.85 +/- 0.09, 9.01 +/- 0.16 and 0.11 for the D-isomer in the duodenum, jejunum, ileum and colon, respectively. 3. There appeared to be a marked regional difference in sensitivity to histamine. In ileal and jejunal preparations pD2 values of 6.24 +/- 0.06 (n = 22) and 6.37 +/- 0.07 (n = 22) were found, whereas the pD2 values in the duodenum and colon were 5.55 +/- 0.05 (n = 36) and 5.68 +/- 0.06 (n = 31) respectively. 4. This regional difference in sensitivity to histamine was not due to variations in receptor affinity since pA2 values for the two enantiomers of chlorpheniramine did not differ markedly among the four tested preparations. Since a similar variation in sensitivity was found for methacholine, it is likely that the signal transfer mechanism in guinea-pig ileum and jejunum is more efficient than in the duodenum and colon.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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