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Characterization of the gastroprotective effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine hydrochloride, a non-H1/non-H2 histamine antagonist.
Digestion. 1990; 47(3):143-8.D

Abstract

N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE) is an antihistamine with a unique profile of activity in the stomach. It is antisecretory and blocks the formation of experimental cold/stress- and ethanol-induced gastric lesions, as well as cysteamine-induced duodenal ulcers in a fashion more potent than observed with histamine H2 antagonists such as cimetidine. We now demonstrate that the antiulcer effects of DPPE are associated with a dramatic (10-fold) rise in the stable prostacyclin hydration product 6-keto-prostaglandin F1 alpha in gastric secretion collected from conscious rats. Cyclooxygenase inhibitors such as acetylsalicylic acid, indomethacin and sodium meclofenamate abolish high-dose DPPE-induced gastroprotection, whereas sodium salicylate, a lipoxygenase inhibitor, does not. These data suggest that DPPE-induced gastroprotection is mediated, at least in part, through an increase in endogenous prostacyclin (prostaglandin I2) synthesis in the gastric mucosa. These data are not consistent with an effect of DPPE primarily at the H2 receptor, but are consistent with the recent suggestion that DPPE antagonizes histamine at HIC, an intracellular histamine site.

Authors+Show Affiliations

Glavin GB
Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Manitoba, Winnipeg, Canada.
Gerrard JM
No affiliation info available

MeSH

6-Ketoprostaglandin F1 alphaAnimalsAnti-Ulcer AgentsEpoprostenolGastric JuiceGastric MucosaHistamine AntagonistsMalePhenyl EthersRatsRats, Inbred StrainsStomach UlcerStress, Physiological

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

2083800

Citation

Glavin, G B., and J M. Gerrard. "Characterization of the Gastroprotective Effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine Hydrochloride, a non-H1/non-H2 Histamine Antagonist." Digestion, vol. 47, no. 3, 1990, pp. 143-8.
Glavin GB, Gerrard JM. Characterization of the gastroprotective effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine hydrochloride, a non-H1/non-H2 histamine antagonist. Digestion. 1990;47(3):143-8.
Glavin, G. B., & Gerrard, J. M. (1990). Characterization of the gastroprotective effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine hydrochloride, a non-H1/non-H2 histamine antagonist. Digestion, 47(3), 143-8.
Glavin GB, Gerrard JM. Characterization of the Gastroprotective Effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine Hydrochloride, a non-H1/non-H2 Histamine Antagonist. Digestion. 1990;47(3):143-8. PubMed PMID: 2083800.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of the gastroprotective effects of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]-ethanamine hydrochloride, a non-H1/non-H2 histamine antagonist. AU - Glavin,G B, AU - Gerrard,J M, PY - 1990/1/1/pubmed PY - 1990/1/1/medline PY - 1990/1/1/entrez SP - 143 EP - 8 JF - Digestion JO - Digestion VL - 47 IS - 3 N2 - N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE) is an antihistamine with a unique profile of activity in the stomach. It is antisecretory and blocks the formation of experimental cold/stress- and ethanol-induced gastric lesions, as well as cysteamine-induced duodenal ulcers in a fashion more potent than observed with histamine H2 antagonists such as cimetidine. We now demonstrate that the antiulcer effects of DPPE are associated with a dramatic (10-fold) rise in the stable prostacyclin hydration product 6-keto-prostaglandin F1 alpha in gastric secretion collected from conscious rats. Cyclooxygenase inhibitors such as acetylsalicylic acid, indomethacin and sodium meclofenamate abolish high-dose DPPE-induced gastroprotection, whereas sodium salicylate, a lipoxygenase inhibitor, does not. These data suggest that DPPE-induced gastroprotection is mediated, at least in part, through an increase in endogenous prostacyclin (prostaglandin I2) synthesis in the gastric mucosa. These data are not consistent with an effect of DPPE primarily at the H2 receptor, but are consistent with the recent suggestion that DPPE antagonizes histamine at HIC, an intracellular histamine site. SN - 0012-2823 UR - https://www.unboundmedicine.com/medline/citation/2083800/Characterization_of_the_gastroprotective_effects_of_NN_diethyl_2_[4__phenylmethyl_phenoxy]_ethanamine_hydrochloride_a_non_H1/non_H2_histamine_antagonist_ DB - PRIME DP - Unbound Medicine ER -
Grapherence [↓3]

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