当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach.

Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach.

Abstract：

:The present study investigated the role of histamine H(3) and H(4) receptors in gastric mucosal defense, by the use of selective ligands. Firstly, the affinities of several histaminergic agonists for the rat histamine H(3) and H(4) receptors were checked in HEK 293T cells transfected with either receptor subtype. Next, functional activities were determined in conscious rat against the ulcerogenic effect of 0.6N HCl. Radioligand binding studies showed that immethridine and methimepip were the most selective agonists at rat H(3) receptors, whereas VUF10460 displayed approximately a 50-fold selectivity for the rat H(4) receptor over the H(3) receptor. In conscious rats, immethridine and methimepip significantly reduced (66% and 48% inhibition, respectively) the gastric lesions induced by HCl; the effect of immethridine was antagonized by the H(3) receptor antagonist A-331440, but not by the H(4) receptor antagonist JNJ7777120. The mixed H(3)/H(4) receptor agonist immepip induced a significant aggravation of HCl damage, which was prevented by JNJ7777120; HCl-induced lesions were also significantly enhanced by the H(4) receptor agonists VUF10460 and VUF8430; however, this effect was not modified by JNJ7777120. Overall, this study indicates that, whereas the histamine H(3) receptor is involved in the protection of rat stomach against concentrated HCl, the functional role of the H(4) receptor is still to be defined, although selective agonists induce proulcerogenic effects under HCl challenge. Finally, the species-dependent variations in affinity and receptor selectivity observed for most ligands need to be carefully addressed in the pharmacological characterization of histamine H(3) and H(4) receptor functions in vivo.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Coruzzi G,Adami M,Pozzoli C,de Esch IJ,Smits R,Leurs R

doi

10.1016/j.ejphar.2011.07.038

subject

Has Abstract

pub_date

2011-11-01 00:00:00

pages

121-7

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(11)00830-2

journal_volume

669

pub_type

杂志文章

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