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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Second-Generation Histamine H2-Receptor Antagonists with Gastric Mucosal Defensive Properties

Author(s): Takafumi Ichikawa, Kyoko Hotta and Kazuhiko Ishihara

Volume 9, Issue 5, 2009

Page: [581 - 589] Pages: 9

DOI: 10.2174/138955709788167646

Price: $65


Unlike the earlier agents in this class, certain of the newer histamine HB2B-receptor antagonists (so-called secondgeneration HB2B-receptor antagonists) have recently been reported to promote gastric mucosal defenses. We review herein the structure, specificity, and mechanisms of these agents with a special focus on their cytoprotective/gastroprotective actions.

Keywords: Calcitonin gene-related peptide (CGRP), capsaicin-sensitive nerves, gastroprotective action, histamine HB2B-receptor antagonists, lafutidine, mucin, roxatidine, structure-activity relationship

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