Abstract

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