In conscious rats implanted with an intracerebroventricular (icv) cannula, effect of icv injections of histamine, chlorpheniramine (H -receptor antagonist) and ranitidine (H -receptor blocker) was investigated in a rat model of acute trigeminal pain. Acute trigeminal pain was induced by putting a drop of 5 M NaCl solution on the corneal surface of the eye and the numbers of eye wipes were count...

In the present study, effects of intracerebroventricular (icv) administration of histamine, mepyramine (H1-receptor antagonist) and famotidine (H2-receptor antagonist) have been investigated on the formalin test in rats. Subcutaneous injection of formalin (50 microl, 1%) into the ventral surface of the left hind paw produced a marked biphasic pain response (first phase: 0-5 min and second phase...

objective: crocin and safranal, as the major constituents of saffron, have many biological activities. this study investigated the effects of crocin and safranal on yawning response induced by intracerebroventricular (i.c.v.) injection of histamine in rats. materials and methods: in ketamine/xylazine-anesthetized rats, a guide cannula was implanted in the right ventricle of the brain and yawnin...

Dr. Iwan de Esch is an assistant professor and Prof. Rob Leurs is full professor and head of the Division of Medicinal Chemistry of the Leiden/Amsterdam Center of Drug Research (LACDR), VU University Amsterdam, The Netherlands. Since the seventies, histamine receptor research has been one of the traditional themes of the division. Molecular understanding of ligand-receptor interaction is obtain...

The present study investigated the effects of intra-dentate gyrus microinjection of naloxone (an opioid antagonist) and thioperamide (an antagonist of histamine H3 receptors) in the formalin test in rats. Subcutaneous injection of formalin (50 μl, 2.5 %) in the ventral surface of right hind paw produced a biphasic pattern (first phase: 0-5 min and second phase: 15 - 60 min) of licking/biting an...

Histamine receptors have been demonstrated on lymphocyte membranes by a variety of techniques. We now report a method that allows for the flow cytometric analysis of histamine receptors on human peripheral T cells. Histamine is conjugated to fluoresceinated human albumin by the coupling agent ECDI. This conjugated histamine compound (FHA-his) binds to approximately 45% of T cells. Fluoresceinat...

The histamine H3 receptor (H3R) has been recognized as a promising target for the treatment of various central and peripheral nervous system diseases. In this study, a non-imidazole compound, ZEL-H16, was identified as a novel histamine H3 receptor agonist. ZEL-H16 was found to bind to human H3R with a Ki value of approximately 2.07 nM and 4.36 nM to rat H3R. Further characterization indicated ...

N alpha-methylhistamine (N alpha-MH) is one of unusual metabolite of histamine that was found in Helicobacter pylori-infected stomach and is believed to interact with specific histamine H1, H2 and H3-receptors to stimulate gastric acid secretion and gastrin release from isolated G-cells but the effects of N alpha-MH on gastric mucosal integrity have been little studied. This study was designed;...

Histamine receptors are present on the surface of various normal and tumor-derived cell types, where their biological function is incompletely understood. Here we report that histamine not only stimulates cell proliferation under serum-free conditions, but also is chemotactic for human carcinoma (Hela and A431) and melanoma (A875) cells expressing H1 type receptors. Histamine was found to be a ...