Prostaglandins (PGE1, PGE2, PGA1) and histamine have opposing effects on gastric HCl secretion, but we found that both stimulate adenylate cyclase activity in cell-free membrane preparations of guinea pig gastric fundic mucosa. The stimulatory effect of prostaglandins was found in this study to be specific and dose-dependent over a concentration range from 10(-7) to 10(-4) M. In similar prepara...

In this study, the effects of intraperitoneal (ip) injection of physostigmine, subcutaneous (sc) injection of atropine, and intracerebroventricular (icv) injections of histamine, chlorpheniramine (H(1)-receptor antagonist), and ranitidine (H(2)-receptor antagonist) in separate and combined treatments were investigated during yawning in rats. Physostigmine at a dose of 0.25 mg/kg produced the hi...

Histamine, in vitro, via H2-receptor activation, exerts an inhibitory effect on polymorphonuclear (PMN) chemotaxis and T-lymphocyte proliferation. The aim of this study was to verify these histamine inhibitory effects in man. Healthy and asymptomatic asthmatic volunteers inhaled a histamine (0.1%), methacholine (0.1%) or saline aerosol for 3 min. Asthmatics were selected on the basis of low bro...

Histamine is an inflammatory mediator present in mast cells, which are abundant in the wall of the gallbladder. We examined the electrical properties of gallbladder smooth muscle and nerve associated with histamine-induced changes in gallbladder tone. Recordings were made from gallbladder smooth muscle and neurons, and responses to histamine and receptor subtype-specific compounds were tested. ...

The histamine H4 receptor is mainly expressed in haematopoietic cells, hence is linked to inflammatory and immune system conditions. It has been recently discovered that the receptor is expressed also in the mammalian central nervous system (CNS), but its role in the brain remains unclear. We address the potential functions of the histamine H4 receptor in the human brain using a 'guilty by asso...

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...

A key role for histamine in the physiological control of gastric acid secretion was established with the advent of the histamine H2-receptor antagonists which have in vivo been shown to inhibit virtually all forms of basal and stimulated secretion.' These data can be seen to support the common mediator hypothesis championed in the last three decades by Code2 3 and which states that secretory st...

The G(i/o)-coupled histamine H(4) receptor is highly expressed in hemopoietic cells and is a promising new target for the treatment of chronic inflammatory diseases. 1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine (JNJ7777120) has been described as a selective antagonist at the H(4) receptor and is widely used to characterize the physiological role of the H(4) receptor. We have investi...

A key role for histamine in the physiological control of gastric acid secretion was established with the advent of the histamine H2-receptor antagonists which have in vivo been shown to inhibit virtually all forms of basal and stimulated secretion.' These data can be seen to support the common mediator hypothesis championed in the last three decades by Code2 3 and which states that secretory st...

A key role for histamine in the physiological control of gastric acid secretion was established with the advent of the histamine H2-receptor antagonists which have in vivo been shown to inhibit virtually all forms of basal and stimulated secretion.' These data can be seen to support the common mediator hypothesis championed in the last three decades by Code2 3 and which states that secretory st...