Histamine plays an important role as neurotransmitter and chemical mediator in multiple physiological and pathophysiological processes in central and peripheral tissues. In the last century the extensive study of its actions in the human body, resulted in the identification of four G protein-coupled receptor (GPCR) subtypes (H1R-H4R), mediating numerous effects. The successful application of H1...

γ-Aminobutyric acid (GABA), which is synthesized by glutamic acid decarboxylase from glutamic acid, is the main inhibitory neurotransmitter and plays a key role in modulating neuronal activity in mammalian central nervous system. Addit ional ly , GABA is considered to be a multifunctional molecule that has different situational functions in some nonneuronal tissues. GABA exerts its actions via ...

It is well known that histamine produces constriction via H1 receptors and decreases tracheal smooth muscle tone via H2 and H3 receptors. In addition, it has already been reported that 3-methylhistamine and phenylethylamine are competitive antagonists of histamine N-methyl-transferase (HMT), the enzyme responsible for rapid inactivation of histamine. Our results suggest the possibility that 3me...

Histamine is present in high concentrations in the intestine and we investigated the possibility that it might have a role here in intestinal transport. When added to the basal side of rabbit ileal mucosa in vitro histamine (10(-4)M) induced a short-lived increase in electrical potential difference and short circuit current. It inhibited net chloride absorption but did not influence sodium tran...

There exists a possibility of interactions of histaminergic system with other neurotransmitters and their receptors in the central nervous system. Experimental evidences suggest a possible inhibitory influence of histaminergic system on the dopaminergic system. To elucidate the possible interaction between the histaminergic and dopaminergic pathways, we devised a strategy to study their effects...

Receptors for small endogenous hormones on human leukocytes were studied by insolubilizing the hormones and incubating them with the cells. Histamine, norepinephrine, and prostaglandin E(2) (PGE(2)) were conjugated to either of two types of carrier: (bovine or rabbit) serum albumin or a random copolymer of DL-alanine and L-tyrosine. The conjugates were linked to agarose beads (Sepharose) and th...

Hemodynamic responses to histamine were investigated in the anesthetized rabbit. Intravenous injections of histamine induced dose-dependent decreases in systemic arterial pressure that were blocked by the H1-receptor antagonist pyrilamine but not the H2 antagonist cimetidine. Injections of histamine and the H1 agonist 6-[2-(4-imidazolyl)ethylamine]- N-(4-trifuormethylphenyl)-heptanecardoxamide ...

The diverse physiological functions of histamine are mediated through distinct histamine receptors. Mast cells are major producers of histamine, yet effects of histamine on mast cells are currently unclear. The present study shows that histamine induces chemotaxis of mouse mast cells, without affecting mast cell degranulation. Mast cell chemotaxis toward histamine could be blocked by the dual H...

Histamine, a biological amine, is considered as a principle mediator of many pathological processes regulating several essential events in allergies and autoimmune diseases. It stimulates different biological activities through differential expression of four types of histamine receptors (H1R, H2R, H3R and H4R) on secretion by effector cells (mast cells and basophils) through various immunologi...