BACKGROUND Atopic dermatitis constitutes a most burdensome chronic inflammatory skin disease. Standard treatment is cumbersome and often targets its main symptom, pruritus, only insufficiently. FINDINGS Recent advances in our understanding of the role of histamine and its four receptors suggest new approaches which target the histamine receptors alone or as combination therapies to more effic...

Histamine membrane receptors are defined as either H1 (blocked by diphenhydramine-like antagonists) or H2 (blocked by cimetidine-like agents). We now report the solubilization, separation, and partial characterization of specific H1 and H2 membrane receptors from calf thymocytes. Membrane fragments were incubated with [3H]histamine either alone or with unlabeled histamine, diphenhydramine, or c...

Histamine and prostaglandins (PGs) play a variety of physiological roles as autacoids, which function in the vicinity of their sources and maintain local homeostasis in the body. They stimulate target cells by acting on their specific receptors, which are coupled to trimeric G proteins. For the precise understanding of the physiological roles of histamine and PGs, it is necessary to clarify the...

Champion, Hunter C., Trinity J. Bivalacqua, David G. Lambert, Rasheed A. Abassi, and Philip J. Kadowitz. Analysis of vasoconstrictor responses to histamine in the hindlimb vascular bed of the rabbit. Am. J. Physiol. 277 (Regulatory Integrative Comp. Physiol. 46): R1179–R1187, 1999.—Hemodynamic responses to histamine were investigated in the anesthetized rabbit. Intravenous injections of histami...

BACKGROUND End tidal inspiratory activity (ETIA) in diaphragm and parasternal intercostal muscles can be evoked in man and in animals by administration of histamine. Exacerbations of asthma and administration of histamine are often accompanied by hyperinflation. The aims of the study were to determine (1) the magnitude of ETIA in response to histamine in man, (2) the relative contributions of c...

Histamine is a well known amine which controls many physiological functions of the CNS, including; fluid balance, appetite, thermoregulation, cardiovascular control, learning and stress response. All these functions are done via three membranous H1, H2 and H3 receptors, which in laboratory animals feeding behaviour is under the control of H1 type. In order to investigate the central effect of h...

Anxiety-related behaviors increase histamine and dopamine release in the brain. On the other hand, central histamine counteracts reward and reinforcement processes mediated by the mesolimbic dopamine system. We investigated the effects of the histaminergic system and dopamine D2 receptors agents and their interactions on anxiety-related behaviors using the elevated plus-maze (EPM). The intra-hi...

Histamine mediates its physiological function through binding to four known histamine receptors. Here, we describe the first selective antagonist of the histamine H4 receptor, the newest member of the histamine receptor family, and provide evidence that such antagonists have anti-inflammatory activity in vivo. 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ 7777120) has a K(i) of 4...

The histamine H2 receptor is a member of the family of G-protein-coupled receptors and is linked to the activation of adenylate cyclase phospholipase C (PLC). In this study we examined the effects of protein kinase C (PKC) activation in Chinese hamster ovary (CHO) cells stably expressing canine histamine H2 receptors. Pretreatment with 100 nM phorbol 12-myristate 13-acetate at 37 degrees C for ...