[3H]Doxepin, a tricyclic antidepressant, binds with high affinity to guinea pig brain membranes with a drug specificity indicating an association with H1 histamine receptors. The [3H]doxepin binding site has been solubilized, with digitonin being the only detergent able to maintain specific binding after solubilization. After solubilization, the kinetics and drug specificity of binding are virt...

Vasoactive intestinal peptide (VIP) is known to induce histamine release in human skin and known to include a NO-dependent dilation in several other vascular beds. However, the relative contribution of histamine and NO to VIP-mediated vasodilation in human skin is unknown. Forty three subjects volunteered to participate in two studies designed to examine the mechanism of VIP-mediated vasodilati...

Serotonin and histamine H1, H2 receptor agonists or antagonists inhibited [3H]histamine uptake by HL-60 cells, according to the following order of potency: impromidine greater than 4-MH greater than histamine greater than AET greater than PEA and: cimetidine, histamine greater than diphenhydramine, serotonin. It is concluded that histamine uptake by HL-60 cells was specifically controlled by th...

Vasoactive intestinal peptide (VIP) is known to induce histamine release in human skin and to include a nitric oxide (NO)-dependent dilation in several other vascular beds. However, the relative contribution of histamine and NO to VIP-mediated vasodilation in human skin is unknown. Forty-three subjects volunteered to participate in two studies designed to examine the mechanism of VIP-mediated v...

Restraint-induced stress (RS) increases histamine concentration in the brain. There is no previous report regarding the role of histamine receptors in immunomodulatory effect of RS. In the present study the role of brain histamine receptors on reduction of humoral and cellular immune function induced by RS was evaluated. For this purpose male Wistar rats (200-250 g) were immunized with sheep re...

Retrieval represents a dynamic process that may require neuromodulatory signaling. Here, we report that the integrity of the brain histaminergic system is necessary for retrieval of inhibitory avoidance (IA) memory, because rats depleted of histamine through lateral ventricle injections of α-fluoromethylhistidine (a-FMHis), a suicide inhibitor of histidine decarboxylase, displayed impaired IA m...

Pharmacodynamic mechanisms of diabetes induced by antipsychotic drugs remain unclear, while numerous receptors have been suspected to be involved in the genesis of this Adverse Drug Reaction (ADR). We investigated potential relationships between antipsychotics׳ receptor occupancy (serotonin 5-HT1A, 5-HT2A, 5-HT2C, histamine H1, muscarinic M3, adrenergic α1, α2 or dopaminergic D2 D3 occupancies)...

The monoterpene 4-carvomenthenol (Carvo) is found in essential oils of plant. Here, we evaluate the Carvo oral pretreatment acute inflammatory experimental models and silico molecular docking. Mice pretreated with were challenged submitted to protocols: paw edema, peritonitis, scratching behavior anaphylactic shock reaction. Besides, used histamine H1 receptor, cyclooxygenases (COX-1 COX-2) pho...

Histamine H1 receptors mediate activation of phospholipase C, with subsequent increases in cytosolic Ca2+ concentration ([Ca2+]i), and H2 receptors mediate accumulation of cAMP. HL-60 promyelocytes possess H2 receptors, but it is not known whether these cells also possess H1 receptors. We studied the effects of histamine on [Ca2+]i and the functional importance of histamine receptors in HL-60 p...