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At least 415 records · Page 23Linked to original sources
PubMed1983

Determination of histamine, methylhistamines and histamine-o-phthaldialdehyde complexes by two high-performance liquid chromatographic procedures. Application to biological samples.

Two high-performance liquid chromatographic procedures were proposed to measure histamine. The first, with UV detection and a strong acid cation exchanger (Partisil 10, SCX Whatman), made it possible to isolate histamine and some methylated derivatives. The second, with a C18 sorbent (mu Bondapak, Waters, 10 microns particle size) eluted with ion-pairing phases, made it possible to isolate the histamine-o-phthaldialdehyde complexes. This last procedure allied with a chromatographic purification step gave lower or identical amounts of histamine than those described in human urine (16 +/- 7 micrograms per 24 h), canine whole blood (1.5 +/- 1 ng/ml) and human gastric juice (2.3 +/- 1.4 ng/ml). The two procedures gave the concentration of a histamine-like compound isolated from the antral mucosa.

Animals↗
PubMed1993

Cutaneous histamine reactivity, histamine content of commercial allergens, and potential for false-positive skin test reactions in dogs.

The cutaneous reactivity of normal and atopic dogs to intradermal injections of histamine phosphate was evaluated. Significant differences were not found in the mean wheal diameters of either group. Commercial allergens used for intradermal skin testing and immunotherapy were determined to contain histamine. To determine whether allergen histamine content was sufficient to cause false-positive skin test results, the cutaneous response of Johnson grass allergic dogs was compared, using commercial Johnson grass allergen and commercial Johnson grass allergen with histamine removed. Significant differences were not noticed between Johnson grass and dehistaminized Johnson grass. Therefore, the histamine content of commercial Johnson grass allergen did not appear to cause false-positive skin test results for this group of Johnson grass allergic dogs.

Allergens↗
PubMed1996

Effects of systemic corticosteroids on cutaneous histamine secretion and histamine-releasing factor in patients with chronic idiopathic urticaria.

BACKGROUND: Enhanced skin mast cell releasability of histamine, increased production of histamine releasing factor (HRF), and cutaneous inflammatory process are the hallmarks of chronic idiopathic urticaria (CU). Although H1-antihistamines are known to alleviate the symptoms effectively in most cases, systemic corticosteroids (CS) are given in more resistant patients. Their mode of action remains a matter of controversy. OBJECTIVES: In the present study, the effects of a 7-day course of CS or placebo on histamine content and HRF production in non-lesional skin of 19 CU patients were examined. METHODS: Using the skin chamber technique, HRF production and histamine content were assessed in normal-appearing skin of patients with CU over a 2-h observation period. Those two parameters were measured before and after treatment, in a double-blind fashion. RESULTS: No significant changes occurred in any parameters after placebo treatment. In contrast with this, significant decrease of HRF activity was observed after 1 week of oral methylprednisolone while no change was documented for histamine secretion. CONCLUSION: These data suggest that CS therapy improves symptoms of CU in association with a decreased production of HRF in uninvolved skin.

Adult↗
PubMed1997

[The influence of multiple histamine inhalation on nonspecific airway hyperresponsiveness to histamine in patients with bronchial asthma].

The study was performed in 19 patients with stable mild/moderate asthma aged from 16 to 66. Nonspecific airway hyperresponsiveness (AH) to histamine was measured according to Cockcroft's et al. method and expresses as PC20H in mg/ml. The study was controlled by inhalation of PBS. The histamine or PBS challenges were performed three times at 45 min. intervals on the third day in case when the stability of AH on two preceding days was observed. The geometric means of PC20H (xg PC20H) during the consecutive three days did not change. They were 0.97, 0.92, 0.87 mg/ml (p > 0.05) respectively. Three times histamine challenges performed on the same day induced the decrease of AH (xg PC20H increased from 1.48 to 6.55 mg/ml) in 5 patients. In 4 other subjects the increase of AH was observed (xg PC20H decreased from 1.14 to 0.20 mg/ml). In 10 subjects the three times histamine challenges performed on the same day had no influence on AH to histamine.

Administration, Inhalation↗
PubMed2005

Inhibition of store-operated calcium entry-mediated superoxide generation by histamine trifluoromethyltoluide independent of histamine receptors.

Store-operated calcium entry (SOCE) plays an important role in shaping the Ca(2+) response of various tissues and cell types. In this report, we show that thapsigargin (TG)-induced SOCE was inhibited by the histamine receptor agonist, histamine-trifluoromethyltoluide (HTMT), in U937 and HL-60 human promyelocytes. Preincubation of HTMT resulted in a significant inhibition of subsequent TG-induced Ca(2+) elevation without affecting Ca(2+) release from intracellular stores. HTMT also inhibited TG-induced Ca(2+) current and Ba(2+)/Mn(2+) influx in a concentration-dependent manner. In contrast with HTMT, other H1 histamine receptor agonists, histamine, 2-methylhistamine and 2-thiazolylethylamine, did not affect TG-induced SOCE. In addition, HTMT also attenuated TG-induced cytosolic superoxide generation. Taken together, our data clearly suggest that the anti-inflammatory effect of HTMT may occur through direct inhibition of SOCE.

Calcium↗
PubMed2001

Histamine N-methyltransferase regulates histamine-induced phosphoinositide hydrolysis in guinea pig cerebellum.

We report here that the dose-response curve of the histamine-stimulated phosphoinositide hydrolysis in the guinea pig cerebellar slices was shifted to the left when the slices were pretreated with SKF 91488 (100 microM), a specific inhibitor of histamine N-methyltransferase (HMT). In contrast, the pretreatment of the cerebellar slices with aminoguanidine (100 microM - 1 mM), an inhibitor of diamine oxidase, had no effect on histamine-induced phosphoinositide hydrolysis. HMT mRNA was expressed abundantly in cerebellum, especially in Purkinje cells. These observations suggest that HMT regulates histaminergic neurotransmission in guinea pig cerebellum more predominantly than diamine oxidase in histamine degradation.

Animals↗
PubMed1985

H2 histaminic receptors in rat cerebral cortex. 3. Inhibition of [3H]histamine by H2 agonists.

The binding of [3H]histamine to H2 receptors in homogenates of rat cerebral cortex is inhibited by 11 H2 agonists in a characteristic and unique manner. At low concentrations of the radioligand (less than 1.5 nM), the inhibitory profiles of individual agonists (A) are distinctly biphasic; specific binding is well described in most cases by the empirical expression Y = F1K1/(K1 + [A]) + F2K2/(K2 + [A]), in which F1 and F2 sum to 1. Maximal inhibition is the same for all agonists. Since values of F2 vary from 0.42 to 0.90, the agonist appears to determine the equilibrium distribution of receptors between two states of affinity. Ratios of apparent affinity (K2/K1) vary from 204 to 3 090 000, and there is no correlation between values of K1 and K2. Compounds lacking H2 activity, including structural analogues of histamine and dimaprit, reveal a Hill coefficient of 1 and inhibit the radioligand only weakly. For six agonists, values of K2 agree and correlate well (P = 0.00047) with H2 pharmacological potency (EC50) in the guinea pig right atrium; for the others, K2 is less than EC50 by 15-61-fold. Four observations suggest that the inhibition corresponding to F1 is allosteric and cooperative: the dissociation constant of the radioligand appears to vary in the presence of an unlabeled agonist, absolute levels of binding corresponding to F1, as defined by dimaprit, decrease at higher concentrations of [3H]histamine, F1 for dimaprit is reduced from 0.48 to 0.32 by 2-methylhistamine (F1 = 0.27) at a concentration of 20 nM (approximately K1(0.5) K2(0.5) for 2-methylhistamine), but the increase in K1 for dimprit is at least 100-fold less than expected from competitive effects, and 1 equiv of some agonists appears to preclude access of [3H]histamine to more than 1 equiv of receptors, with no evidence that an appreciable fraction of the unlabeled drug is bound. Noncompetitive effects also may account in part for the inhibition corresponding to F2.

Animals↗
PubMedDate not supplied

Histamine upregulates Th1 and downregulates Th2 responses due to different patterns of surface histamine 1 and 2 receptor expression.

Histamine, which acts via G protein-coupled receptors, is an important mediator of immediate hypersensitivity and is also able to influence the nature of T cell responses. We demonstrated that TH1 and Th2 cells express distinct surface histamine receptor patterns and that Th1-type responses are enhanced by histamine, whereas Th2-type responses are negatively regulated, due to different intracellular signals generated by histamine stimulation. These findings account for negative feedback regulation in a wide variety of pathologies.

Cells, Cultured↗
PubMed1996

Prophylactic administration of histamine 1 and/or histamine 2 receptor blockers in the prevention of heparin- and protamine-related haemodynamic effects.

The efficacy of prophylactic administration of H1 and H2 receptor blockers to prevent adverse haemodynamic responses to heparin and protamine was studied. The control group (n = 10) received no histamine receptor blocker, group H1 (n = 10) received oral terfenadine 60 mg, group H2 (n = 10) received oral ranitidine 300 mg, and group H1+H2 (n = 10) received both terfenadine and ranitidine on the night before the operation and on call to the operating room. Heparin sulphate 300 U/kg was injected directly into the right atrium, and protamine hydrochloride was administered at the conclusion of bypass over at least three minutes through a peripheral route. Following the injection of heparin, plasma histamine-like activity (H-LA) was increased significantly in all four groups. While systolic, diastolic, mean arterial and central venous pressures were decreased significantly in the control group, no significant changes were observed in the H1 and H2 groups. Protamine infusion did not lead to an increase in H-LA. Prophylactic administration of histamine receptor blockers (H1 or H2) attenuated the heparin-induced adverse haemodynamic response but did not change the protamine-related haemodynamic effects. Factors other than histamine may play a major role in protamine induced cardiovascular changes.

Administration, Oral↗
PubMed2004

Methamphetamine and brain histamine: a study using histamine-related gene knockout mice.

The central histamine (HA) neurons that originate from the posterior hypothalamus modulate a variety of physiological functions. In order to investigate the roles of brain histaminergic neuron system in the behavioral effects of methamphetamine (METH), we administrated METH repeatedly to L-histidine decarboxylase (HDC)-, histamine H1 receptor-, H2 receptor-gene knockout (KO) mice, H1/H2 receptor-gene double KO mice, and wild type (WT) mice corresponding to each of them, and we measured locomotor activities. We also measured the contents of monoamines and amino acids in the brain of HDC-gene KO and WT mice after a single administration of METH. METH-induced locomotor hyperactivity and the development of behavioral sensitization were facilitated more in the HDC-gene KO mice and H1/H2 gene double KO mice than the WT mice, suggesting that brain histamine has an inhibitory effect on the METH action through both H1 and H2 receptors. In addition, neurochemical study suggested the involvement of the GABAergic neuron system in the inhibitory effect of brain histamine.

Animals↗
PubMed1983

Inhibitory effects of histamine antagonists on the skin reaction with house dust allergen, histamine and compound 48/80 in Japanese monkeys.

Using the skin of monkeys, we studied the participation of histamine receptors in the immediate skin reaction. Intradermal injection of H2 agonist produced whealing reaction to a significant degree, although this effect was not so remarkable as the effect of H1 agonist. A non-thiourea H2 antagonist showed a significant inhibitory effect on the whealing reaction to allergen, compound 48/80, and histamine. These results suggest that H2 antagonist prevented the whealing reaction by changing the vascular reaction to secreted or exogenous histamine. However, the participation of histamine receptors on dermal mast cells in the immediate skin allergic reaction is still left inconclusive.

Animals↗
PubMed2003

[Effect of fexofenadine--selective antagonist of histamine receptor (H1) on histamine-induced bronchoconstriction].

The aim of the study was to evaluate the effect of single and repeated fexofenadine (120 mg/day) doses on histamine-induced bronchoconstriction. Sixteen patients with mild, stabile asthma were examined. Bronchial reactivity was estimated as histamine dose (in mg/ml) causing a 20% FEV1 fall. A significant blockade of histamine H1 receptors in the airways was observed from the 1st to the 3rd day of the study. In all patients treated with fexofenadine, histamine in 16 mg/ml dose failed to induce bronchoconstriction. After another three days without fexofenadine, bronchial responsiveness returned to the initial value. The study points out that fexofenadine blocks H1 receptors in the bronchial tree.

Adult↗
PubMedDate not supplied

[Effect of H1- and H2-histamine receptor blockaders on lesions of the gastric mucosa evoked by exogenous histamine in guinea pigs].

It was demonstrated in experiments on guinea pigs with the use of a histamine model of ulcerogenesis that blocking agents of H1-histamine receptors produced a more marked gastro-protective effect than H2-antagonists. The results of the study confirm the hypothesis that histamine-induced ulceration of the gastric mucosa occurs through the mediation of H1-receptors. H2-histamine receptors play a secondary role in this process.

Animals↗
PubMed1987

Histamine and growth: interaction of antiestrogen binding site ligands with a novel histamine site that may be associated with calcium channels.

N,N-Diethyl-2-[(4-phenylmethyl)-phenoxy]ethanamine hydrochloride (DPPE) is a novel paradiphenylmethane derivative with antiproliferative and antiestrogenic properties. Like tamoxifen (TAM), DPPE binds to the microsomal antiestrogen binding site with high affinity (Kd approximately 50 nM), but, conversely, not to estrogen receptor or calmodulin. We now demonstrate that DPPE competes for [3H]histamine binding in rat cerebral cortex with an affinity (Ki = 4.5 +/- 2.6 X 10(-6) M) significantly greater than that of the H1 antagonist pyrilamine (Ki = 7.2 +/- 2.2 X 10(-5) M), despite the previous demonstration that pyrilamine is up to 1000 times more potent than DPPE in antagonizing histamine-induced contraction in canine tracheal smooth muscle. DPPE demonstrates antiproliferative activity against MCF-7 cells at concentrations between 1 X 10(-7) and 1 X 10(-5) M; the IC50 value of DPPE for growth inhibition at 7 days in this assay is 5 X 10(-6) M, a value equivalent to its Ki value for histamine binding. DPPE also competes for [3H]verapamil binding in membranes from whole rat brain with an affinity equal to that for verapamil (Kd = 4.0 +/- 1.8 X 10(-7) M); however, verapamil competes for [3H]DPPE binding in brain membranes and rat liver microsomes with an affinity markedly lower (Ki approximately 1 X 10(-4) M) than that of DPPE, suggesting allosteric interactions between the verapamil and DPPE sites. Unlike DPPE, verapamil is not antiproliferative in vitro against MCF-7 cells at concentrations up 1 X 10(-5) M, but, like DPPE, is cytotoxic at concentrations of 1 X 10(-4) M. In immature oophorectomized rats, verapamil or DPPE alone is antiuterotropic; however, verapamil shows no antagonism of exogenous estradiol on uterine growth, as opposed to DPPE which is a partial antagonist. Thus, the antiproliferative and antiestrogenic properties of DPPE either are not associated with calcium channel antagonism, or result from a qualitatively different effect on channels than verapamil. The in vitro antiproliferative effect of DPPE (7.5 X 10(-6) M) on MCF-7 cells at 72 h is significantly reversed by 10 mM L-histidine (70.2 +/- 12.6% reversal) and L-methionine (92.4 +/- 11.1% reversal), but not by L-ornithine, L-arginine, L-phenylalanine, or exogenous histamine. At lower concentrations of TAM (0.75 X 10(-6) M), where growth inhibition is estrogen-reversible, L-ornithine, but not L-histidine or L-methionine, causes significant reversal of growth inhibition (66.8 +/- 13.3%; p less than 0.001).(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMed1995

[Effect of loratadine, selective antagonist of histamine H1 receptors, on histamine-induced bronchoconstriction].

The aim of this study was to assess the duration of Loratadine effect on histamine H1 receptor in the airway. Six patients with mild or moderate asthma were examined. Bronchial reactivity to histamine was measured according to Cockcroft. The significant blockade of histamine H1 receptors in airway was observed from the 2nd day when 10 mg of Lo was given daily. The maximal protection with 10 mg doses was observed after 3-4 days. After another 5-6 days without Loratadine bronchial responsiveness return to the initial values. Single dose of 30 mg Loratadine given better protection against histamine bronchoconstriction than 10 mg given for 5 days. This effect was observed as early as 60 minutes after administration of Loratadine.

Adult↗
PubMed2005

Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.

The histamine H(4) receptor (H(4)R) is involved in the chemotaxis of leukocytes and mast cells to sites of inflammation and is suggested to be a potential drug target for asthma and allergy. So far, selective H(4)R agonists have not been identified. In the present study, we therefore evaluated the human H(4)R (hH(4)R) for its interaction with various known histaminergic ligands. Almost all of the tested H(1)R and H(2)R antagonists, including several important therapeutics, displaced less than 30% of specific [(3)H]histamine binding to the hH(4)R at concentrations up to 10 microM. Most of the tested H(2)R agonists and imidazole-based H(3)R ligands show micromolar-to-nanomolar range hH(4)R affinity, and these ligands exert different intrinsic hH(4)R activities, ranging from full agonists to inverse agonists. Interestingly, we identified 4-methylhistamine as a high-affinity H(4)R ligand (K(i) = 50 nM) that has a >100-fold selectivity for the hH(4)R over the other histamine receptor subtypes. Moreover, 4-methylhistamine potently activated the hH(4)R (pEC(50) = 7.4 +/- 0.1; alpha = 1), and this response was competitively antagonized by the selective H(4)R antagonist JNJ 7777120 [1-[(5-chloro-1H-indol-2-yl)-carbonyl]-4-methylpiperazine] (pA(2) = 7.8). The identification of 4-methylhistamine as a potent H(4)R agonist is of major importance for future studies to unravel the physiological roles of the H(4)R.

Cell Line↗
PubMed1983

Histamine release into tracheal lumen and bronchial reactivity. Effect of local allergen administration on histamine release and bronchial reactivity.

The influence of tracheal lavage with an allergen on the airway response to bronchial challenge with histamine, acetylcholine, and ascaris extract was investigated in 36 dogs. High histamine concentrations were measured in the tracheal solution after lavage with allergen. This amine, released on the mucosal surface, was observed in only very small concentrations in the circulation. Airway response to acetylcholine inhalation was significantly increased after tracheal lavage with allergen. This hyperreactivity of the lower airways induced by tracheal lavage with an allergen suggests that a reflex mechanism is involved. After histamine inhalation a significantly larger antigen-induced histamine release to tracheal lumen was observed. No influence on airway response was found after tracheal lavage with H2O.

Acetylcholine↗
PubMed1983

Histamine and histamine-N-methyltransferase in the CSF of patients with multiple sclerosis.

The CSF of twenty-six patients with multiple sclerosis (MS) and of twelve control persons was analysed for histamine and histamine-N-methyltransferase (HMT) activity. Both in patients with remitting and progressive type of disease the histamine level was about 60% higher than in the controls. On the other hand in both groups of patients the HMT activity was significantly lower (32% and 40% respectively) than that of controls. These results suggest an altered histamine metabolism in MS. This might be associated with the immune reaction in MS brain.

Adolescent↗