Distribution of histamine receptors in isolated canine airways

1983 ◽  
Vol 54 (3) ◽  
pp. 693-700 ◽  
Author(s):  
S. L. Bradley ◽  
J. A. Russell
Keyword(s):  
Smooth Muscle ◽  
Histamine Receptors ◽  
Receptor Activity ◽  
Histamine H2 Receptor ◽  
H2 Receptor ◽  
H2 Antagonist ◽  
Histamine H1 Receptors ◽  
H1 Antagonist ◽  
Dose Dependent

The distribution of histamine receptors was examined in isolated trachealis smooth muscle strips and helical strips of large (5 mm) and small (1.5 mm) intrapulmonary airways. All airways contracted in response to histamine, but the sensitivity to this agent was significantly greater in intrapulmonary airways than in trachealis strips. A dose-dependent tachyphylaxis to histamine occurred when airways were exposed repeatedly to 10(-4) M histamine but not to 5 X 10(-6) M histamine. The H1-agonist, 2-methylhistamine, also caused airway contractions, although they were less forceful than those caused by histamine. Both histamine- and 2-methylhistamine-induced contractions were blocked by the H1-antagonist, pyrilamine. The H2-agonists, 4-methylhistamine and dimaprit, as well as histamine in the presence of pyrilamine failed to relax both acetylcholine- and 5-hydroxytryptamine-induced contractions. Moreover, the H2-antagonist, metiamide, had no effect on histamine-induced contractions. We conclude that histamine H1-receptors are present in both extrapulmonary and intrapulmonary airways of the dog and cause contraction when stimulated. In contrast, histamine H2-receptor activity could not be demonstrated in the airways of this species.

Effect of histamine on microvascular permeability in the rat stomach

1983 ◽  
Vol 245 (2) ◽  
pp. G201-G207
Author(s):  
H. Nagata ◽  
P. H. Guth
Keyword(s):  
Histamine Receptors ◽  
Microvascular Permeability ◽  
In Vivo Microscopy ◽  
Rat Stomach ◽  
Serosal Surface ◽  
H2 Antagonist ◽  
H1 Antagonist ◽  
Dose Dependent ◽  
Muscularis Externa

The effect of histamine on gastric microvascular permeability to macromolecules in the rat was studied using fluorescent in vivo microscopy. Histamine was applied topically to the serosal surface for study of the muscularis externa, to the submucosa, and to the superficial mucosa, and the area of leaks of a fluorescein-albumin conjugate from microvessels was quantitated. In the muscularis externa both histamine and an H1-agonist, but not an H2-agonist, caused dose-dependent leak of conjugate from venules. An H1-antagonist, but not an H2-antagonist, decreased the histamine-induced leak. In the submucosa histamine caused dose-dependent dilatation of arterioles but not leak of conjugate. In contrast, bradykinin caused both dose-dependent dilatation of arterioles and leak of conjugate from venules. In the superficial mucosa histamine did not cause any leak. In conclusion, topical histamine 1) increased microvascular permeability to macromolecules from venules in the muscularis externa via H1-receptors, 2) did not affect microvascular permeability in the submucosa (this may be due to lack of histamine receptors on the venules as bradykinin increased venular permeability), and 3) did not affect microvascular permeability in the superficial mucosa, but there might not have been adequate histamine backdiffusion.

Histamine receptor in bullfrog gastric mucosa

1981 ◽  
Vol 241 (2) ◽  
pp. G93-G97
Author(s):  
S. J. Hersey
Keyword(s):  
Gastric Mucosa ◽  
Histamine Receptor ◽  
Histamine Receptors ◽  
Histamine Antagonists ◽  
Competitive Antagonism ◽  
H2 Antagonist ◽  
H2 Receptors ◽  
High Concentrations ◽  
H1 Antagonist ◽  
Very High

The histamine receptor of isolated bullfrog gastric mucosa was characterized in terms of respiration and acid secretory responses to histamine antagonists and agonists. Cimetidine, a selective H2-antagonist, showed competitive antagonism of histamine responses with a pA2 value of 6.55. In contrast, the H1-antagonist, mepyramine, showed inhibition only at very high concentrations. Based on these results, the histamine receptor would be classified as the H2 type. Measurements of agonist potency sequence revealed a marked difference between the amphibian and mammalian gastric histamine receptors. The selective H1-agonists, 2-pyridylethylamine and 2-aminoethylthiozol, were found to be more efficacious than the selective H2-agonists, dimaprit and impromidine. The lack of efficacy for dimaprit and impromidine does not appear to be due to a lack of binding to the receptor because these agents inhibit responses to histamine. For dimaprit, the inhibition was found to be competitive with an apparent pA2 value of 5.37. These results indicate that there is a molecular difference between H2-receptors in mammals versus amphibians.

VIP and histamine H2 receptor activity in human fetal gastric glands

1986 ◽  
Vol 42 (4) ◽  
pp. 423-425 ◽  
Author(s):  
S. Emami ◽  
E. Chastre ◽  
N. Mulliez ◽  
M. Gonzales ◽  
C. Gespach
Keyword(s):  
Receptor Activity ◽  
Gastric Glands ◽  
Histamine H2 Receptor ◽  
H2 Receptor

Histamine H2 receptor activity and histamine metabolism in human U-937 monocyte-like cells and human peripheral monocytes

1986 ◽  
Vol 18 (1-2) ◽  
pp. 124-128 ◽  
Author(s):  
Christian Gespach ◽  
Anne Courillon-Mallet ◽  
Jean Marie Launay ◽  
Hélène Cost ◽  
Jean-Pierre Abita
Keyword(s):  
Receptor Activity ◽  
Histamine Metabolism ◽  
Histamine H2 Receptor ◽  
H2 Receptor

Up- and down-regulation of membrane receptors as possible mechanisms related to the antiulcer actions of milk in rat gastric mucosa

1987 ◽  
Vol 7 (2) ◽  
pp. 135-142 ◽  
Author(s):  
C. Gespach ◽  
S. Emami ◽  
E. Chastre ◽  
J.-M. Launay ◽  
G. Rosselin
Keyword(s):  
Gastric Mucosa ◽  
Competitive Inhibition ◽  
Membrane Receptors ◽  
Receptor Activity ◽  
Milk Diet ◽  
H2 Receptor Antagonist ◽  
Adult Rats ◽  
Parallel Displacement ◽  
Histamine H2 Receptor ◽  
H2 Receptor

The effects of a cow's milk diet on receptor activity and histamine metabolism in gastric glands and mucosa isolated from adult rats were examined. The milk diet was associated with (1) a decreased mobilization of H2 receptors by histamine and (2) an increased mobilization of PGE2 (prostaglandin E2) receptors in mucous cells (cytoprotective effect) and parietal cells (antiacid effect). These changes are not observed for the receptors reducing pentagastrin- and histamine-induced gastric acid secretion (pancreatic/enteroglucagons, somatostatin) and stimulating mucus, bicarbonate and pepsin secretions in the rat (secretin). Cimetidine produced a parallel displacement of the histamine dose-response curve, suggesting competitive inhibition between this classical H2 receptor antagonist and histamine in the two experimental groups. Prostaglandins and other components in milk such as EGF (epidermal growth factor) and somatostatin might therefore protect gastric mucosa by a differential control of PGE2 and histamine H2 receptor activity either directly (PGE2 in milk) or indirectly (inhibition of endogeneous histamine synthesis/release and stimulation of PGE-I synthesis/release).

Characterization of H1- and H2-receptor function in pulmonary and systemic circulations of sheep

1982 ◽  
Vol 53 (1) ◽  
pp. 175-184 ◽  
Author(s):  
T. Ahmed ◽  
K. B. Mirbahar ◽  
W. Oliver ◽  
P. Eyre ◽  
A. Wanner
Keyword(s):  
Vascular Tone ◽  
Base Line ◽  
H2 Receptor ◽  
Receptor Response ◽  
H2 Antagonist ◽  
H2 Receptors ◽  
H1 Antagonist ◽  
Vasodepressor Response

We investigated the histamine H1- and H2-receptor function in the pulmonary and systemic circulations of sheep by in vivo and in vitro techniques. Combined H1 and H2 stimulation (by intravenous histamine) in vivo increased pulmonary vascular resistance (PVR) to 435% of base line and decreased systemic vascular resistance (SVR) to 49% of base line. Selective H2 stimulation (histamine after chlorpheniramine pretreatment) decreased PVR and SVR to 86 and 82% at base line, respectively, while selective H1 stimulation (histamine after metiamide pretreatment) increased PVR to 424% of base line and decreased SVR to 64% of base line. Combined H1- and H2-antagonist pretreatment completely blocked the effects of histamine on SVR, while PVR still decreased to 85% of base line, suggesting a mild “atypical” H2-receptor response in the pulmonary circulation under conditions of resting vascular tone. With increased pulmonary vascular tone (hypoxia), histamine decreased PVR to 55% (H1-antagonist pretreatment) and to 58% (combined H1- and H2-antagonist pretreatment) of posthypoxia values, respectively, demonstrating a marked atypical H2-receptor response. In vitro, both pulmonary arterial and venous strips showed a contractile dose-response to histamine, which was blocked by the H1-antagonist pyrilamine (mepyramine). In precontracted strips, both histamine and the H2-agonists (dimaprit and impromidine) elicited a relaxant response, which was neither blocked by H1-antagonist alone nor by combined H1- and H2-antagonists. We conclude that in sheep the histamine-induced pulmonary vasoconstrictor response is mediated by H1-receptors, while the pulmonary vasodepressor response is mediated by atypical H2-receptors. The systemic vasodepressor response is mediated by both H1- and typical H2-receptors.

Increase of human platelet serotonin uptake by atypical histamine receptors

1994 ◽  
Vol 266 (2) ◽  
pp. R526-R536 ◽  
Author(s):  
J. M. Launay ◽  
D. Bondoux ◽  
M. J. Oset-Gasque ◽  
S. Emami ◽  
V. Mutel ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Human Platelet ◽  
Human Platelets ◽  
Histamine Receptors ◽  
Receptor Antagonists ◽  
H2 Receptor Antagonists ◽  
Histamine H2 Receptor ◽  
H2 Receptor ◽  
5 Ht Uptake

Histamine and the guanosine 3',5'-cyclic monophosphate (cGMP)-inducing agent sodium nitroprusside both increased serotonin (5-HT) uptake and cGMP levels in isolated human platelets in vitro. Histaminergic stimulation was observed at concentrations ranging from 10 nM to 0.25 microM [mean effective concentration (EC50) = 0.1 microM histamine]. The inhibition produced by the H2-receptor antagonists tiotidine, metiamide, and cimetidine was 10-10(5) times more potent on histamine receptors regulating 5-HT uptake and cGMP generation in human platelets than on the histaminergic receptors H1, HIC, H2, and H3 in other tissues. The in vitro histamine-induced 5-HT uptake was prevented by preincubation of isolated human platelets in the presence of the nitric oxide synthase inhibitor NG-monomethyl-L-arginine or the cGMP-lowering agent LY-83583. Histamine was ineffective in stimulating cAMP generation in human platelets and did not interact with effector sites known to downregulate 5-HT uptake, including imipramine, gamma-aminobutyric acid A, peripheral type benzodiazepine-binding sites, and V1a vasopressin receptors inducing human platelet shape change and aggregation. These atypical human platelet histaminergic receptors differ from the previously classified histamine receptors by their apparent high affinity to histamine H2-receptor antagonists and their apparent link with the soluble, nitric oxide-dependent guanylate cyclase. These findings suggest that human platelets express a new subtype H2h of histamine receptors.

Histamine H2 receptor activity during the differentiation of the human monocytic-like cell line U-937

FEBS Letters ◽  
1985 ◽  
Vol 184 (2) ◽  
pp. 207-213 ◽  
Author(s):  
Christian Gespach ◽  
Hélène Cost ◽  
Jean-Pierre Abita
Keyword(s):  
Cell Line ◽  
Receptor Activity ◽  
Histamine H2 Receptor ◽  
H2 Receptor
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