Relaxation and contraction responses to histamine in the human lung parenchymal strip

Vincenc, K. S.; Black, Judith L.; Shaw, John H.

doi:10.1016/0014-2999(84)90591-0

Cited by 26 publications

(10 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Thus, the pA2 values found in the present study, 9.57 and 8.75 for mepyramine In some species, bronchodilatation is mediated via H2-receptors (Okpako et al, 1978;Chand & De Roth, 1979). In contrast, and Vincec et al (1984) have described a histamine-induced tracheal relaxation not affected by H2-antagonists and have suggested the existence of HIreceptor subtypes or a third histamine receptor in the trachea. In the present study, histamine (10-9 M-10-6 M) induced a relaxation of precontracted tracheal segments followed by a contraction at higher concentrations.…”

Section: Discussionsupporting

confidence: 52%

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea

Cardell

Edvinsson

1994

British J Pharmacology

View full text Add to dashboard Cite

1 The histamine receptors were characterized on isolated circular segments of trachea and pulmonary arteries from the guinea-pig. The motor responses to histamine HI-, H2-and H3-receptor agonists and antagonists were tested and the responses obtained were analysed in relation to the respiratory epithelium and the vascular endothelium. 2 Histamine induced a biphasic response in trachea and in pulmonary arteries. In low concentrations, histamine acted as a potent relaxant agent of precontracted segments and in moderate concentrations it constricted both precontracted and resting segments. When arterial segments from different parts of the pulmonary vascular tree were compared, only small interregional differences in the vasomotor response were seen. 3 Mepyramine caused a parallel shift to the right of the histamine-induced concentration-response curves for both the trachea and the pulmonary artery, indicating a contractile HI-receptor. Cimetidine did not affect the histamine-induced contraction of the trachea, but a shift to the left was evident for low concentrations of histamine in the pulmonary artery. This is consistent with a dilator H2-receptor in the pulmonary artery. The pA2-value for mepyramine in the pulmonary artery, 8.75, was not affected by the presence of cimetidine. Thioperamide, a selective H3 antagonist, shifted the concentration-response for the trachea to the left. Schild analysis for histamine and mepyramine yielded a line with a slope of 0.61, whereas the same analysis in the presence of thioperamide yielded a line with a slope of 1.05 and an approximated pA2-value of 9.57. These results indicate the presence of a relaxant H3 receptor in the trachea. In precontracted tracheal segments, application of mepyramine and cimetidine did not affect the low dose histamine relaxation. Thioperamide caused a parallel shift of the histamine concentrationresponse curve to the right, supporting the suggestion of a dilator H3-receptor in the trachea. The pA2-value for thioperamide, in the presence of mepyramine, was 7.79. In precontracted pulmonary arteries the histamine-induced dilatation was small. In the presence of mepyramine a rather strong histamine-induced dilatation became evident and this concentration-response curve could be shifted to the right by cimetidine, with a pA2-value of 6.49. This is compatible with a dilator H2-receptor. 4 The H1-receptor agonists, thiazolylethylamine, 2-methylhistamine and pyridylethylamine and the rather unselective H2-agonist, 4-methylhistamine, induced contraction of resting tracheal and pulmonary arterial segments. In precontracted segments of trachea, all H1 and H2 agonists studied induced a dilator response. The two rather unselective histamine receptor agonists 2-methylhistamine and 4-methylhistamine were about 100 times more potent than other H1 and H2 agonists tested. In the pulmonary artery, the H2 agonists, impromidine, dimaprit and 4-methylhistamine induced a concentration-dependent relaxation. The relaxation of the pulmonary artery, elicited by the H1 a...

show abstract

Section: Discussionsupporting

confidence: 52%

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea

Cardell

Edvinsson

1994

British J Pharmacology

View full text Add to dashboard Cite

show abstract

“…In the presence of the latter, high hista mine concentrations elicited only pure relaxation sug gesting that from the studied antagonists dithiadene most selectively or intensively suppressed the effect of histamine on H| receptors. Chand and Eyre [1978] and Vincenc et al [1984] described however also hista mine-induced tracheal smooth muscle relaxation which was not affected by II2 antagonists and sug gested the possible existence of H| receptor subtypes or of a third histamine receptor in the trachea. The fact that histamine in the presence of dithiadene with the selective H2 antagonist ranitidine did not induce any relaxation would appear to support the involve ment of H2 and not H | or H3 receptors in the described relaxation.…”

Section: Discussionmentioning

confidence: 99%

Effect of Stobadine and Histamine H<sub>1</sub> and H<sub>2</sub> Blockers on Histamine–Induced Contraction of Guinea Pig Airways in vitro

Matyas

Bauer³

1990

Respiration

View full text Add to dashboard Cite

Histamine, a nonselective histamine receptor agonist, activates simultaneously both H₁ and H₂receptors in the guinea pig trachea and lung strip. The resulting contraction is due to the prevalence of H₁ receptors, because they are blocked by the selective H₁antagonist diphenhydramine. The H₂ receptor antagonists cimetidine and ranitidine increased the sensitivity of both tissues to histamine by affecting primarily the amplitude of contractions induced by high histamine concentrations. Since the lung strips were more sensitized by ranitidine and low concentrations of the other studied antagonists (diphenhydramine, dithiadene, stobadine) than the tracheal smooth muscle, it is inferred that the density of H₂ receptors is higher in peripheral than central airways. From all the studied histamine receptor antagonists only dithiadene was able to unmask the relaxation induced by H₂ receptor activation indicative of its highest H₁ selectivity. In the light of the concentration-dependent antihistaminic effect of stobadine, i.e. potentiation in low and inhibition in high concentrations, stobadine is suggested to belong to antihistaminics with no histamine receptor subtype selectivity

show abstract

“…Published data have shown that overnight storage of tissue does not alter its reactivity (Brink et al, 1980;Ghelani et al, 1980;Guillot et al, 1984;Vincenc et al, 1984). The tissue was stored overnight at 4°C and the experiment was carried out the next day.…”

Section: Human Bronchusmentioning

confidence: 99%

Effects of Noradrenaline on the Isolated Human Bronchus. Comparison With the Isolated Guinea Pig Trachea

Naline¹,

Advenier²,

Matran

et al. 1988

Fundamemntal Clinical Pharma

View full text Add to dashboard Cite

The pharmacodynamic activity of noradrenaline was evaluated comparatively in vitro on isolated human bronchi and on guinea pig tracheal spirals. Noradrenaline exerted a contractile effect on both preparations under resting tone and in the presence of propranolol 10(-6) M; maximal noradrenaline-induced contraction was 15-20% of maximal acetylcholine (ACh)-induced contraction. Without propranolol, the contractile effect of noradrenaline was negligible when the preparations were under resting tone and absent when they were precontracted with ACh. In contrast, noradrenaline exerted a strongly relaxant effect on both human bronchi (-log ED50 5.24 +/- 0.17; N = 5) and guinea pig tracheae (-log ED50 6.15 +/- 0.29; N = 8). With maximal contraction induced by ACh 3.10(-3) M the -log ED50 of both preparations were shifted to the right by functional antagonism and became 4.72 +/- 0.17 and 5.31 +/- 0.11, respectively. The pKD values of noradrenaline, calculated according to Furchgott and Bursztyn (1967), were 4.79 +/- 0.04 in human bronchi (N = 5) and 4.77 +/- 0.16 in guinea-pig tracheae (N = 8). In the presence of cocaine plus phenoxybenzamine these values were not significantly modified in human bronchi and only slightly modified in guinea pig tracheae. It is concluded that noradrenaline induces a strong beta-adrenergic response and a negligible alpha-adrenergic response from both human bronchi and guinea pig tracheae in vitro.

show abstract

Relaxation and contraction responses to histamine in the human lung parenchymal strip

Cited by 26 publications

References 24 publications

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea

Effect of Stobadine and Histamine H<sub>1</sub> and H<sub>2</sub> Blockers on Histamine–Induced Contraction of Guinea Pig Airways in vitro

Effects of Noradrenaline on the Isolated Human Bronchus. Comparison With the Isolated Guinea Pig Trachea

Contact Info

Product

Resources

About

Relaxation and contraction responses to histamine in the human lung parenchymal strip

Cited by 26 publications

References 24 publications

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H3 receptors in the trachea

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H3 receptors in the trachea

Effect of Stobadine and Histamine H<sub>1</sub> and H<sub>2</sub> Blockers on Histamine–Induced Contraction of Guinea Pig Airways in vitro

Effects of Noradrenaline on the Isolated Human Bronchus. Comparison With the Isolated Guinea Pig Trachea

Contact Info

Product

Resources

About

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea

Characterization of the histamine receptors in the guinea‐pig lung: evidence for relaxant histamine H₃ receptors in the trachea