2001
DOI: 10.1038/sj.bjp.0703934
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Protective effect of a PAR2‐activating peptide on histamine‐induced bronchoconstriction in guinea‐pig

Abstract: 1 Protease activated receptor-2 (PAR2) is a seven transmembrane domain G protein coupled receptor proteolytically activated. PAR2, together with other PARs, can be also activated by peptides mimicking the sequence of the receptor tethered ligand. We have evaluated the eect of systemic administration of a peptide activating PAR2 (PAR2-AP, SLIGRL) on histamine-induced increase in lung resistances in the guinea-pig. 2 Intravenous administration of PAR2-AP (1 mg kg 71 ) signi®cantly inhibited histamine-induced inc… Show more

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Cited by 29 publications
(24 citation statements)
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References 23 publications
(29 reference statements)
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“…14,15,19,[23][24][25] Most studies show that PAR-2 has a proinflammatory effect via PAR-2 agonist experiments, but some reports suggest that PAR-2 can have a protective effect against inflammation. 18,[24][25][26][27][28] Clearly, the role(s) of PAR-2 in inflammation is still not fully understood. Other recent results include the finding of increased PAR-2 expression in respiratory epithelial cells from patients with asthma.…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…14,15,19,[23][24][25] Most studies show that PAR-2 has a proinflammatory effect via PAR-2 agonist experiments, but some reports suggest that PAR-2 can have a protective effect against inflammation. 18,[24][25][26][27][28] Clearly, the role(s) of PAR-2 in inflammation is still not fully understood. Other recent results include the finding of increased PAR-2 expression in respiratory epithelial cells from patients with asthma.…”
Section: Discussionmentioning
confidence: 99%
“…25 However, there is also evidence that PAR-2 may play a protective role in the airways. PAR-2 activation induces bronchodilation 18,26,27 and attenuates antigen-induced bronchoconstriction in animal models. 28 We conducted an association study of PAR-2 polymorphisms with susceptibility to atopy in a Korean childhood cohort.…”
mentioning
confidence: 99%
“…However, there is controversy about whether PAR2 agonists protect or promote airway inflammation. In support of a protective role are observations that PAR2 agonists induce an eicosanoid-dependent bronchodilation in rats, mice, and guinea pigs (8,12,13), and that intranasal administration of a PAR2 agonist in mice reduces the infiltration of neutrophils into bronchoalveolar lavage (BAL) after treatment with LPS (11). PAR2 agonists also relax the guinea pig trachea and human bronchi by releasing eicosanoids and NO from the epithelium (9,10).…”
Section: Protease-activated Receptor 2 Mediates Eosinophil Infiltratimentioning
confidence: 99%
“…In the mouse, rat, and guinea pig, PAR2 agonists partially reverse serotonin-and histamine-induced bronchoconstriction by stimulating the release of eicosanoids (8,12,13), and in mice a PAR2 agonist reduces the infiltration of neutrophils into BAL after treatment with LPS (11). PAR2 agonists also stimulate release-protective eicosanoids in the intestinal mucosa (22) and protect against gastric ulcers by stimulating secretion of mucus (39).…”
Section: Par2 Mediates Allergic Inflammation Of the Airwaysmentioning
confidence: 99%
“…According to the different in vitro preparations and experimental conditions used, proteases can mediate either relaxation [3] or contraction [4]. Moreover, the intravenous administration of the PAR-2 activating peptide (PAR-2 AP) SLIGRL (1 mg kg K1 ) can prevent in vivo histamine-induced bronchoconstriction in guinea-pigs [5]. Also the involvement of cyclooxygenase metabolites and NO in the relaxing effect of PARs agonists has been further investigated in guinea-pigs [3,5].…”
Section: Introductionmentioning
confidence: 99%