Abstract:
:The H1-histaminergic agonists 2-pyridylethylamine (2-PEA) and 2-methylhistamine relaxed potassium-constricted, perfused, rabbit middle cerebral arteries at low concentrations (3 x 10(-11) to 3 x 10(-8) M) and constricted them at high concentrations (3 x 10(-7) to 3 x 10(-4) M). The relaxation and the contraction were not antagonized by propranolol (up to 3 x 10(-6) M) given 30 min before, suggesting that beta-adrenergic mechanisms were not involved. When 2-PEA was tested on arteries constricted with uridine triphosphate (UTP), similar results were obtained. In the UTP-constricted arteries, the 2-PEA-induced responses were competitively antagonized by 3 x 10(-9) M mepyramine. Together with previous work (Ea Kim et al., 1986), these results are compatible with the hypothesis that H1-receptors were responsible for both the relaxation and the contraction observed. When either indomethacin (10(-8), 3 x 10(-7), or 10(-5) M), dexamethasone (10(-5) M), or tranylcypromine (10(-5) or 10(-4) M) were tested on the response to 2-PEA or 2-methylhistamine, these inhibitors suppressed the relaxation or reversed it to a contraction. Furthermore, they potentiated the contraction induced by these agonists. These results favour the hypothesis that the H1-mediated relaxation in rabbit cerebral arteries may in part involve the release of prostaglandins, especially prostacyclin. The participation of such a prostanoid in histaminergic relaxation seems exclusively an H1-mediated mechanism, since the relaxation induced by the H2-agonist dimaprit (in the presence of mepyramine) was not antagonized by either indomethacin (3 x 10(-7) M) or tranylcypromine (10(-4) M).
journal_name
Fundam Clin Pharmacoljournal_title
Fundamental & clinical pharmacologyauthors
Ea Kim L,Sercombe R,Oudart Ndoi
10.1111/j.1472-8206.1988.tb00648.xsubject
Has Abstractpub_date
1988-01-01 00:00:00pages
463-75issue
6eissn
0767-3981issn
1472-8206journal_volume
2pub_type
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