Abstract：
:FR 172357, a new non-peptide antagonist of the kinin B(2) receptor was tested in three isolated vessels, the human umbilical vein, the rabbit jugular vein, and the pig coronary artery, to evaluate its antagonistic activities against bradykinin. FR 172357 displaced to the right the concentration-response curves of bradykinin. The displacements were parallel to the controls without reduction of the maximum effect in the human umbilical vein and in the rabbit jugular vein, but not in the pig coronary artery. Schild plots confirmed that FR 172357 acts as a competitive antagonist in the human umbilical vein (pA(2) 8.65) and in the rabbit jugular vein (pA(2) 9. 07), and as a non-competitive antagonist in the pig coronary artery (pK(B) 10.14). FR 172357 is selective for the kinin B(2) receptor since it does not influence the effects of Lys-des-Arg(9)-bradykinin in the human umbilical vein, in the rabbit aorta, and in the pig renal vein. It is specific because it does not affect the contractions induced by angiotensin II, noradrenaline, 5-hydroxytryptamine, or endothelin-1 in the human umbilical vein. It, however, interacts with the tachykinin NK(1) receptor of the rabbit jugular vein and pig coronary artery. Compared to other bradykinin B(2) receptor antagonists, FR 172357 emerges as a very potent compound, which may represent a choice for experimental (and clinical?) applications.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Rizzi C,Rizzi A,Calò G,Jorizzo G,Agnello G,Mollica G,Inamura N,Regoli Ddoi
10.1016/s0014-2999(99)00711-6keywords:
subject
Has Abstractpub_date
1999-12-10 00:00:00pages
25-31issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(99)00711-6journal_volume
386pub_type
杂志文章abstract：:The structure-activity relationships of 35 novel derivatives of 2-(carboxypropyl)-3-amino-4-methyl-6-phenyl pyridazine (SR 95103) were examined as gamma-aminobutyric acid (GABA) antagonists in the flap preparation of the parasitic nematode, Ascaris suum, using a two-microelectrode current-clamp technique. All but one ...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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更新日期：1983-12-09 00:00:00
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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更新日期：1982-03-12 00:00:00
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更新日期：1998-04-17 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1996-05-15 00:00:00
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更新日期：1999-08-20 00:00:00
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journal_title：European journal of pharmacology
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更新日期：1977-08-01 00:00:00
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pub_type： 杂志文章,评审
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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更新日期：2004-08-16 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：2003-11-28 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1975-02-01 00:00:00
abstract：:Galantamine is a drug in clinical use for the treatment of Alzheimer's disease, but its mechanism(s) of action remains controversial. Here we addressed the question whether galantamine could potentiate neurotransmitter release by inhibiting small conductance Ca2+ -activated K+ channels (KCa2). Galantamine potentiated ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.07.032
更新日期：2006-10-24 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2008.02.086
更新日期：2008-05-13 00:00:00
abstract：:With the aim of studying the mechanism by which peripherally injected interleukin-1 increases the serum levels of insulin in conscious rats, the effects of indomethacin, a cyclooxygenase inhibitor, on interleukin-1-induced hyperinsulinemia were examined using male Wistar rats implanted with intra-atrial cannulas. The ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90089-9
更新日期：1991-01-03 00:00:00
