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Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788.
Being a potent and selective ETB receptor antagonist, BQ-788 may be considered as a powerful tool for investigating the role of ET in physiological and pathological processes. Expand
Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor.
Novel potent endothelin (ET) antagonists that are highly potent and selective for the ETA receptor (selective to ET-1) are described, which should provide a powerful tool for exploring the therapeutic uses of ETA antagonists in putativeET-1-related disorders. Expand
J-104129, a novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors.
J-104129 ((R)-4r) may effectively facilitate bronchodilation in the treatment of obstructive airway disease and be a new class of 4-acetamidopiperidine derivatives synthesized and investigated for human muscarinic receptor subtype selectivity. Expand
Biochemical and pharmacological profile of a potent and selective endothelin
We describe the characteristics of a potent and selective endothelin (ET) B-receptor antagonist, BQ-788Expand
Design, synthesis, and discovery of a novel CCR1 antagonist.
This work has identified xanthene-9-carboxamide 1a, the first murine CCR1 receptor antagonist, which may be a useful tool for clarifying the role of C CR1 receptors in murine models of disease. Expand
Role of endothelin ETB receptors in bronchoconstrictor and vasoconstrictor responses in guinea-pigs.
In anesthetized and ventilated guinea-pigs, intravenous injections of endothelin (ET)-1, ET-3, and [Ala1,3,11,15]ET-1, an ETB-selective receptor agonist, induced bronchoconstrictor and transient vasoconstriction responses, whilst the sustained pressor response is mediated by ETA receptors. Expand
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.
A potent M(3) antagonist, 14a (K(i) = 0.31 nM), with novel structural features was identified, which showed high selectivity for M( 3) receptors over the other muscarinic receptor subtypes. Expand
Structure-activity relationships of 2-(benzothiazolylthio)acetamide class of CCR3 selective antagonist.
Derivatization of 1a including incorporation of substituent(s) into each benzene ring of the benzothiazole and piperidine side chain resulted in the identification of potent and selective compounds exhibiting nano-molar binding affinity and greater than 800-fold selectivity for the CCR3 receptor over the C CR1 receptor. Expand
Endothelin-converting enzyme and its in vitro and in vivo inhibition.
The results suggest an essential role of phosphoramidon-sensitive enzyme(s) in the vascular conversion of big ET-1, and the existence of such enzymes also in nonendothelial cells. Expand
Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing
It is demonstrated that compound A has high selectivity for M(3) receptors over M(2) receptors, displays a potent, oral M( 3) antagonistic activity without inhibition of central muscarinic receptors because of low brain penetration, and may have fewer cardiac or CNS side effects than nonselective compounds. Expand