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Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.
CGS 15943A is a potent adenosine receptor antagonist with a novel nonxanthine heterocyclic ring structure. In vitro, CGS 15943A competitively inhibited the 2-chloroadenosine-induced A2Expand
Expression of mRNAs Encoding for Two Different Olfactory Receptors in a Subset of Olfactory Receptor Neurons
Abstract : Evidence has accumulated to support a model for odorant detection in which individual olfactory receptor neurons (ORNs) express one of a large family of G protein‐coupled receptor proteinsExpand
Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines.
A wide variety of 2-substituted aminoadenosines were prepared for comparison with the moderately A2 receptor selective adenosine agonist 2-anilinoadenosine (CV-1808). High selectivity combined withExpand
Characterization of CGS 8515 as a selective 5-lipoxygenase inhibitor using in vitro and in vivo models.
CGS 8515 inhibited 5-hydroxyeicosatetraenoic acid (5-HETE) and leukotriene B4 synthesis in guinea pig leukocytes (IC50 = 0.1 microM). The compound did not appreciably affect cyclooxygenase (sheepExpand
Pharmacological profiles of two new angiotensin‐converting enzyme (ACE) inhibitors: CGS 13945 and CGS 13934
CGS 13945 and CGS 13934 are two nonthiol ACE inhibitors having novel chemical structures. CGS 13945 is a monoester derivative of the free dicarboxylic acid CGS 13934. Based on studies from in vitroExpand
Characterization of CGS 8515 as a selective 5-lipoxygenase (5-LO) inhibitor.
1. CGS 8515 selectively inhibited 5-LO (IC50 = 0.1 microM) with negligible effect on CO, 12-LO, 15-LO and TxS at concentrations up to 100 microM. 2. CGS 8515 selectively inhibited A23187-inducedExpand
Protective effects of CGS 30440, a combined angiotensin-converting enzyme inhibitor and neutral endopeptidase inhibitor, in a model of chronic renal failure.
The purpose of these studies was to compare the effects of CGS 30440 (CGS), a dual angiotensin-converting enzyme inhibitor (ACEI)/neutral endopeptidase inhibitor (NEPI) to benazepril (BZ), an ACEI,Expand
Disposition of pentopril, a new orally active angiotensin-converting enzyme inhibitor, and its active metabolite in rats.
The disposition characteristics of pentopril (the ethyl ester) and its active carboxylic acid metabolite (CGS 13934) were determined in conscious rats after separate intravenous administrations ofExpand
Synthesis and diuretic profile of 3-(3-amino-1,2,4-oxadiazol-5-yl)-5-chloro-2,6-pyrazinediamine, an amiloride-type diuretic.
The synthesis of an analogue of amiloride in which the acylguanidine moiety has been replaced by a 1,2,4-oxadiazol-3-amine unit is described. This substance (3, CGS 4270) exhibited a diuretic profileExpand
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 4. 8-[[(4-Chlorophenyl)sulfonyl]amino]-4-(3-(3-pyridinyl) propyl)octanoic acid and analogs.
The title compound (10a) and its analogs were synthesized and found to possess two activities, the inhibition of the biosynthesis of thromboxane A2 and antagonism of its receptors. The in vitro andExpand