Arch Int Pharmacodyn Ther
December 1994
We have compared the ability of a new calcium channel-blocking agent, fantofarone (SR 33557), to modify the cardiovascular function in anesthetized dogs, with that of nifedipine. Administration of fantofarone (50 micrograms/kg, i.v.
View Article and Find Full Text PDFIn guinea pigs anaesthetized with sodium pentobarbital, SR 48692, a non peptide neurotensin receptor antagonist blunted the blood pressure increase induced by exogenous neurotensin in a dose dependent manner. Furthermore, in isolated spontaneously beating guinea pig atria, both the tachycardia and inotropic responses induced by neurotensin were potently antagonized. SR 48692 did not show any intrinsic effect in vivo or in vitro.
View Article and Find Full Text PDFSR 47436, 2-n-butyl-3-[(2'-(1H-tetrazol-5-yl)-biphenyl-4-yl) methyl]-1,3-diaza-spiro[4,4]non-1-en-4-one, is a new potent and selective AT1 angiotensin II (AII) receptor antagonist. It competitively inhibited [125I]AII binding to AT1 subtype receptors in rat liver membranes (IC50 = 1.7 nM) and did not interact with AT2 subtypes in rat adrenal cortical membranes.
View Article and Find Full Text PDFSR 46349 (trans-4-[(3Z)3-(2-dimethylaminoethyl)oxyimino-3(2-fluorophe nyl) propen-1-yl] phenol, hemifumarate) is the first member of a newly-developed 5-HT2 antagonist series. SR 46349 potently inhibited serotonin-induced aggregation of rabbit and human platelets (IC50 = 1 and 3.9 nM respectively) but had no effect on the action of other platelet aggregating agents.
View Article and Find Full Text PDFA cardiac phosphodiesterase (PDE) which specifically hydrolyzes cAMP and is inhibited by cyclic GMP has been suggested to be the site of action of new cardiotonic drugs. To investigate the effect of inhibitors, canine cyclic nucleotide PDEs were isolated from left ventricle and from sinoatrial node-enriched tissue, using identical techniques. Four PDE forms could be chromatographically resolved from each tissue, including a peak I PDE (calmodulin-activated phosphodiesterase, CaM-PDE), a peak II PDE (cyclic GMP-stimulated phosphodiesterase, CGS-PDE) and a peak III PDE (specific for cyclic AMP).
View Article and Find Full Text PDFThis article is concerned with a prospective study about the systematical, simultaneous and comparative assay of four biological markers (carcino-embryonic antigen, lactate dehydrogenase, gammaglutamyl transferase and phosphohexose isomerase). This study was conducted in a department of Hematology and oncology on 258 patients. The dosage of each marker separately does not appear to be of diagnostical interest because of a lack of sensibility and specificity.
View Article and Find Full Text PDF