Wien Klin Wochenschr
August 1996
Thomapyrin has been on the German market as analgesic for the past 50 years. It is the prescription-free preparation with the highest sales there. This is an occasion to survey current state of scientific knowledge concerning combination analgesics with acetyl salicylic acid, paracetamol and caffeine.
View Article and Find Full Text PDFThe actions of urapidil, prazosin, idazoxan, and haloperidol on the turnover of noradrenaline in the hypothalamus and dopamine in the nucleus accumbens of the rat were investigated using changes in the ratios of 3-methoxy-4-hydroxyphenyl-glycol/noradrenaline (MHPG/NA) and 3,4-dihydroxyphenylacetic acid/dopamine (DOPAC/DA), respectively, as measures for drug-induced effects. Urapidil (2.5-30 mg kg-1 i.
View Article and Find Full Text PDFThe present study was undertaken to investigate beta-adrenoceptor-adenylate cyclase coupling in a myocardial ventricular membrane preparation and in isolated renal glomeruli of cellophane perinephritis hypertensive rats. Adenylate cyclase activity and [125I]iodocyanopindolol binding were differentially affected in these preparations. In isolated glomeruli of hypertensive rats a reduced intrinsic activity of isoproterenol was associated with an apparent loss of the guanine nucleotide-sensitive high-affinity state of the beta-adrenoceptors, whereas their absolute number was unchanged when compared with the normotensive control rats.
View Article and Find Full Text PDFWe investigated the effects of sodium 2[5-(4-chlorophenyl)-pentyl]-oxirane-2-carboxylate (POCA) on regional myocardial function and metabolism in anesthetized, thoracotomized dogs subjected to a 53.5% reduction in flow through the circumflex branch of the left coronary artery (LCX). Regional function in the area supplied by the LCX and the left anterior descending coronary artery (LAD) was assessed by means of two pairs of subendocardially inserted ultrasonic transducers.
View Article and Find Full Text PDFVasodilators were characterized on the basis of their first-dose effect on systolic and diastolic blood pressure, heart rate, on the product of heart rate and systolic blood pressure and on plasma renin activity (PRA) in conscious normotensive dogs. The compounds were given orally to the animals and the effects were studied over a period of 4 h. The arterial vasodilators (propyldazine, dihydralazine and labetalol) caused a marked reduction of systolic and diastolic blood pressure with excessive stimulation of the sympathetic nervous system, leading to an increase in myocardial oxygen demand.
View Article and Find Full Text PDFThe magnitude and the persistence of blood pressure reduction by propyldazine (PDZ) was investigated following treatment over a period of 4 days. The experiments were performed on 6 normotensive dogs trained to submit to puncture of the femoral artery and to stand quietly in a special frame over the experimental period of 7 to 8 hours. The first dose effect of orally administered PDZ (0.
View Article and Find Full Text PDFAn investigation is presented of the effects of the acylcarnitine-transferase blocking agent sodium 2[5-(4-chlorophenyl)-pentyl]-oxirane-2-carboxylate (POCA; 20 mg/kg i.v.) on cardiodynamics and myocardial metabolism in normoxic, anesthetized dogs.
View Article and Find Full Text PDFJ Cardiovasc Pharmacol
May 1984
A decrease in isoproterenol-stimulated adenylate cyclase activity has been shown in various tissues of hypertensive rats, a finding often associated with decreased beta-adrenoceptor number. The present study was undertaken to investigate whether adenylate cyclase stimulation by other hormones is similarly affected. Adenylate cyclase activity in cerebral microvessels under control conditions and following stimulation by isoproterenol, prostaglandin E1, and the adenosine analog 5'-(N-ethylcarboxamide)-adenosine (NECA) was significantly diminished in deoxycorticosterone acetate (DOCA)-hypertensive rats as compared with control rats, as was adenylate cyclase stimulation by GTP, fluoride, and forskolin.
View Article and Find Full Text PDFThe magnitude and the persistence of blood pressure reduction by dihydralazine and urapidil were investigated following treatment over a period of 4 days. The experiments were performed on six normotensive dogs, trained to submit to puncture of the femoral artery and to stand quietly in a special frame. The first-dose effects of orally administered dihydralazine (1.
View Article and Find Full Text PDFBasic Res Cardiol
February 1984
Radioactively labeled microspheres were used to investigate the effect of 2',3'-di-O-nitro-5'-(N-ethylcarboxamido)-adenosine (10 micrograms/kg orally), a long-acting adenosine analog, on blood flow through various organs over an experimental period of three hours in conscious dogs. There was a significant increase in myocardial, cerebral, intestinal, and renal cortical blood flow, whereas the flow through skeletal muscle, liver, pancreas, and renal medulla was unaffected. The endocardial/epicardial flow ratio, which was more than one under control conditions, decreased significantly.
View Article and Find Full Text PDFThe responses of plasma renin activity (PRA) and plasma catecholamine levels to molsidomine, administered both intravenously and orally, were investigated in conscious trained dogs. Intravenous administration of molsidomine at increasing dosage up to 0.4 mg/kg with a constant dose interval of 4 hours did not lead to a sustained increase in PRA.
View Article and Find Full Text PDFThe effect of adenosine-5'-N-ethylcarboxamide, (NECA), a long-lasting adenosine derivative with pronounced vasoactivity was investigated on glucagon and insulin release from the in situ isolated blood perfused pancreas in the anesthetized dog: NECA (10(-9) to 10(-5) mol/l) led to a dose-dependent glucagon release. Insulin release was inhibited by NECA at low concentrations, but significantly increased at higher concentrations of the adenosine analogue. Similar effects were observed with infusion of adenosine at 10(-7) and 10(-6) mol/l.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
April 1982
N6-Cyclohexyl[3H]adenosine([3H]CHA,[3H]adenosine, and 5'N-ethylcarboxamide[3H]adenosine ([3H]NECA), potent agonists in adenosine-responsive cellular systems, have been used to identify adenosine binding sites in rat liver plasma membranes. Endogenous ligands were removed by prior dialysis of the membranes. Specific binding of the ligands tested was characterized by rapid forward and reverse kinetics and heterogeneity as indicated by curvilinear Scatchard plots.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
November 1980
The actions of adenosine-5'-ethylcarboxamide (744-96), a long-acting adenosine analogue, on liver, portal and intestinal balances of glucose, lactate and pyruvate and on hepatic and portal blood flow were investigated in 6 chloralose-anaesthetized mongrel dogs. 744-96 led to an increase in portal and hepatic blood flow. Glucose release by the liver and glucose uptake by the non-hepatic splanchnic area (portal balance) were markedly increased by 744-96.
View Article and Find Full Text PDFArzneimittelforschung
December 1979
2-[Bicyclo(2,2,1)heptane-2-endo-3-endo-dicarboximido]-glutarimide (taglutimide, K-2004) proved to be a new sedative-hypnotic drug which did not produce any toxic effects when administered orally to mice even at a very high dosage. Central-nervous depression was demonstrated by a reduction in spontaneous motor activity, potentiation of the central-depressant effect of pentobarbital, antagonism of the central-stimulant effect of amphetamine after oral administration and by narcotic activity after i.v.
View Article and Find Full Text PDFArch Int Pharmacodyn Ther
January 1979
The effect of adenosine-5'-(N-ethylcarboxamide) (744-96), a highly vasoactive adenosine analogue, was investigated on insulin and glucagon release from isolated rat islets of Langerhans. The compound inhibited glucose-induced insulin release in a dose-dependent manner (concentration range 10(-8) to 10(-5 M). No effect of 744-96 was observed on basal or on arginine-induced glucagon release.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
October 1978
An investigation was carried out in conscious dogs concerning the effects of three adenosine derivatives substituted at the 5'-(744-96) or 2'-, 3'-, and 5'-positions (744-98, 744-99), with pronounced and long-lasting coronary dilator activity, on glucagon release. All three compounds (10 microgram/kg i.v.
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