Corpus ID: 29345544

Studies on the physiologic disposition and activity of phenylpropanolamines in the mouse.

  title={Studies on the physiologic disposition and activity of phenylpropanolamines in the mouse.},
  author={M. Levitt and W. R. Cumiskey and L. Shargel},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  volume={2 2},
The metabolism, distribution, uptake, release, and activity of m -aminophenylpropanolamine (MAPP), a nonphenolic amine, was studied in the mouse. Only a single radioactive peak was detected in urine after administration of tritiated MAPP. In distribution studies we found that tritiated MAPP and metaraminol (MA) were concentrated and retained in cardiac tissue compared to liver, spleen, kidney, and lung. Desipramine, cocaine, bretylium, and norepinephrine blocked the uptake of MAPP and MA into… Expand
Effects of dl-norephedrine and its enantiomers on norepinephrine uptake and release in isolated rat caudal artery.
Results indicate that inhibition of NE reuptake may be a component of the mechanism of action of NOR, but that a displacement of NE from neuronal storage sites is not, and that the blockade of NE uptake by NOR is only a minor component of its vasoactive properties. Expand
Effect of phenylpropanolamine and related compounds on beta-adrenoceptor-induced activation of adenylyl cyclase.
It is demonstrated that PPA and its diastereomers do not act directly at beta-adrenoceptors to alter cardiac function and supports the hypothesis that significant agonist activity of beta-phenethylamines at the beta- adrenoceptor requires phenolic/aryl ether substitution on the phenyl-ring. Expand
Formation of α-methylnorepinephrine as a metabolite of metaraminol in guinea pigs
Iprindole pretreatment reduced the concentration of α-methylnorepinephrine in heart and liver of metaraminol-treated rats but did not alter the depletion of norepineleigh in these tissues, raising the possibility that α- methylnore-pinephrine is involved in some of the pharmacological effects of metARaminol in guinea pigs. Expand
Tissue levels of metaraminol and its metabolite, alpha-methylnorepinephrine, in control and 6-hydroxydopamine-pretreated guinea pigs.
The idea that metaraminol and α-methylnorepinephrine are retained in noradrenergic fibers and that this retention is a dominant factor in their rates of disappearance from tissues is supported. Expand
AkrinorTM, a Cafedrine/ Theodrenaline Mixture (20:1), Increases Force of Contraction of Human Atrial Myocardium But Does Not Constrict Internal Mammary Artery In Vitro
AkinorTM increased cardiac contractile force by direct sympathomimetic actions and PDE inhibition, did not constrict A. mammaria interna rings, but shifted the noradrenaline curve rightward from -logEC50 6.18 ±0.08 to 5.23 ± 0.05 M.mam maria rings, compatible with an α-AR antagonistic effect or PDE inhibited. Expand
A review of the physiological bases of the anorexic action of phenylpropanolamine (d,l-norephedrine)
  • P. Wellman
  • Medicine, Psychology
  • Neuroscience & Biobehavioral Reviews
  • 1990
The present review compares the acute anorexic effects of PPA with those of amphetamine in animals and humans, describes the persistent chronic effects of the PPA on feeding as well as differences in anoreXic potency between the norephedrine enantiomers (d-nore phedrine less than 1- norePhedrine) and summarizes the generality of P PA anorexia. Expand
Comparison between phenylpropanolamine and structurally related compounds on gastric transit in the rat
The pharmacological differences between PPA and its structurally related compounds, as determined by their ability to inhibit gastric transit in the rat, are investigated. Expand
Pharmacology and safety of phenylpropanolamine
  • David A. Johnson
  • Medicine
  • 1991
The pharmacology of PPA is reviewed, with an emphasis on how the drug effects smooth muscle tissues, and research pertaining to its toxicity is also reviewed. Expand
Self-administration of phenylpropanolamine (PPA) by rats previously trained to self-administer amphetamine
It is shown that rats with prior exposure to amphetamine will self-administer PPA during the initial portion of a three-hour test, similar to that observed for amphetamine. Expand
Urodynamic and haemodynamic effects of a single oral administration of ephedrine or phenylpropanolamine in continent female dogs.
Urethral function was improved after both ephedrine and PPA, and bladder function also improved during micturition following ephedine, and arterial blood pressures at 4-6 h were compensated by a decreased heart rate over 12 h. Expand