The physiological disposition of p-octopamine in man

@article{Hengstmann2004ThePD,
  title={The physiological disposition of p-octopamine in man},
  author={J{\"u}rgen H. Hengstmann and Walter Konen and C. Konen and Michel F Eichelbaum and Hans J. Dengler},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2004},
  volume={283},
  pages={93-106}
}
SummaryAfter oral administration of 3H-p-octopamine (8 mg≙300 μCi) more 3H-activity (93% of the dose) is excreted in the urine within 24 h than after intravenous infusion (2 mg≙300 μCi) over 2.5 h (82% of the dose). This proves that p-octopamine is absorbed quantitatively in man. The absorption proceeds rapidly, peak plasma levels are reached between 30 and 60 min.The only metabolic pathways for p-octopamine are deamination and conjugation. The predominant step is oxidative deamination by… 

Bioavailability of m-octopamine in man related to its metabolism

SummaryThe diminished sympathomimetic pressor activity of monohydroxylated phenylalkylamines after oral administration has been attributed to incomplete enteric absorption. Therefore, urinary

Pharmacokinetics of3H-phenylephrine in man

Metabolism to phenolic conjugates mainly after oral ingestion, and tom-hydroxymandelic acid after i.v. injection, again demonstrated thatm-Hydroxylated amines are predominantly conjugated during the “first-pass” metabolism.

The physiological disposition of etilefrine in man

This metabolic pattern seems to confirm the hypothesis that phenylalkylamines with the hydroxyl group in the m-position of the benzene ring are predominantly conjugated in contrast to p-hydroxylated compounds which are mainly deaminated.

Physiological functions and pharmacological and toxicological effects of p-octopamine

  • S. Stohs
  • Biology
    Drug and chemical toxicology
  • 2015
A need exists for both animal and human safety and efficacy studies involving oral administration of p-octopamine, which is considered to be a CNS stimulant in spite of the fact that it binds poorly to adrenergic receptors.

Analysis of octopamine in human doping control samples.

Urine samples collected after administration of nutritional supplements containing octopamine and/or synephrine as well as urinary concentration of the target compound increased from baseline levels below the lower limit of detection to 142 µg/mL, while urine samples collected before and after therapeutic application did not yield any evidence for elevated renal excretion ofOctopamine.

Cytochrome P450 2D6 and 3A4 enzyme inhibition by amine stimulants in dietary supplements.

Results of this study illustrate that several amine stimulants associated with dietary supplements inhibit CYP2D6 and CYP3A4 in vitro, and these compounds may participate in adverse drug-dietary supplement interactions in vivo.

THE EFFECT OF ENDURANCE EXERCISE TRAINING AND OCTOPAMINE SUPPLEMENTATION ON NLRP1 INFLAMMASOME, PI3K, APOPTOSIS, AND HISTOPATHOLOGICAL CHANGES IN HEART TISSUE OF RATS POISONED WITH DEEP-FRIED OIL

Taking octopamine with aerobic exercise for 4 weeks can control the inflammasome complex (reduction of NLRP1 mRNA) followed by reduction of apoptosis and improvement of cardiac cell regeneration capacity (PI3K protein expression) in the model of nutritional disorders induced by DFO.

The performance and physiological effects of caffeine and octopamine supplementation during endurance cycle exercise

The aim of this thesis was to further characterise the performance and physiological effects of caffeine during prolonged exercise, while elucidating a potential ergogenic role for octopamine.

References

SHOWING 1-10 OF 17 REFERENCES

Bioavailability of m-octopamine in man related to its metabolism

SummaryThe diminished sympathomimetic pressor activity of monohydroxylated phenylalkylamines after oral administration has been attributed to incomplete enteric absorption. Therefore, urinary

Pharmacological action of octopamine with special reference to biochemical conversion to noradrenaline.

In the present experiments it was attempted to correlate sympathomimetic effects of octopamine with the endogenous noradrenaline by means of pharmacological, biochemical and histochemical techniques.

The biosynthesis of octopamine

Using dopamine-β-hydroxylase inhibitors it was found that the half life of octopamine in the rat brain is twice as fast as in the heart, indicating an alternate pathway forOctopamine formation from catecholamines.

SUBCELLULAR DISTRIBUTION OF SOME SYMPATHOMIMETIC AMINES AND THEIR BETA-HYDROXYLATED DERIVATIVES IN THE RAT HEART.

Retention in the microsomal fraction isolated from tissue homogenates parallels retention of the amine after administration of tyramine or guanethidine and norepinephrine, which contains both.

Identification of Octopamine as l-p-Hydroxyphenylethanolamine

So far back as 19401 and again in 1948 2, it had been observed that extracts of posterior salivary glands of Octopus vulgaris possessed intense adrenaline-like actions on blood-pressure and isolated

Supersensitivity and subsensitivity to sympathomimetic amines.

The purpose of a critical appraisal of the various hypotheses concerned with the mechanism of supersensitivity to sympathomimetic amines is not so much to belabor the negative aspect as to emphasize the pressing need for the recognition that this field is much more complicated than is generally realized.

Octopamine: Normal Occurrence in Sympathetic Nerves of Rats

Octopamine has been identified in several organs of normal rats by means of a sensitive enzymatic assay. It is localized within the sympathetic nerve endings.