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Chemical Compound Review:

MOXA 4-[1-hydroxy-2-(propan-2- ylamino)ethyl]-2...

Synonyms: Metiprenalina, Metiprenaline, Methylprenalin, Metiprenalinum, Egyt 402, ...

Magaribuchi, T. et al., Marino, V. et al., Azevedo, I. et al., Hayer-Zillgen, M. et al., Horvath, G. et al., et al.

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Disease relevance of O-Methylisoprenaline

Isoproterenol (125 mumol/kg) and its metabolite, 3-O-methylisoproterenol (125 mumol/kg), caused hypothermia of a lesser intensity [1].

High impact information on O-Methylisoprenaline

Corticosterone and O-methylisoprenaline (1 microM each), but not desipramine, inhibited NE uptake, a profile indicative of NE uptake by EMT, but not OCT-1 [2].
Corticosterone was about 100 fold more potent as inhibitor of hOCT3 than of hOCT1 or hOCT2, and O-methylisoprenaline (OMI) inhibited almost exclusively hOCT3 [3].
A major renal metabolite, 3-O-methylisoproterenol, appeared in the urine and renal vein perfusate and also accumulated in the renal tissue [4].
IC50 values for inhibition of the O-methylisoprenaline-sensitive component of uptake were (in mumol/l): corticosterone (0.3), papaverine (1.1), O-methylisoprenaline (3.0), cimetidine (6.0), (-)noradrenaline (460), and tetraethylammonium (2230) [5].
The addition of uptake2 inhibitors (3-O-methylisoprenaline, 100 mumol/l; normetanephrine, 100 mumol/l; corticosterone, 100 mumol/l) to the perfusion medium significantly reduced the positive chronotropic response to the perfusion with isoprenaline (3 nmol/l) and tropolone (100 mumol/l) [6].

Analytical, diagnostic and therapeutic context of O-Methylisoprenaline

In addition, the accumulation of 3H-isoprenaline (3H-ISO) in the tissue as well as the formation of 3-O-methylisoprenaline (3H-OMI) were determined by liquid scintillation counting [7].

References

3-O-,4-O-diacetylisoproterenol and 3-O-,4-O-dibenzoylisoproterenol: hypothermic effects in mice and the involvement of beta-adrenergic receptors. Dooley, D.J., Hungar, A.A., Nelson, W.L., Bowden, D.M. Eur. J. Pharmacol. (1981) [Pubmed]
Norepinephrine transport by the extraneuronal monoamine transporter in human bronchial arterial smooth muscle cells. Horvath, G., Sutto, Z., Torbati, A., Conner, G.E., Salathe, M., Wanner, A. Am. J. Physiol. Lung Cell Mol. Physiol. (2003) [Pubmed]
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Hayer-Zillgen, M., Brüss, M., Bönisch, H. Br. J. Pharmacol. (2002) [Pubmed]
Isoproterenol excretion and metabolism in the isolated perfused rat kidney. Szefler, S.J., Acara, M. J. Pharmacol. Exp. Ther. (1979) [Pubmed]
Evidence for uptake2-mediated O-methylation of noradrenaline in the human amnion FL cell-line. Marino, V., de la Lande, I.S., Newlyn, M., Parker, D.A. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
Effects of extraneuronal uptake inhibitors on the positive chronotropic response to isoprenaline and on the accumulation of isoprenaline in perfused rat heart after inhibition of catechol-O-methyl transferase. Magaribuchi, T., Hama, T., Kurahashi, K., Fujiwara, M. Naunyn Schmiedebergs Arch. Pharmacol. (1987) [Pubmed]
Uptake, distribution and metabolism of isoprenaline in the dog saphenous vein. Azevedo, I., Osswald, W. Naunyn Schmiedebergs Arch. Pharmacol. (1976) [Pubmed]

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