Phenylpropanolamine Constricts Mouse and Human Blood Vessels by Preferentially Activating α2-Adrenoceptors

@article{Flavahan2005PhenylpropanolamineCM,
  title={Phenylpropanolamine Constricts Mouse and Human Blood Vessels by Preferentially Activating $\alpha$2-Adrenoceptors},
  author={Nicholas A Flavahan},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={313},
  pages={432 - 439}
}
  • N. Flavahan
  • Published 1 April 2005
  • Biology, Medicine, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
Phenylpropanolamine (dl-norephedrine) was one of the most widely used therapeutic agents to act on the sympathetic nervous system. Because of concerns regarding incidents of stroke, its use as a nasal decongestant was discontinued. Although considered an α1-adrenergic agonist, the vascular adrenergic pharmacology of phenylpropanolamine was not fully characterized. Unlike most other circulations, the vasculature of the nasal mucosa is highly enriched with constrictor α2-adrenoceptors. Therefore… 

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References

SHOWING 1-10 OF 51 REFERENCES

Differential distribution of postjunctional alpha 2 adrenoceptors in human omental small arteries.

It is suggested that both alpha 1 and alpha 2 adrenoceptors are present in the human omental small arteries, but whereas postjunctionalalpha 2 adrenOceptors appear to be located predominantly in the resistance arteries, postjunctionsal alpha 1 adrenoception appears to be distributed evenly along the arterial tree.

Pharmacological characterization of postjunctional alpha-adrenoceptors in isolated human omental arteries and veins.

The results suggest that in human omental arteries, the postjunctional alpha-adrenoceptors are mainly of the alpha 1-type, even if a small population of alpha 2- adrenoception cannot be excluded.

Postjunctional α-adrenoceptors in human superficial epigastric arteries and veins

The data suggest that the rank order of potency of subtype selective agonists cannot be used for characterization of the α-adrenoceptors in human superficial epigastric arteries and veins.

A knockout approach indicates a minor vasoconstrictor role for vascular alpha1B-adrenoceptors in mouse.

By combining antagonist pharmacology and genetics, this work provides a simplified analysis ofalpha(1)-mediated vasoconstriction, demonstrating that alpha(1D) and alpha(2A) are the major subtypes involved in vasoconStriction, with a minor but definite contribution from alpha( 1B) in every vessel.

Human postjunctional alpha-1 and alpha-2 adrenoceptors: differential distribution in arteries of the limbs.

Experiments were performed in order to characterize the post-junctional alpha adrenoceptors that mediate contraction in arteries of human limbs. Blood vessels were obtained from patients undergoing

Postjunctional α2-adrenoceptors are not present in proximal arterioles of rat intestine.

Results suggest that α2-adrenoceptor-dependent pathways do not influence either resting tone or sympathetic constriction of proximal arterioles in the intestinal submucosa and that luminal shear stress in these vessels significantly decreases with sympathetic constricted.

Sympathetic vascular control of the pig nasal mucosa: adrenoceptor mechanisms in blood flow and volume control

It is concluded that α2‐adrenoceptor mechanisms in the pig nasal mucosa are dominating for the BF, V and LDF responses to exogenous agonists, α1‐Adrenoceptors also seem to be involved in the sympathetic control of BF, LDF.

Regulation of alpha(2)-adrenoceptors in human vascular smooth muscle cells.

It is found that alpha2C-ARs can be dramatically and selectively induced via a p38 MAPK-dependent pathway and altered expression of alpha2-ars may contribute to pathological changes in vascular function.

Postjunctional alpha-adrenoceptors in human superficial epigastric arteries and veins.

A pharmacological characterization of the postjunctional alpha-adrenoceptors in human superficial epigastric artery and vein was performed, using several alpha-adrenoceptor subtype selective
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