Heterogeneity of biochemical actions among vasodilators.

@article{Greenslade1982HeterogeneityOB,
  title={Heterogeneity of biochemical actions among vasodilators.},
  author={Forrest C. Greenslade and C K Scott and Kristin L. Newquist and K M Krider and Mark Chasin},
  journal={Journal of pharmaceutical sciences},
  year={1982},
  volume={71 1},
  pages={
          94-100
        }
}
Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to beta-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to alpha-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil… 
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References

SHOWING 1-10 OF 15 REFERENCES
Identification of alpha-adrenergic receptors in uterine smooth muscle membranes by [3H]dihydroergocryptine binding.
TLDR
Compounds devoid of significant alpha-adrenergic activity, such as pyrocatechol, 3,4-dihydroxymandelic acid, normetanephrine, and D-lysergic Acid, did not effectively compete for [3H]dihYDroergocryptine binding sites and appear to have characteristics indistinguishable from those of the physiologically active alpha- adrenergic receptors.
Identification of adenylate cyclase-coupled beta-adrenergic receptors in frog erythrocytes with (minus)-[3-H] alprenolol.
(minus)-Alprenolol, a potent, competitive beta-adrenergic antagonist labeled to high specific activity with tritium (17 Ci per mmol), has been used to identify binding sites in frog erythrocyte
The Effects of Flunarizine, a New Calcium Antagonist, on Human Red Blood Cells in vitro
TLDR
Red blood cells can all be explained by the localization of one site of action of flunarizine in the membrane of red blood cells, resulting in an inhibi tion of calcium accumulation and maintenance of normal red blood cell defor mability.
A survey of the effects of isoxsuprine on nonvascular smooth muscle.
TLDR
Results suggested that isoxsuprine has the highest degree of inhibitory activity against uterine and biliary muscle, and that it has the lowest activity against intestinal smooth muscle.
The pharmacologic basis of antihypertensive therapy: The role of vasodilator drugs.
TLDR
In some patients, the therapeutic approach with adrenergicinhibiting drugs is successful, and a hypotensive effect can be achieved with only a moderate disruption of the overall control function of the adrenergic nervous system, however, in others, either the desired vasodepressor effect is not achieved, or it is obtained only at the expense of an unacceptable degree of disruption of adrenergic function such that homeostatic control of the circulation is severely compromised.
Vasodilator drugs in the treatment of hypertension.
TLDR
Treatment with vasodilating drugs specifically reverses the major hemodynamic abnormality of primary hypertension and well-tolerated doses of hydralazine (200 mg/day) can normalize the hemodynamics of most hypertensives.
Stimulus-Secretion Coupling in the Gastrointestinal Tract
TLDR
All readers interested in the more fundamental aspects of one of the principal functions of the alimentary tract will benefit from reading this book.
Metabolic dependence of red cell deformability.
TLDR
It is proposed that the changes seen in the physical properties of ATP-depleted erythrocytes represent ATP-calcium-dependent sol-gel changes occurring at the interface between the membrane and the cell interior, and that thesol-gel balance determines membrane deformability.
Vasodilator therapy--a physiologic approach to the treatment of heart failure.
  • E. Braunwald
  • Medicine
    The New England journal of medicine
  • 1977
Experiments on isolated cardiac tissue have established that myocardial-fiber shortening is dependent on three factors: the preload, which determines the muscle fiber's end-diastolic length; the co...
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