Inhibitory effect of noradrenaline uptake inhibitors on contractions of rat aortic smooth muscle

  title={Inhibitory effect of noradrenaline uptake inhibitors on contractions of rat aortic smooth muscle},
  author={Y. Huang},
  journal={British Journal of Pharmacology},
  • Y. Huang
  • Published 1 February 1996
  • Biology, Chemistry, Medicine
  • British Journal of Pharmacology
1 The effects of noradrenaline (NA) uptake inhibitors on contractions induced by NA, high K+, and 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA) in rat isolated aorta were investigated. 2 Protriptyline (0.3 μm) and amitriptyline (0.3 μm) produced an approximately parallel shift to the right in the dose‐response curve to NA. Protriptyline (>0.3 μm), amitriptyline (>0.3 μm) and xylamine (0.01‐1 μm) significantly reduced the maximal contractile response to NA. The IC50 values for inhibition of the… 
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Amitriptyline, fluoxetine and tranylcypromine relax rat aorta in vitro and partially delay vascular smooth muscle reactions to adrenergic agonists and can lead to sustained hypotension episodes despite administration of sympathomimetic drugs.
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The signaling of amitriptyline-induced inhibitory effect on electrical field stimulation response in colon smooth muscle
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Serotonin reuptake inhibitor fluoxetine decreases arteriolar myogenic tone by reducing smooth muscle [Ca2+]i.
Fluoxetine reduces [Ca2+]i and tone of arteriolar smooth muscle, likely by interfering with Ca2+ entry, and it is speculated that the "calcium antagonist" effect of fluxetine may be an additional element in the therapeutic actions of this drug.
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At least three subtypes of functional α1‐adrenoceptors have been demonstrated in these studies and it is shown that contractions to exogenous noradrenaline or phenylephrine in rat vas deferens, spleen and aorta are mediated by non‐α1A, non‐ α1B‐ad RenoceptORS, due to the high potency of the α1A‐selective antagonists and sensitivity to CEC.
Studies on the mechanism of the inhibitory effect of desipramine (DMI) on vascular smooth muscle contraction.
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  • Biology, Medicine
    The Journal of pharmacology and experimental therapeutics
  • 1970
The findings suggest that DMI exerted its inhibitory action at a site along the "excitation-contraction coupling" pathway which was common to adrenergic and nonadrenergic stimulants.
Differential effects of putative protein kinase C inhibitors on contraction of rat aortic smooth muscle.
It is suggested that staurosporine and H-7, which are known to act on the catalytic domain of PKC carrying high degree of sequence homology with other protein kinases, are relatively nonselective for PKC.
The postsynaptic effects of antidepressant drugs in the rat anococcygeus muscle
The ability of tricyclic, but not atypical agents, to increase the concentration of noradrenaline bound to postsynaptic α‐adrenoceptors may be severely limited by the antagonistic effect these agents have at this receptor.
12-Deoxyphorbol 13-isobutyrate contracts isolated rat thoracic arteries.
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Correlation between phosphatidylinositol labeling and contraction in rabbit aorta: effect of alpha-1 adrenergic activation.
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Inhibition of noradrenaline uptake by drugs
  • L. Iversen
  • Biology, Chemistry
    Advances in drug research
  • 1965
The present study was undertaken as a quantitative investigation of the potencies of cocaine, reserpine, guanethidine, imipramine, chlorpromazine and the adrenergic blocking agents dichloroisoprenaline, ergotamine and phenoxybenzamine as inhibitors of noradrenaline uptake.
It is concluded that DMI acts on the heart by releasing norepinephrine and producing specific supersensitivity to this catecholamine on its cardiac sites of action and antagonizes several pharmacological properties of guanethidine.