Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha1A‐adrenoceptor subtype in the rat

@article{AlvarezGuerra1999SelectiveBB,
  title={Selective blockade by nicergoline of vascular responses elicited by stimulation of alpha1A‐adrenoceptor subtype in the rat},
  author={Miriam Alvarez-Guerra and Nadine Bertholom and Ricardo P. Garay},
  journal={Fundamental \& Clinical Pharmacology},
  year={1999},
  volume={13}
}
Abstract— The alpha1‐adrenergic blocking activity of nicergoline was re‐examined in rats, with a particular emphasis on alpha1‐adrenoceptor subtypes. In pithed rats, nicergoline and prazosin infused at a single small dose (0.5 μg/kg/min i.v.) produced a substantial and identical shift to the right of the control dose pressor response curve to the specific alpha1‐agonist cirazoline (ED50 = 4.0 ± 0.1, 4.0 ± 0.1 and 0.9 ± 0.01 μg/kg i.v. for nicergoline, prazosin and vehicle respectively). In the… 
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References

SHOWING 1-10 OF 22 REFERENCES
Effects of Nicergoline on the Cardiovascular System of Dogs and Rats
TLDR
Nicergoline appears to decrease blood pressure by blocking α-adrenoceptors and, at least at some doses, by a central inhibition of the sympathetic tone.
Identical antagonist selectivity of central and peripheral alpha 1-adrenoceptors.
TLDR
Testing the relationship between binding affinity for alpha 1 -adrenoceptors and functional antagonism of drug-induced effects mediated by this type of alpha 1-receptor sites for alpha -sympatholytic drugs demonstrates that the binding affinity in vitro of antagonists foralpha 1-adrenOceptors corresponds with their functional antagonisms in vivo and in vitro.
Functional distribution and role of alpha-1 adrenoceptor subtypes in the mesenteric vasculature of the rat.
TLDR
The data suggest that the density or role of alpha-1a adrenoceptors may be greater in resistance vessels than in conduit vessels.
Effect of acidosis on alpha 1- and alpha 2-adrenoceptor-mediated vasoconstrictor responses in isolated arteries.
TLDR
It is concluded that acidosis selectively reduces the vasoconstriction mediated by alpha 2-adrenoceptors in vitro.
Comparison of alpha 1-adrenergic receptor subtypes distinguished by chlorethylclonidine and WB 4101.
TLDR
The results suggest that the C EC-sensitive and -insensitive 125IBE 2254-binding sites are equivalent to those with a low and high affinity for WB 4101, respectively, and the CEC-sensitive binding sites with aLow affinity forWB 4101 are the alpha 1-adrenergic receptors linked to inositol phospholipid hydrolysis.
Effect of ergolines on neurotransmitter systems in the rat brain.
TLDR
Previous results on nicergoline's effects on catecholamine turnover are confirmed and shows that its metabolite MMDL shares its effects on dopamine, and both ergolines were more effective in old than in young rats.
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