Binding characteristics of [3H]guanfacine to rat brain alpha-adrenoceptors. Comparison with [3H]clonidine.

@article{Timmermans1982BindingCO,
  title={Binding characteristics of [3H]guanfacine to rat brain alpha-adrenoceptors. Comparison with [3H]clonidine.},
  author={Pieter B.M.W.M. Timmermans and Andreas Schoop and Pieter A. van Zwieten},
  journal={Biochemical pharmacology},
  year={1982},
  volume={31 6},
  pages={
          899-905
        }
}
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14 Citations
Background Citations
2
Methods Citations
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14 Citations

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Citation Type

Binding characteristics of [3H]quinupramine to rat brain membrane fractions.
TLDR
The specific binding of [3H]quinupramine observed here can be accounted for by both muscarinic cholinergic and serotonin S2 receptors.
Alpha 1-adrenoceptor-mediated vasoconstriction in vivo to enantiomers of SK & F 89748-A.
Quantitative description of α2-adrenergic potency in terms of receptor affinity and intrinsic activity
TLDR
The results support current concepts in receptor theory stating that only when both efficacy and affinity are known, can the activity of the agonist be predicted with reasonable certainty.
1 Pharmacology and Structure-Activity Relationships of α2-Adrenoceptor Antagonists
Characterization of α1-and α2-Adrenergic Receptors
Biochemistry of alpha-2 Adrenergic Receptors
TLDR
Physiologic and pharmacologic studies provide the present basis for the classification of alpha-adrenergic receptors and call for the existence of discrete alpha-1 and alpha-2 adrenergic receptors with the extant possibility of further subdivision among the alpha- 2 adrenergic receptor subtypes.
Animal pharmacology of guanfacine.
  • G. Scholtysik
  • Biology, Medicine
    The American journal of cardiology
  • 1986
Evidence against the involvement of a noradrenergic mechanism in the release by diazepam of novelty-induced hypophagia in rats.
Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in‐vivo α1‐, α2‐ and 5‐HT2‐receptor antagonism and in‐vitro affinity for α1‐, α2‐ and 5‐HT2‐receptors: comparison with ketanserin
TLDR
It is concluded that of the compounds investigated butanserin is the most potent and selective α1‐adrenoceptor antagonist, whereas ritanserin was found to be a potent and select 5‐HT2‐antagonist.
Antihypertensive Activity of 2[(2-Hydroxyphenyl) amino] -4(3H)-quinazolinone
TLDR
Two 2-substituted 4(3H)-quinazolinones were synthesized through an easy one-step synthetic procedure and one contained a guanidino moiety and showed antihypertensive activity following cumulative intravenous administration to anesthetized spontaneously hypertensive rats.
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References

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Binding of an imidazolidine (clonidine), an oxazoloazepin (B-HT 933) and a thiazoloazepin (B-HT 920) to rat brain alpha-adrenoceptors and relation to cardiovascular effects.
Displacement of [3H]clonidine binding by clonidine analogues in membranes from rat cerebral cortex.
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3H-catecholamine binding to α-receptors in rat brain: Enhancement by reserpine
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Distinct α-noradrenergic receptors differentiated by binding and physiological relationships
Characterization of alpha-adrenoceptors participating in the central hypotensive and sedative effects of clonidine using yohimbine, rauwolscine and corynanthine.
Binding characteristics of 3H-prazosin to rat brain α-adrenergic receptors
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TLDR
It is concluded that in the normotensive rat, central alpha 2-adrenoreceptors play a major role in the hypotensive effects of clonidine and related compounds.
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