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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Agonist-antagonist interactions at angiotensin receptors: application of a two-state receptor model.

Interactions between agonists and antagonists at angiotensin receptors are characterized by a number of features: variation of antagonist dynamics between apparent simple competition, insurmountable antagonism and, occasionally, augmentation; the tendency for insurmountable antagonism to be saturable; slow recovery of agonist responses following agonist-induced tachyphylaxis; and the ability of competitive antagonists to accelerate recovery from the latter intervention. Some of these phenomena have also been observed in studies of 5-HT2 receptors where they were attributed to the operation of a two-state model with an allosteric site. In this article, Mark Robertson and colleagues propose that the properties of angiotensin AT1 receptors may be explained by a similar model, but without the need to evoke an allosteric site.[1]

References

  1. Agonist-antagonist interactions at angiotensin receptors: application of a two-state receptor model. Robertson, M.J., Dougall, I.G., Harper, D., McKechnie, K.C., Leff, P. Trends Pharmacol. Sci. (1994) [Pubmed]
 
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