PMID: 9658586Jul 11, 1998Paper

Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism?

Il Farmaco
C MelchiorreA Leonardi

Abstract

In this article the use of competitive antagonists as tools in receptor characterization and classification is discussed. It is pointed out that caution is required in receptor characterization because negative antagonism (inverse agonism) rather than neutral antagonism could play a relevant role. This implies that antagonists should be evaluated not only with regard to their affinity, but also with regard to their ability to affect the equilibrium between the two receptor states, namely active and inactive states. Since affinity and efficacy of a negative antagonist are system dependent the use of negative antagonists as competitive antagonists in receptor characterization may give rise to false differences in receptor subtypes. Finally, this article summarizes recent developments in the design of new alpha 1-adrenoreceptor antagonists which are structurally related to prazosin or WB 4101.

References

Mar 1, 1995·Trends in Pharmacological Sciences·P Leff
Jan 1, 1995·Trends in Pharmacological Sciences·G MilliganM Lee
Aug 1, 1993·Trends in Pharmacological Sciences·R J LefkowitzT Costa
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May 17, 2000·Pharmaceutica acta Helvetiae·C MelchiorreV Tumiatti

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Citations

May 17, 2000·Pharmaceutica acta Helvetiae·C MelchiorreV Tumiatti
Oct 1, 2006·Expert Opinion on Drug Discovery·Anna MinariniCarlo Melchiorre
May 23, 2018·Bioorganic & Medicinal Chemistry·Gianni SagratiniDario Giardinà
Jan 7, 2005·Journal of Medicinal Chemistry·Alessandra AntonelloCarlo Melchiorre
Apr 4, 2003·Journal of Medicinal Chemistry·Livio BrasiliElena Poggesi

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