Putative agonists and antagonists at 5-HT1-like receptors

  • Wasyl Feniuk
  • Patrick P. A. Humphrey
Part of the Developments in CardioCardiovascular Pharmacology of 5-Hydroxytryptamine book series (DICM, volume 106)


There is little doubt that the classification of 5-hydroxytryptamine (5-HT) receptors has gone through a major transition over the last few years. Indeed it has been argued [1] that even the recent classification of Bradley and colleagues [2] is now outmoded. This need for change has largely arisen from some major advances from radioligand binding studies. However the acceptability and credibility of any receptor classification will be clearly dependent upon the selectivity and specificity of the agonists and antagonists which are used to define such receptor sites. It is perhaps worth emphasising, even at this early stage, that few selective and specific agonists and no specific antagonists are available in the area of 5-HT1 receptor research. Consequently the classification of 5-HT1 receptors, which has been so markedly influenced by the data generated from ligand binding studies, has on occasion, been met with scepticism [3]. Not withstanding such a criticism, certain new drug tools particularly agonists showing high degrees of selectivity [4] have recently become available. These may help unify a classification which seems in part to be based on ligand binding studies and in part on functional studies [1, 2].


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© Springer Science+Business Media Dordrecht 1990

Authors and Affiliations

  • Wasyl Feniuk
  • Patrick P. A. Humphrey

There are no affiliations available

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