Affinity and activity profiling of unichiral 8-substituted 1, 4-benzodioxane analogues of WB4101 reveals a potent and selective α 1B-adrenoceptor antagonist

L Fumagalli, M Pallavicini, R Budriesi, M Gobbi…

Index: Fumagalli, Laura; Pallavicini, Marco; Budriesi, Roberta; Gobbi, Marco; Straniero, Valentina; Zagami, Michael; Chiodini, Giuseppe; Bolchi, Cristiano; Chiarini, Alberto; Micucci, Matteo; Valoti, Ermanno European Journal of Medicinal Chemistry, 2012 , vol. 58, p. 184 - 191

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Citation Number: 8

Abstract

Unichiral 8-substituted analogues of 2-[(2-(2, 6-dimethoxyphenoxy) ethyl) aminomethyl]-1, 4- benzodioxane (WB4101) were synthesized and tested for binding affinity at cloned human α1a-, α1b-and α1d-adrenoreceptor (α1a-, α1b-and α1d-AR) and at native rat 5-HT1A receptor and for antagonist affinity at α1A-, α1B-and α1D-AR and at α2A/D-AR. Among the selected 8-substituents, namely fluorine, chlorine, methoxyl and hydroxyl, only the last ...

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