Discovery of LASSBio-772, a 1, 3-benzodioxole N-phenylpiperazine derivative with potent alpha 1A/D-Adrenergic receptor blocking properties

…, F Noël, JB Nascimento, CV Araújo, E Tibiriçá…

Index: Romeiro, Luiz A.S.; Da Silva Ferreira, Marcos; Da Silva, Leandro L.; Castro, Helena C.; Miranda, Ana L.P.; Silva, Claudia L.M.; Noel, Franois; Nascimento, Jessica B.; Araujo, Claudia V.; Tibirica, Eduardo; Barreiro, Eliezer J.; Fraga, Carlos A.M. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 3000 - 3012

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Citation Number: 21

Abstract

Abstract We described herein the discovery of 1-(2-(benzo [d][1, 3] dioxol-6-yl) ethyl)-4-(2- methoxyphenyl) piperazine (LASSBio-772), as a novel potent and selective alpha 1A/1D adrenoceptor (AR) antagonist selected after screening of functionalized N-phenylpiperazine derivatives in phenylephrine-induced vasoconstriction of rabbit aorta rings. The affinity of LASSBio-772 for alpha 1A and alpha 1B AR subtypes was determined through ...