914096-52-9Relevant academic research and scientific papers
1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: A new series of potent and selective dopamine D3 receptor antagonists
Micheli, Fabrizio,Arista, Luca,Bonanomi, Giorgio,Blaney, Frank E.,Braggio, Simone,Capelli, Anna Maria,Checchia, Anna,Damiani, Federica,Di-Fabio, Romano,Fontana, Stefano,Gentile, Gabriella,Griffante, Cristiana,Hamprecht, Dieter,Marchioro, Carla,Mugnaini, Manolo,Piner, Jacqui,Ratti, Emiliangelo,Tedesco, Giovanna,Tarsi, Luca,Terreni, Silvia,Worby, Angela,Ashby Jr., Charles R.,Heidbreder, Christian
, p. 374 - 391 (2010)
The discovery of new highly potent and selective dopamine (DA) D 3 receptor antagonists has recently allowed the characterization of the DA D3 receptor in a range of preclinical animal models of drug addiction. A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes, members of which showed a high affinity and selectivity for the DA D3 receptor and excellent pharmacokinetic profiles, is reported here. Members of a group of derivatives from this series showed good oral bioavailability and brain penetration and very high in vitro affinity and selectivity for the DAD3 receptor, as well as high in vitro potency for antagonism at this receptor. Several members of this series also significantly attenuate the expression of conditioned place preference (CPP) to nicotine and cocaine. 2009 American Chemical Society.
