Homobivalent ligands of the atypical antipsychotic clozapine: design, synthesis, and pharmacological evaluation

…, IT Crosby, E Yuriev, JR Lane, B Capuano

Index: McRobb, Fiona M.; Crosby, Ian T.; Yuriev, Elizabeth; Lane, J. Robert; Capuano, Ben Journal of Medicinal Chemistry, 2012 , vol. 55, # 4 p. 1622 - 1634

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Citation Number: 28

Abstract

To date all typical and atypical antipsychotics target the dopamine D2 receptor. Clozapine represents the best-characterized atypical antipsychotic, although it displays only moderate (submicromolar) affinity for the dopamine D2 receptor. Herein, we present the design, synthesis, and pharmacological evaluation of three series of homobivalent ligands of clozapine, differing in the length and nature of the spacer and the point of attachment to ...