Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.

A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.

[1]  M. Nader,et al.  Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents. , 2005, Journal of medicinal chemistry.

[2]  P. Seeman.  Targeting the dopamine D2 receptor in schizophrenia , 2006, Expert opinion on therapeutic targets.

[3]  A. Zhang,et al.  Recent advances towards the discovery of dopamine receptor ligands , 2006 .

[4]  P D Leeson,et al.  3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. , 1996, Journal of medicinal chemistry.

[5]  R. Mach,et al.  Progress in developing D3 dopamine receptor ligands as potential therapeutic agents for neurological and neuropsychiatric disorders. , 2003, Current pharmaceutical design.

[6]  Robert H Mach,et al.  Synthesis and characterization of selective dopamine D2 receptor antagonists. , 2006, Bioorganic & medicinal chemistry.

[7]  Patrik Brundin,et al.  Pathogenesis of parkinson's disease: dopamine, vesicles and α-synuclein , 2002, Nature Reviews Neuroscience.

[8]  Erin E. Carlson,et al.  Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor. , 2005, Journal of medicinal chemistry.

[9]  S. Kapur,et al.  Half a century of antipsychotics and still a central role for dopamine D2 receptors , 2003, Progress in Neuro-Psychopharmacology and Biological Psychiatry.

[10]  G. Harriman,et al.  Synthesis of 4-substituted 4-arylpiperidines , 2000 .

[11]  A. Shafiee,et al.  Synthesis of 3‐formylbenzo[b]furan and 1‐methyl‐3,4‐dihydrobenzo[b]‐furo[2,3‐c]pyridine , 1978 .

[12]  B. Roth,et al.  Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors. , 2004, Bioorganic & medicinal chemistry letters.

[13]  J. Swanson,et al.  Dopamine in drug abuse and addiction: results from imaging studies and treatment implications , 2004, Molecular Psychiatry.

[14]  Anne W. Schmidt,et al.  Design, synthesis, and evaluation of metabolism-based analogues of haloperidol incapable of forming MPP+-like species. , 2004, Journal of medicinal chemistry.

[15]  R. Spealman,et al.  Behavioral effects of cocaine and dopaminergic strategies for preclinical medication development , 2002, Psychopharmacology.

[16]  R. Mach,et al.  Characterization of 125I‐IABN, a novel azabicyclononane benzamide selective for D2‐like dopamine receptors , 2000, Synapse.