Synthesis and in vitro binding of N-alkyl-2,3- dimethoxy[3.3.1]azabicyclononane benzamides at dopamine D2 and D3 receptors

Biao Yang, Douglas E. Johnston, Robert R. Luedtke, Philip S. Hammond, Robert H. Mach

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Abstract

A series of N-alkyl analogues of 2,3-dimethoxy-N-(9-benzyl)-9- azabicyclo[3.3.1]nonan-3β-yl benzamide was prepared and their affinity for dopamine D2 and D3 receptors was measured in vitro to explore the spatial requirements and relative degree of bulk tolerance in the N-benzyl region of the lead compound. These results suggest a higher degree of bulk tolerance in this binding region of the D2 receptor than in the D3 receptor subtype. These results provide information for the development of pharmacophoric models of the D2 and D3 dopamine receptor subtypes that can be used for the future development of selective antagonists at these two structurally and pharmacologically similar receptor subtypes.

Original languageEnglish
Pages (from-to)115-131
Number of pages17
JournalMedicinal Chemistry Research
Volume8
Issue number3
StatePublished - 1 Jan 1998

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