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Selective high-affinity antagonists for the dopamine D₃ receptor (D₃R) are sought for treating substance use disorders. Positron emission tomography (PET) with an effective D₃R radioligand could be a useful tool for the development of such therapeutics by elucidating pharmacological specificity and target engagement in vivo. Currently, a D₃R-selective radioligand does not exist. The D₃R ligand, N -(4-(4-(3-chloro-2-methoxyphenyl)piperazin-1-yl)butyl)-1 H -indole-2-carboxamide (BAK4-51, 1 ), has attractive properties for PET radioligand development, including full antagonist activity, very high D₃R affinity, D₃R selectivity, and moderate lipophilicity. We labeled 1 with the positron-emitter carbon-11 ( t  1/2 = 20.4 min) in the methoxy group for evaluation as a radioligand in animals with PET. However, [ 11 C] 1 was found to be an avid substrate for brain efflux transporters and lacked D₃R-specific signal in rodent and monkey brain in vivo.

molecules/molecules online/molecules annual

[O-methyl-11C]N-(4-(4-(3-Chloro-2-methoxyphenyl)-piperazin-1-yl)butyl)-1H-indole-2-carboxamide ([11C]BAK4-51) Is an Efflux Transporter Substrate and Ineffective for PET Imaging of Brain D3 Receptors in Rodents and Monkey