These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: [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.
    Author: Liow JS, Morse CL, Lu S, Frankland M, Tye GL, Zoghbi SS, Gladding RL, Shaik AB, Innis RB, Newman AH, Pike VW.
    Journal: Molecules; 2018 Oct 23; 23(11):. PubMed ID: 30360553.
    Abstract:
    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)-1H-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 (t1/2 = 20.4 min) in the methoxy group for evaluation as a radioligand in animals with PET. However, [11C]1 was found to be an avid substrate for brain efflux transporters and lacked D₃R-specific signal in rodent and monkey brain in vivo.
    [Abstract] [Full Text] [Related] [New Search]