AZD-5213 / AstraZeneca 
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  • ||||||||||  AZD-5213 / AstraZeneca
    Journal:  Development of [carbonyl-11C]AZ13198083, a novel histamine type-3 receptor radioligand with favorable kinetics. (Pubmed Central) -  May 24, 2019   
    ...To address this, we herein report the development of three novel candidate HR radioligands, namely, [ carbonyl-C]AZ13153556 ([ carbonyl-C]4), [ carbonyl-C]AZD5213([ carbonyl-C]5), and [ carbonyl-C]AZ13198083 ([ carbonyl-C]6), and their subsequent preclinical evaluation in nonhuman primates (NHP)...After pre-treatment or displacement with 5 (0.1 mg/mg), a uni-form low distribution of radioactivity across the NHP brain was observed. Collectively, this work demonstrates that [carbonyl-11C]6 is a promising candidate for H3R imaging in human subjects.