Synthesis and in Vivo Validation of [O-Methyl-11C] 2-{4-[4-(7-methoxynaphthalen-1-yl) piperazin-1-yl] butyl}-4-methyl-2 H-[1, 2, 4] triazine-3, 5-dione: A Novel 5-HT1A …

…, H Tamir, J Prabhakaran, NR Simpson…

文献索引：Kumar, J.S. Dileep; Majo, Vattoly J.; Hsiung, Shu-Chi; Millak, Matthew S.; Liu, Kuo-Peing; Tamir, Hadassah; Prabhakaran, Jaya; Simpson, Norman R.; Van Heertum, Ronald L.; Mann, J. John; Parsey, Ramin V. Journal of Medicinal Chemistry, 2006 , vol. 49, # 1 p. 125 - 134

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被引用次数: 48

摘要

Antagonist 5-HT1A PET ligands are available, but an agonist ligand would give more information about signal transduction capacity. Synthesis and in vivo evaluation of [O-methyl- 11C] 2-{4-[4-(7-methoxynaphthalen-1-yl) piperazin-1-yl] butyl}-4-methyl-2 H-[1, 2, 4] triazine- 3, 5-dione (10), a potential high affinity (K i= 1.36 nM) 5-HT1A agonist PET tracer is described. Piperazine 10 is a 5-HT1A agonist with an EC50 comparable to serotonin, ...