Kumata, Katsushi; Hatori, Akiko; Yamasaki, Tomoteru; Zhang, Yiding; Mori, Wakana; Fujinaga, Masayuki; Xie, Lin; Nengaki, Nobuki; Zhang, Ming-Rong published the article 《Synthesis and evaluation of 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide for PET imaging of the metabotropic glutamate receptor 2 in the rat brain》. Keywords: carbon 11 fluoromethoxyphenyl methylpyridinyl methoxypicolinamide preparation brain mGluR2 PET; In vitro autoradiography; Metabotropic glutamate receptor 2; Positron emission tomography; Radiotracer; Schizophrenia.They researched the compound: Picolinamide( cas:1452-77-3 ).Application In Synthesis of Picolinamide. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1452-77-3) here.
Metabotropic glutamate receptor 2 (mGluR2) has been suggested as a therapeutic target for treating schizophrenia-like symptoms arising from increased glutamate transmission in the human forebrain. However, no reliable positron emission tomog. (PET) radiotracer allowing for in vivo visualization of mGluR2 in the human brain is currently available. In this study, we synthesized 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide ([11C]1) and evaluated its potential as a PET tracer for imaging mGluR2 in the rodent brain. Compound 1, a neg. allosteric modulator (NAM) of mGluR2, showed high in vitro binding affinity (IC50: 26 nM) for mGluR2 overexpressed in human cells. [11C]1 was synthesized by O-[11C]methylation of the phenol precursor 2 with [11C]methyl iodide. After the reaction, HPLC purification and formulation, [11C]1 of 7.4 ± 2.8 GBq (n = 8) was obtained from [11C]carbon dioxide of 22.5 ± 4.8 GBq (n = 8) with >99% radiochem. purity and 70 ± 32 GBq/μmol (n = 8) molar activity at the end of synthesis. In vitro autoradiog. for rat brains showed that [11C]1 binding was heterogeneously distributed in the cerebral cortex, striatum, hippocampus, and cerebellum. This pattern is consistent with the regional distribution pattern of mGluR2 in the rodent brain. The radioactivity was significantly reduced by self- or MNI-137 (a mGluR2 NAM) blocking. Small-animal PET studies indicated a low in vivo specific binding of [11C]1 in the rat brain. The brain uptake was increased in a P-glycoprotein and breast cancer resistant protein double knockout mouse, when compared to a wild-type mouse. While [11C]1 presented limited potential as an in vivo PET tracer for mGluR2, we suggested that it can be used as a lead compound for developing new radiotracers with improved in vivo brain properties.
There is still a lot of research devoted to this compound(SMILES：O=C(N)C1=NC=CC=C1)Application In Synthesis of Picolinamide, and with the development of science, more effects of this compound(1452-77-3) can be discovered.
Reference:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem