Radiosynthesis and Evaluation of a C-11 Radiotracer for Transient Receptor Potential Canonical 5 in the Brain

Clapham DE, Runnels LW, Strübing C (2001) The TRP ion channel family. Nat Rev Neurosci 2:387–396

CAS  Article  Google Scholar 

Riccio A, Li Y, Moon J et al (2009) Essential role for TRPC5 in amygdala function and fear-related behavior. Cell 137:761–772

CAS  Article  Google Scholar 

Sharma S, Hopkins CR (2019) Review of transient receptor potential canonical (TRPC5) Channel modulators and diseases. J Med Chem 62:7589–7602

CAS  Article  Google Scholar 

Wang H, Cheng X, Tian J et al (2020) TRPC channels: structure, function, regulation and recent advances in small molecular probes. Pharmacol Ther 209:107497

CAS  Article  Google Scholar 

Wright DJ, Simmons KJ, Johnson RM, Beech DJ, Muench SP, Bon RS (2020) Human TRPC5 structures reveal interaction of a xanthine-based TRPC1/4/5 inhibitor with a conserved lipid binding site. Commun Biol 3:704

CAS  Article  Google Scholar 

GFB-887 for TRPC5-Rac1-Mediated FSGS. Goldfinch Bio Company website (2022) https://www.goldfinchbio.com/pipeline/gfb-887/. Accessed 28 July 2022

Yu Y, Liang Q, Liu H et al (2019) Development of a carbon-11 PET radiotracer for imaging TRPC5 in the brain. Org Biomol Chem 17:5586–5594

CAS  Article  Google Scholar 

Yu Y, Liang Q, Du L et al (2020) Synthesis and characterization of a specific iodine-125-labeled TRPC5 radioligand. ChemMedChem 15:1854–1860

CAS  Article  Google Scholar 

Chenard B, Gallaschun R (2014) Substituted xanthines and methods of use thereof. Global patent, WO2014143799 A2

Just S, Chenard BL, Ceci A et al (2018) Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice. PLoS One 13:e0191225

Article  Google Scholar 

Song K, Wei M, Guo W et al (2021) Structural basis for human TRPC5 channel inhibition by two distinct inhibitors. Elife 10:e63429

CAS  Article  Google Scholar 

Waterhouse RN (2003) Determination of lipophilicity and its use as a predictor of blood-brain barrier penetration of molecular imaging agents. Mol Imaging Biol 5:376–389

Article  Google Scholar 

Pike VW (2016) Considerations in the development of reversibly binding PET Radioligands for brain imaging. Curr Med Chem 23:1818–1869

CAS  Article  Google Scholar 

Wilson AA, Jin L, Garcia A, DaSilva JN, Houle S (2001) An admonition when measuring the lipophilicity of radiotracers using counting techniques. Appl Radiat Isot 54:203–208

CAS  Article  Google Scholar 

Strübing C, Krapivinsky G, Krapivinsky L, Clapham DE (2001) TRPC1 and TRPC5 form a novel cation channel in mammalian brain. Neuron 29:645–655

Article  Google Scholar 

Chung YH, Sun Ahn H, Kim D et al (2006) Immunohistochemical study on the distribution of TRPC channels in the rat hippocampus. Brain Res 1085:132–137

CAS  Article  Google Scholar 

Riccio A, Medhurst AD, Mattei C et al (2002) mRNA distribution analysis of human TRPC family in CNS and peripheral tissues. Brain Res Mol Brain Res 109:95–104

CAS  Article  Google Scholar 

Fowler MA, Sidiropoulou K, Ozkan ED, Phillips CW, Cooper DC (2007) Corticolimbic expression of TRPC4 and TRPC5 channels in the rodent brain. PLoS One 2:e573

Article  Google Scholar 

Zhang L, Villalobos A, Beck EM et al (2013) Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand. J Med Chem 56:4568–4579

CAS  Article  Google Scholar 

Jeffries B, Wang Z, Graton J et al (2018) Reducing the lipophilicity of perfluoroalkyl groups by CF(2)-F/CF(2)-Me or CF(3)/CH(3) Exchange. J Med Chem 61:10602–10618

CAS  Article  Google Scholar 

Shultz MD (2013) Setting expectations in molecular optimizations: strengths and limitations of commonly used composite parameters. Bioorg Med Chem Lett 23:5980–5991

CAS  Article  Google Scholar 

Phelan KD, Shwe UT, Abramowitz J et al (2013) Canonical transient receptor channel 5 (TRPC5) and TRPC1/4 contribute to seizure and excitotoxicity by distinct cellular mechanisms. Mol Pharmacol 83:429–438

CAS  Article  Google Scholar 

Alawi KM, Russell FA, Aubdool AA et al (2017) Transient receptor potential canonical 5 (TRPC5) protects against pain and vascular inflammation in arthritis and joint inflammation. Ann Rheum Dis 76:252–260

CAS  Article  Google Scholar 

留言 (0)

沒有登入
gif