scholarly journals MS Binding Assays for Glycine Transporter 2 (GlyT2) Employing Org25543 as Reporter Ligand

ChemMedChem ◽  
2020 ◽  
Author(s):  
Klaus Theodor Wanner ◽  
Thomas M. Ackermann ◽  
Lars Allmendinger ◽  
Georg Höfner

2004 ◽  
Vol 26 (4) ◽  
pp. 518-529 ◽  
Author(s):  
Koji Ohno ◽  
Michael Koroll ◽  
Oussama El Far ◽  
Petra Scholze ◽  
Jesus Gomeza ◽  
...  


2016 ◽  
Vol 99 ◽  
pp. 94-102 ◽  
Author(s):  
Rita I. Aroeira ◽  
Sandra H. Vaz ◽  
Ana M. Sebastião ◽  
Cláudia A. Valente


2019 ◽  
Vol 2019 ◽  
pp. 1-17 ◽  
Author(s):  
Fuhai Bai ◽  
Yongyuan Ma ◽  
Haiyun Guo ◽  
Yuheng Li ◽  
Feifei Xu ◽  
...  

The concept of “acupoint sensitization” refers to the functional status of acupoint switches from silent to active under pathological conditions. In clinic, acupoint sensitization provides important guidance for acupoints selection in different diseases. However, the mechanism behind this phenomenon remains unclear. We generated a model of knee osteoarthritis (KOA) by intra-articular injection of monosodium iodoacetate (MIA) into the left knee of rats. The paw withdrawal mechanical threshold (PWMT) and the total number of mast cells as well as mast cell degranulation rate (MCDR) of acupoint tissue were used to test whether the acupoints were sensitized. The results showed that KOA resulted in a reduced mechanical threshold and elevated total number of mast cell as well as mast cell degranulation rate at bilateral ST35 (Dubi) but not GB37 (Guangming) or nonacupoint area. The acupoint sensitization was accompanied by upregulation of glycine transporter 2 (GlyT2) and reduction of extracellular glycine levels in the bilateral dorsal horns of the spinal cord at L3-5. Selective inhibition of GlyT2 or intrathecal administration of glycine attenuated ST35 acupoint sensitization. The sensitization of bilateral ST35 was blocked after intraspinal GlyT2 short hairpin (sh) RNA (GlyT2-shRNA) microinjection to specifically downregulate GlyT2 expression in the left side (ipsilateral) L3-5 spinal cord dorsal horn before MIA injection. Moreover, electroacupuncture (EA) stimulation at ST35 ameliorated articular pathological lesions and improved KOA-related pain behaviors. GlyT2-shRNA injection reversed EA-induced pain relief but not EA-induced reduction of joint lesions. Overall, this study demonstrated that spinal GlyT2, especially elevated GlyT2 expression in the ipsilateral dorsal horn of the spinal cord, is a crucial mediator of ST35 acupoint sensitization in KOA rats.



2014 ◽  
Vol 290 (4) ◽  
pp. 2150-2165 ◽  
Author(s):  
Esther Arribas-González ◽  
Jaime de Juan-Sanz ◽  
Carmen Aragón ◽  
Beatriz López-Corcuera


IBRO Reports ◽  
2017 ◽  
Vol 3 ◽  
pp. 9-16 ◽  
Author(s):  
Toshikazu Kakizaki ◽  
Hiroyuki Sakagami ◽  
Kenji Sakimura ◽  
Yuchio Yanagawa


2010 ◽  
Vol 110 (2) ◽  
pp. 615-621 ◽  
Author(s):  
Yasunori Haranishi ◽  
Koji Hara ◽  
Tadanori Terada ◽  
Seiya Nakamura ◽  
Takeyoshi Sata


2007 ◽  
Vol 58 ◽  
pp. S91
Author(s):  
Akira Kawata ◽  
Hiroyuki Hayashi ◽  
Hideko Tsuzuki ◽  
Shigehiko Oguri ◽  
Tomohisa Sugiyama ◽  
...  


2018 ◽  
Vol 597 (1) ◽  
pp. 173-191 ◽  
Author(s):  
Swen Hülsmann ◽  
Yoshihiko Oke ◽  
Guillaume Mesuret ◽  
A. Tobias Latal ◽  
Michal G. Fortuna ◽  
...  




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