Results 121 to 130 of about 13,221 (154)

Structure optimization of positive allosteric modulators of GABAB receptors led to the unexpected discovery of antagonists/potential negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2020
Positive allosteric modulators (PAMs) of GABAB receptor represent an interesting alternative to receptor agonists such as baclofen, as they act on the receptor in a more physiological way and thus are devoid of the side effects typically exerted by the agonists.
Claudia Mugnaini, Antonella Brizzi, Rafaela Mostallino, Maria Paola Castelli, Federico Corelli   +4 more
openaire   +3 more sources

6-Aryl Isoindolin-1-ones: Novel mGluR2 Negative Allosteric Modulators

ACS Medicinal Chemistry Letters
This highlight presents novel 6-aryl isoindolin-1-one derivatives that developed as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 2 (mGluR2). Chemical synthesis and potency (IC50) data for both mGluR2 and mGluR3 are disclosed.
Yinlong Li, Steven H. Liang
openaire   +2 more sources

Nanobodies as negative allosteric modulators for human calcium sensing receptor

Biochemical and Biophysical Research Communications
Human calcium sensing receptor (CaSR) senses calcium ion concentrations in vivo and is an important class of drug targets. Mutations in the receptor can lead to disorders of calcium homeostasis, including hypercalcemia and hypocalcemia. Here, 127 CaSR-targeted nanobodies were generated from camels, and four nanobodies with inhibitory function were ...
Qianqian Cui, Lu Wang, Haonan Wang, Xiaochen Chen, Li Han, Tengjie Geng, Yongjun Kou, Wenqing Zhang, Mei Dai, Huarui Qiao, Zengchao Sun, Lingyun Li, Zhongyun Lan, Hongxi Xu, Jiaqiang Xu, Yuanyuan Dai, Yong Geng   +16 more
openaire   +2 more sources

mGlu₅negative allosteric modulators: a patent review (2013 - 2016)

Expert Opinion on Therapeutic Patents, 2017
The pursuit of small molecule mGlu5 NAMs as treatments for a variety of psychiatric and neurodegenerative disorders has developed into a mature field. In addition to extensive preclinical studies, multiple compounds have advanced into clinical trials with the most advanced studies occurring in patients with FXS, PD-LID, and MDD.
openaire   +2 more sources

mGlu₅negative allosteric modulators: a patent review (2010 – 2012)

Expert Opinion on Therapeutic Patents, 2013
The design and development of small molecule negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) has been an area of intense interest for over a decade. Potential roles have been established for mGlu5 NAMs in the treatment of diseases such as pain, anxiety, gastroesophageal reflux disease (GERD), Parkinson's ...
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IP562083 a novel mGluR7 negative allosteric modulator

Pharmacological Reports, 2015
Piotr Brański, Grzegorz Burnat, Anna Stankiewicz, Ryszard Bugno, Maria Paluchowska, Katarzyna Kaczorowska, Barbara Chruścicka, Andrzej Bojarski, Andrzej Pilc   +8 more
openaire   +1 more source

Elaboration and Design of α7 nAChR Negative Allosteric Modulators

2015
VCU Theses and ...
openaire   +1 more source

Small Molecules as Negative Allosteric Modulators of Alpha7 nAChRs

2012
VCU Theses and ...
openaire   +1 more source

Bio-Inspired Microwave Modulator for High-Temperature Electromagnetic Protection, Infrared Stealth and Operating Temperature Monitoring

Nano-Micro Letters, 2021
Yuping Duan, Tong-Min Wang
exaly  

β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors

Cell, 2020
Lauren M Slosky, Krisztian Toth, Alexandra Badea   +2 more
exaly