scholarly journals Activity of LUF6000 and LUF6096 as positive allosteric modulators (PAMs) for the A3 adenosine receptor (AR) is species‐dependent

2012 ◽  
Vol 26 (S1) ◽  
Author(s):  
Lili Du ◽  
Zhan-Guo Gao ◽  
Jacobus P. D. Veldhoven ◽  
Adriaan P. IJzerman ◽  
Kenneth A. Jacobson ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Allosteric Modulators ◽  
A3 Adenosine Receptor ◽  
Positive Allosteric Modulators

scholarly journals Allosterism vs. Orthosterism: Recent Findings and Future Perspectives on A2B AR Physio-Pathological Implications

2021 ◽  
Vol 12 ◽  
Author(s):  
Elisabetta Barresi ◽  
Claudia Martini ◽  
Federico Da Settimo ◽  
Giovanni Greco ◽  
Sabrina Taliani ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Chronic Obstructive ◽  
Receptor Subtypes ◽  
Allosteric Modulators ◽  
Future Perspectives ◽  
Obstructive Pulmonary Disease ◽  
Protein Receptor ◽  
Inflammatory Processes ◽  
Positive Allosteric Modulators ◽  
Orthosteric Ligands

The development of GPCR (G-coupled protein receptor) allosteric modulators has attracted increasing interest in the last decades. The use of allosteric modulators in therapy offers several advantages with respect to orthosteric ones, as they can fine-tune the tissue responses to the endogenous agonist. Since the discovery of the first A1 adenosine receptor (AR) allosteric modulator in 1990, several efforts have been made to develop more potent molecules as well as allosteric modulators for all adenosine receptor subtypes. There are four subtypes of AR: A1, A2A, A2B, and A3. Positive allosteric modulators of the A1 AR have been proposed for the cure of pain. A3 positive allosteric modulators are thought to be beneficial during inflammatory processes. More recently, A2A and A2B AR allosteric modulators have also been disclosed. The A2B AR displays the lowest affinity for its endogenous ligand adenosine and is mainly activated as a consequence of tissue damage. The A2B AR activation has been found to play a crucial role in chronic obstructive pulmonary disease, in the protection of the heart from ischemic injury, and in the process of bone formation. In this context, allosteric modulators of the A2B AR may represent pharmacological tools useful to develop new therapeutic agents. Herein, we provide an up-to-date highlight of the recent findings and future perspectives in the field of orthosteric and allosteric A2B AR ligands. Furthermore, we compare the use of orthosteric ligands with positive and negative allosteric modulators for the management of different pathological conditions.

scholarly journals Species differences and mechanism of action of A3 adenosine receptor allosteric modulators

2017 ◽  
Vol 14 (1) ◽  
pp. 59-71 ◽  
Author(s):  
Lili Du ◽  
Zhan-Guo Gao ◽  
Silvia Paoletta ◽  
Tina C. Wan ◽  
Elizabeth T. Gizewski ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Adenosine Receptor ◽  
Species Differences ◽  
Allosteric Modulators ◽  
A3 Adenosine Receptor

scholarly journals Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters

2020 ◽  
Vol 36 (1) ◽  
pp. 286-294
Author(s):  
Elisabetta Barresi ◽  
Chiara Giacomelli ◽  
Laura Marchetti ◽  
Emma Baglini ◽  
Silvia Salerno ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Allosteric Modulators ◽  
A2b Adenosine Receptor ◽  
Positive Allosteric Modulators ◽  
Bone Mineralisation

Recent Advances on QSAR-Based Profiling of Agonist and Antagonist A3 Adenosine Receptor Ligands

2013 ◽  
Vol 13 (9) ◽  
pp. 1048-1068 ◽  
Author(s):  
Changliang Deng ◽  
Feng Luan ◽  
Maykel Cruz- Monteagudo ◽  
Fernanda Borges ◽  
M. Natalia D. S. Cordeiro
Keyword(s):  
Adenosine Receptor ◽  
Receptor Ligands ◽  
Recent Advances ◽  
A3 Adenosine Receptor ◽  
Agonist And Antagonist ◽  
Adenosine Receptor Ligands

scholarly journals Effects of alpha 7 positive allosteric modulators in murine inflammatory and chronic neuropathic pain models

2013 ◽  
Vol 65 ◽  
pp. 156-164 ◽  
Author(s):  
Kelen Freitas ◽  
Sudeshna Ghosh ◽  
F. Ivy Carroll ◽  
Aron H. Lichtman ◽  
M. Imad Damaj
Keyword(s):  
Neuropathic Pain ◽  
Allosteric Modulators ◽  
Chronic Neuropathic Pain ◽  
Pain Models ◽  
Positive Allosteric Modulators ◽  
Alpha 7
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