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- Title
A<sub>1</sub> Adenosine Receptor Partial Agonists and Allosteric Modulators: Advancing Toward the Clinic?
- Authors
Vincenzi, Fabrizio; Pasquini, Silvia; Battistello, Enrica; Merighi, Stefania; Gessi, Stefania; Borea, Pier Andrea; Varani, Katia
- Abstract
Keywords: adenosine; positive allosteric modulators; partial agonists; A1 adenosine receptors; clinical trials EN adenosine positive allosteric modulators partial agonists A1 adenosine receptors clinical trials N.PAG N.PAG 1 12/11/20 20201209 NES 201209 Introduction Adenosine is an endogenous autacoid that exerts a variety of physiological effects by interacting with cell surface G-protein-coupled receptor subtypes, namely A SB 1 sb , A SB 2A sb , A SB 2B sb , and A SB 3 sb adenosine receptors (ARs) ([4]). Through activation of pre- and post-synaptic A SB 1 sb ARs, adenosine plays an important role as an endogenous neuroprotective modulator mainly by inhibiting the excessive release of excitatory neurotransmitters like glutamate, an effect that also underlies the anticonvulsant action of adenosine. The reduction of hyperalgesia by intrathecal injection of T62, consistent with ongoing spinal adenosine release in this model of neuropathic pain, represents the first proof of concept of the potential antinociceptive effect of A SB 1 sb AR positive allosteric modulators. Thank to its capability to increase adenosine affinity for A SB 1 sb AR subtypes, the positive allosteric modulator TRR469, as opposed to CCPA, completely abrogated glutamate-mediated cell injury ([32]).
- Subjects
CYCLOSERINE; ADENOSINES; VENTRICULAR remodeling; TYPE 2 diabetes; CARDIOVASCULAR diseases
- Publication
Frontiers in Pharmacology, 2020, Vol 11, pN.PAG
- ISSN
1663-9812
- Publication type
Article
- DOI
10.3389/fphar.2020.625134