Adenosine a3 receptor agonists. Medical search. Frequent questions

Valsartan is an angiotensin II type 1 receptor antagonist indicated in the treatment of hypertension and mild to moderate heart failure of ischamatic or cardiomyopatheic origin. (iajpr.com)
Novel fluorescent antagonist as a molecular probe in A3 adenosine receptor binding assays using flow cytometry. (units.it)
We report a new fluorophore-conjugated human (h) A3AR antagonist for application to cell-based assays in ligand discovery and for receptor imaging. (units.it)
Responses to the previously studied non-selective adenosine-receptor (AR) agonist adenosine, the A3-selective agonist Cl-IB-MECA and the A3-selective antagonist MRS 1191 were all enhanced to varying degrees, in time and magnitude, by corneal impalement. (edu.hk)
Following our report that A3 adenosine receptor (AR) antagonist 1 exhibited a polypharmacological profile as a dual modulator of peroxisome proliferator-activated receptor (PPAR)γ/δ, we discovered a new template, 1′-homologated adenosine analogues 4a-4t, as dual PPARγ/δmodulators without AR binding. (ewha.ac.kr)
One cryoEM and over 50 high-resolution X-ray crystallographic structures are available for antagonist- or agonist-bound A 2A AR and for its ternary complex with an agonist and an engineered G protein, making this receptor an excellent model system for investigating GPCR structural dynamics. (nature.com)
DR=EC 50 with the addition of various concentrations of receptor antagonist)/EC 50 without the addition of a receptor antagonist. (avma.org)
Remarkably, the PTX-sensitive beta(2)-AR inotropic effect was inhibited by the A(1) adenosine receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine and ecto-5'-phosphodiesterase inhibitor alpha,beta-methyleneadenosine 5'-diphosphate sodium salt, indicating that beta(2)-AR coupling to G(i) is indirect and dependent on A(1) receptor activation. (unifesp.br)

N6-2-(4-Amino-3-[125I]iodophenyl)ethyladenosine, a high affinity A1AR agonist, has served as the only radioligand available for study of the A3AR. (aspetjournals.org)
Blocking ADK activity in the spinal cord provided greater than 90% attenuation of OIH and antinociceptive tolerance through A3 adenosine receptor (A3AR) signaling. (unime.it)
Supplementing adenosine signaling with selective A3AR agonists blocked OIH and antinociceptive tolerance in rodents of both sexes. (unime.it)
These findings suggest A3AR-dependent adenosine signaling is compromised during sustained morphine to allow the development ofmorphine-induced adverse effects. (unime.it)
These findings raise the intriguing possibility that A3AR agonists may be useful adjunct to opioids to manage their unwanted effects. (unime.it)
We report that in rodents, these adverse effects are due to reduced adenosine signaling at the A3AR, resulting in NOD-like receptor pyrin domain-containing 3-interleukin-1β neuroinflammation in spinal cord. (unime.it)
These effects are attenuated by A3AR agonists, suggesting that A3AR may be a target for therapeutic intervention with selective A3AR agonist as opioid adjuncts. (unime.it)
We recently reported that activation of the Gi/Gq-coupled A3 adenosine receptor (A3AR) with selective A3AR agonists (i.e. (cancer8.info)
Our results unravel a mechanistic link into biomolecular Bibf1120 (Vargatef) signaling pathways employed by A3AR activation in neuropathic pain while providing the foundation to consider use of A3AR agonists as therapeutic brokers in CIPN patients. (cancer8.info)
Further binding analysis of MRS5549 suggested multiple agonist binding states of the A3AR. (units.it)
The A3 adenosine receptor (A3AR) is attributed with multiple beneficial actions in ischemic-reperfused myocardium, including modulation of oncotic and apoptotic cell death and enhancement of contractile function. (edu.au)
Available evidence indicates that this receptor sub-type is minimally activated by endogenous adenosine during ischemia (A3AR antagonists exerting no effects on ischemic outcome), and is thus amenable to activation with exogenous agonists. (edu.au)
Protected phenotypes arise with both pre- and post-ischemic treatment with A3AR agonists, and transient A3AR agonism also triggers early and delayed preconditioned states. (edu.au)
Nonetheless, A3ARs may be more promising as therapeutic "anti-ischemic" targets compared with other adenosine receptor subtypes, since A3AR agonists elicit fewer and less significant side-effects. (edu.au)

the A2 receptor antagonists 8-(p-sulfophenyl)theophylline, 3,7-dimethyl-1-(2-propynyl)xanthine, 1,3,7-trimethyl-8-(3-chlorostyryl)xanthine, and 3-propylxanthine, but not A1 and A3 receptor antagonists, decreased the suppressive effect of HS, indicating that HS suppresses neutrophils via A2 receptor activation. (escholarship.org)
Antagonists of P2 receptors counteracted the enhancing effects of ATP, suggesting that HS costimulates neutrophils by means of P2 receptor activation. (escholarship.org)
Ki values of known AR antagonists in inhibition of MRS5449 binding in whole cell FCM were consistent with radioligand binding in membranes, but agonist binding was 5-20 fold weaker than obtained with agonist radioligand [125I]I-AB-MECA. (units.it)
The role of adenosine and the adenosine A1, A3, A2A and A2B receptors was studied by using adenosine deaminase and the selective antagonists DPCPX (1 μM), MRS 1191(1 μM), ZM241385 (1 μM) and MRS1754 (1 μM). (sun.ac.za)
The appropriate selective agonists/antagonists for purinergic receptors as well as the respective enzyme inhibitors may profoundly interfere with microglial functions and reconstitute the homeostasis of the CNS disturbed by neuroinflammation. (preprints.org)
Values for the control samples were obtained without addition of receptor antagonists. (avma.org)

Here, we report that HS dose-dependently releases adenosine 5'-triphosphate (ATP) from neutrophils and that extracellular ATP is rapidly converted to adenosine or activates p38 MAPK and enhances N-formyl-methionyl-lencyl-phenylalanine-induced superoxide formation. (escholarship.org)
Conversely, inhibition of PVA neuronal activity using DREADDs (designer receptors exclusively activated by designer drugs) or inactivation of PVA extracellular signal-regulated kinase at the critical time window blunted mechanical hyperalgesia in chronic pain models. (iasp-pain.org)
Extracellular adenosine mediates a multitude of biological effects, including wakefulness, antiarrythmia, bronchoconstriction and response to ischemia and oxidative stress. (co-bioer.com)
Extracellular Adenosine Stimulates Vacuolar ATPase-Dependent Proton Secretion in Medullary Intercalated Cells. (harvard.edu)
Assuming that the increment of intracellular cAMP is followed by cAMP efflux and extracellular generation of adenosine, the contribution of the extracellular cAMP-adenosine pathway on the beta(2)-AR inotropic response was also addressed. (unifesp.br)
the involvement of the extracellular cAMP-adenosine pathway in beta(2)-AR signaling would provide a negative feedback loop that may limit stimulatory G protein-coupled receptor positive inotropism and potential deleterious effects of excessive contractile response. (unifesp.br)

CP-532,903 is a selective adenosine A3 subtype receptor agonist. (wikipedia.org)
Hemodynamic effects of histamine release elicited by the selective adenosine A 3 receptor agonist 2-Cl-IB-MECA in conscious rats. (rndsystems.com)
A fluorescent adenosine receptor ligand derived from NECA, non-selective adenosine agonist. (hellobio.com)

An adenosine A3 receptor agonist inhibits DSS-induced colitis in mice through modulation of the NF-κB signaling pathway. (rndsystems.com)
Adenosine deaminase treatment abolished the suppressive effect of HS, indicating that HS inhibits neutrophils through adenosine generation. (escholarship.org)
The nuclear factor kappa B (NF-κB) system promotes the release of proinflammatory mediators, whereas the glucocorticoid-glucocorticoid receptor alpha (G-GRα) complex inhibits inflammation [ 5 ]. (springeropen.com)

2-Cl-IB-MECA is a high affinity and extremely selective A 3 adenosine receptor agonist (K i = 0.33 nM). (rndsystems.com)
125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. (aspetjournals.org)
a3 adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity. (longdom.org)
Probe dependence of allosteric enhancers on the binding affinity of adenosine A1 -receptor agonists at rat and human A1 -receptors measured using NanoBRET. (hellobio.com)
2-Cl derivatives exhibited dual receptor-binding affinity to PPARγ/δ, which was absent for the corresponding 2-H derivatives. (ewha.ac.kr)
Among the adenosine derivatives, some 5'-chloro-5'-deoxy-N6-cycloalkyl(bicycloalkyl)- analogues were found A1 agonists with high affinity and selectivity for rat A1 AR or partial agonists for this AR subtype. (unicam.it)
On the base of these findings, in the second part of my work, a series of 5'-substituted derivatives of potent and selective A1 AR agonists were synthesized and tested for affinity and selectivity at different model of adenosine receptor subtypes. (unicam.it)
In particular, a series of 5'-carbamoyl or 5'-thionocarbamoyl derivatives of 2'-Me-CPA, 2'-Me-CCPA, N6-[(R)-3-tetrahydrofuranyl]adenosine and 2-chloro analogue were synthesized and evaluated for binding affinity at ARs from bovine, porcine and human species. (unicam.it)
Moreover, a series of 5'-chloro-5'-deoxy-N6-cycloalkyl(bicycloalkyl)-substituted adenosine and 2'-C-methyladenosine derivatives and 2-chloro analogues were synthesized and evaluated for affinity and efficacy at all cloned human AR subtypes. (unicam.it)
In this study, two adenosine derivatives displayed the highest affinity in the subnanomolar range and relevant selectivity for hA1 vs the other human receptor subtypes. (unicam.it)

Basal adenosine modulates the functional properties of AMPA receptors in mouse hippocampal neurons through the activation of A1R A2AR and A3R. (rndsystems.com)
At the same time, adenosine modulates striatal DA release by stimulating glutamate release at adenosine receptors in the striatum , which increases dopamine levels. (adxs.org)
The physiological agonist adenosine modulates a variety of functions through four receptor subtypes classified as A1, A2A, A2B and A3. (unicam.it)

Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. (rndsystems.com)

In this respect, it has been reported that A1 partial agonist may be therapeutically advantageous. (unicam.it)

In the search for potent and selective A1 AR agonists we have previously investigated a series of 2'-C-methylribofuranosyl analogues of selective A1 AR agonists and 2-chloro- 2'-C-methyl-N6-cyclopentyl-adenosine (2'-Me-CCPA) emerged as a potent and highly selective full agonist at rat, bovine and human A1 vs A2A, A2B and A3 ARs. (unicam.it)

Enhancing endogenous adenosine A2A receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function. (harvard.edu)

Metabotropic purinergic receptors in lipid membrane microdomains. (hellobio.com)

Allosteric Modulation of Adenosine A2A Receptors as a New Therapeutic Avenue. (harvard.edu)

Activation of the A(3) adenosine receptor suppresses superoxide production and chemotaxis of mouse bone marrow neutrophils. (wikipedia.org)
In contrast, adenosine suppresses superoxide formation. (escholarship.org)

2. Possible pharmacological mechanisms of adenosine receptor and cordycepin from Cordyceps militaris in the prevention and treatment of COVID-19 pneumonia. (antivirii.com)

The complex pharmacology of G-protein-coupled receptors (GPCRs) is defined by their multi-state conformational dynamics. (nature.com)

CD39 limits P2X7 receptor inflammatory signaling and attenuates sepsis-induced liver injury. (harvard.edu)

The physiological role of the A3 adenosine receptor (AR) was explored in cardiac ischaemia, inflammatory diseases and cancer. (units.it)

exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development. (longdom.org)

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. (rndsystems.com)
We have previously shown that hypertonic stress (HS) can suppress chemoattractant-induced neutrophil responses via cyclic adenosine monophosphate and enhance these responses through p38 mitogen-activated protein kinase (MAPK) activation. (escholarship.org)
We conclude that hypertonic stress regulates neutrophil function via a single molecule (ATP) and its metabolite (adenosine), using positive- and negative-feedback mechanisms through the activation of P2 and A2 receptors, respectively. (escholarship.org)
Inhibition of LPS-induced neutrophil ROS production by various adenosine receptor agonists. (avma.org)

Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. (rndsystems.com)
A(3)AR activation with a specific agonist deregulates the NF-kappaB signaling pathway in inflammatory cells and initiates immunomodulatory effects. (drugbank.com)

Displays 2500- and 1400-fold selectivity over A 1 and A 2A receptors respectively. (rndsystems.com)
Exhibits high selectivity over the Na + -independent adenosine transporter. (rndsystems.com)
2-Substitution of N 6 -benzyladenosine-5'-uronamides enhances selectivity for A 3 adenosine receptors. (rndsystems.com)

A3 receptor agonists and/or agonists may have important clinical value in the treatment of asthma and inflammation. (co-bioer.com)

Inhibition of erythroblast growth and fetal hemoglobin production by ribofuranose-substituted adenosine derivatives. (rndsystems.com)
MRS5449 antagonized hA3AR agonist-induced inhibition of cyclic AMP accumulation in a concentration-dependent manner (KB = 4.8 nM). (units.it)

The ribose recognition domain of adenosine derivatives appears to be of considerable importance not only for cytotoxic activity, but also for agonistic activity at adenosine receptors (ARs). (unicam.it)
Pharmacophoric modification of the formyl group provided a number of new fused-b-carboline derivatives which have been investigated for his or her k-opioid receptor (KOR) agonistic exercise. (topigen.com)

Therefore, smFRET has been limited to studies of inter-receptor interactions in cellular membranes and receptors in detergent environments. (nature.com)

TDI decreased the stimulation of lymphocyte c-Adenosine-monophosphate (cAMP) concentrations by the receptor agonists isoproterenol and prostaglandin-E1. (cdc.gov)
Hearts were preconditioned with 5 min isoproterenol 0.1 μM ( 1/ 2-AR agonist), or formoterol 1 nM ( 2-AR agonist) or BRL 37344 1 μM ( 3-AR agonist) followed by 5 min reperfusion. (sun.ac.za)

N6-[(R)-phenylisopropyl]adenosine = NECA was observed, and in RBL-2H3 cells (-)-N6-[(R)-phenylisopropyl]adenosine and NECA were equipotent. (aspetjournals.org)

Adenosine receptors are closely associated with dopamine receptors and form heteromer s with them. (adxs.org)

Pulsed electromagnetic fields increased the anti-inflammatory effect of A 2 A and A 3 adenosine receptors in human T/C-28a2 chondrocytes and hFOB 1.19 osteoblasts. (rndsystems.com)
The G i -coupled A 3 adenosine receptor (A 3 AR) mediates anti-inflammatory, anticancer and anti-ischemic protective effects. (uconn.edu)
The present review summarizes preclinical and clinical human studies demonstrating that A 3 AR agonists induce specific anti-inflammatory and anticancer effects via a molecular mechanism that entails modulation of the Wnt and the NF-κB signal transduction pathways. (uconn.edu)
A review through the activation of adenosine receptors A1, A2A, A2B, and A3, adenosine plays an important role in the pathological process of acute lung injury, such as anti-inflammatory, inhibiting cytokine storm, protecting organ damage, and repairing and remodeling tissues. (antivirii.com)

PPARγ/δdual modulators functioning as both PPARγpartial agonists and PPARδantagonists promoted adiponectin production, suggesting their therapeutic potential against hypoadiponectinemia-associated cancer and metabolic diseases. (ewha.ac.kr)

Moreover, she identified a new therapeutic target (adenosine A3 receptor, A3R) whose activation with a selective agonist demonstrated to improve the survival of RGC contributing to the maintenance of the RGC function, in a preclinical model of glaucoma. (iapb.org)
The receptor is overexpressed in inflammatory and cancer cells, while low expression is found in normal cells, rendering the A 3 AR as a potential therapeutic target. (uconn.edu)

The latest IL-17 and IL-23 inhibitors include bimekizumab, netakimab and mirikizumab as well as oral small molecules, such as deucravacitinib, a tyrosine kinase 2 selective inhibitor, and piclidenoson, an agonist of the Gi protein-associated A3 adenosine receptor. (univr.it)
Here, we performed smFRET experiments on functionally active human A 2A adenosine receptor (A 2A AR) molecules embedded in freely diffusing lipid nanodiscs to study their intramolecular conformational dynamics. (nature.com)
These three phenomena indicate that receptors are highly dynamic molecules and sample several active and inactive states stochastically (for review, see refs. (nature.com)
In the nonstressed physiologic state, adequate oxygen and glucose are delivered intracellularly to mitochondria that generate 36 adenosine triphosphate (ATP) molecules per glucose molecule via aerobic metabolism and the Krebs cycle. (medscape.com)

Results are reported as the percentage of radioligand binding without addition of an agonist. (avma.org)

a component of adenosine triphosphate and adenosine diphosphate. (adxs.org)

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (harvard.edu)

Adenosine receptors and membrane microdomains. (hellobio.com)

Release of endogenous catecholamines and activation of the beta-adrenergic receptors (b-AR) have also been shown to be involved in ischaemic preconditioning. (sun.ac.za)
Activation of the human melanocortin 1 receptor (hMC1R) expressed on melanocytes by α-melanocortin (α-MSH) performs a central function in regulating human pigmentation, and lowering the genotoxicity of ultraviolet radiation (UV) by activating DNA restore and antioxidant defenses. (topigen.com)
beta(2)-Adrenoceptor (beta(2)-AR) agonists increase skeletal muscle contractile force via activation of G(s) protein/adenylyl cyclases (AC) and increased generation of cAMP. (unifesp.br)

Cordycepin is also an activator of adenosine receptors. (antivirii.com)
P-selectin, soluble endothelial protein C receptor, soluble thrombomodulin, plasminogen activator inhibitor 1, ADAMTS-13, von Willebrand factor, tissue factor, soluble intercellular adhesion molecule 1, and vascular cell adhesion molecule 1 were more elevated in LF patients than in controls. (cdc.gov)
Endothelial protein C receptor, thrombomodulin, intercellular adhesion molecule 1, plasminogen activator inhibitor 1, D-dimer, and hepatocyte growth factor were higher in fatal than nonfatal LF cases. (cdc.gov)
the effects of clenbuterol/fenoterol (beta(2)-AR agonists), forskolin (AC activator), cAMP/8-bromo-cAMP, and adenosine were evaluated on isometric contractility of mouse diaphragm muscle induced by supramaximal direct electrical stimulation (0.1 Hz, 2 ms duration). (unifesp.br)

The A3 adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP-sensitive potassium channel. (wikipedia.org)
Recent animal model studies have shown that A3 receptors play important roles in brain ischemia, immunosuppresion, and bronchospasm. (co-bioer.com)

1. ACE2 (angiotensin-converting enzyme 2), COVID-19, and ACE inhibitor and Ang II (angiotensin II) receptor blocker use during the pandemic: The pediatric perspective. (antivirii.com)
the late descending phase of the beta(2)-AR agonist inotropic effect was mimicked by either cAMP or adenosine and abolished by preincubation of diaphragm with pertussis toxin (PTX) (G(i) signaling inhibitor) or the organic anion transporter inhibitor probenecid, indicating a delayed coupling of beta(2)-AR to G(i) protein which depends on cAMP efflux. (unifesp.br)

Mice lacking A3 receptors display reduced mast cell degranulation and bronchoconstriction in response to adenosine. (co-bioer.com)

In the central nervous system, the purine nucleoside adenosine has been implicated in beneficial and detrimental actions ofmorphine, but the extent of their interaction remains poorly understood. (unime.it)

CF-101 is an adenoside A3 agonist for the treatment of a variety of autoimmune-inflammatory disorders, particularly rhematoid arthritis. (drugbank.com)
Small molecule drugs, A 3 AR-selective agonists, are currently in advanced clinical trials for the treatment of hepatocellular carcinoma, autoimmune inflammatory diseases, such as rheumatoid arthritis, psoriasis, and dry eye disease, and other conditions. (nih.gov)

Coregulator complexes that repress transcription are recruited to unliganded receptors or receptors bound to inverse agonists generally. (biodiversityhotspot.org)

Fluorescent adenosine receptor agonist (pEC 50 values are 8.57, 8.47, 6.76 and 5.69 for A 3 , A 1 , A 2A and A 2B respectively). (hellobio.com)

The protective effects of this phenomenon have been demonstrated to be mediated by release of autocoids such as adenosine, opioids and bradykinin. (sun.ac.za)

A family of four G-protein coupled adrenoceptors, A1, A2A, A2B and A3, is responsible for these effects. (co-bioer.com)
Nuclear receptors are transcription factors that regulate gene expression through the ligand-controlled recruitment of the different group of protein referred to as coregulators. (biodiversityhotspot.org)
Subsequently, it is becoming apparent that coregulator protein play a central function in mediating transcriptional legislation by nuclear receptors. (biodiversityhotspot.org)

Attenuation of adverse effects of noise induced hearing loss on adult neurogenesis and memory in rats by intervention with Adenosine A2A receptor agonist. (harvard.edu)
however the clinical application of A1 full agonists is hampered by several side effects. (unicam.it)
Concentration of cAMP in equine neutrophils induced by 5 adenosine A 2A receptor agonists (A) and effects of ZM241385 and MRS1706 on ATL313-induced accumulation of cAMP (B). Each point represents the mean ± SEM of 3 replicates. (avma.org)

A3, which couples to Gi/o, is expressed in a wide range of human tissues, but most predominantly in the lung and liver. (co-bioer.com)

Here, we demonstrate that morphineinduced OIH and antinociceptive tolerance in rats is associated with a twofold increase in adenosine kinase (ADK) expression in the dorsal horn of the spinal cord. (unime.it)

the respective roles of the A1-, A2-, A3-adenosine receptors as well as the involvement of the PI3-K/PKB/Akt and ERKp44/p42 signal transduction pathways, in the cardioprotective phenomemon of -adrenergic preconditioning and (iv) the contribution of the mitochondrial KATP channels (mKATP), reactive oxygen species and NO to the mechanism of -AR-induced cardioprotection. (sun.ac.za)

In normal tissues, there is low adenoside A3 receptor expression. (drugbank.com)
A1 adenosine receptors (A1 ARs) are expressed in high density in the brain, in adipose tissue and in medium to low levels in many peripheral organ and tissues such as heart, lung and kidney. (unicam.it)

Objectif principal : étude rétrospective monocentrique de la perméabilité primaire d'une FAV proximale mise en place en première intention chez des patients insuffisants rénaux chroniques âgés de 75 ans ou plus. (nephrologuemarseille.fr)
Le temps de saignement après incision à l'oreille chez 8 lapins était significativement prolongé après l'injection intraveineuse d'alun. (who.int)
Ces résultats semblent indiquer que l'utilisation de l'alun en tant qu'antiplaquettaire oral pourrait faire l'objet d'études complémentaires, en tenant compte des effets secondaires éventuels notamment chez les patients dont la fonction rénale est altérée. (who.int)

Highly selective A 3 AR agonists have been synthesized and molecular recognition in the binding site has been characterized. (uconn.edu)
This molecular probe may serve as a companion tool to identify and stratify patient populations based on the prevalence of the target A 3 adenosine receptors. (nih.gov)

Anatomy13

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Chemicals and Drugs201

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Psychiatry and Psychology2

Phenomena and Processes18

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Health Care1

Antagonist8

A3AR14

Antagonists6

Extracellular6

Selective adenosine3

Inhibits3

Affinity10

Modulates3

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Full agonist1

Endogenous adenosine1

Purinergic receptors1

Allosteric Modulation1

Suppresses superoxide2

Pharmacological1

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P2X71

Physiological1

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Inflammation1

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Isoproterenol2

NECA1

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Anti-inflammatory4

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