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Search results for: Adenosine A1 receptor

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#34846650   2021/11/30 To Up

Exogenous adenosine activates A2A adenosine receptor to inhibit RANKL-induced osteoclastogenesis via AP-1 pathway to facilitate bone repair.

Adenosine is a purine nucleoside involved in regulating bone homeostasis through binding to A1, A2A, A2B, and A3 adenosine receptors (A1R, A2AR, A2BR, and A3R, respectively). However, the underlying mechanisms by which adenosine and receptor subtypes regulate osteoclast differentiation remain uncertain. This study aims to assess the role of exogenous adenosine and receptor subtypes in receptor activator of NF-κB ligand (RANKL)-induced osteoclast formation and explore the underlying molecular mechanisms.
Xin Cheng, Chengcheng Yin, Yongqiang Deng, Zubing Li

1651 related Products with: Exogenous adenosine activates A2A adenosine receptor to inhibit RANKL-induced osteoclastogenesis via AP-1 pathway to facilitate bone repair.

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#34831054   2021/10/21 To Up

Adenosine Receptor Antagonists to Combat Cancer and to Boost Anti-Cancer Chemotherapy and Immunotherapy.

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Rafael Franco, Rafael Rivas-Santisteban, Gemma Navarro, Irene Reyes-Resina

2781 related Products with: Adenosine Receptor Antagonists to Combat Cancer and to Boost Anti-Cancer Chemotherapy and Immunotherapy.

0.1 mg1000 100.00 ug100ul100 1 ml100 μg100ul100 100.00 ul

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#34808556   2021/11/19 To Up

Cordycepin suppresses glutamatergic and GABAergic synaptic transmission through activation of A adenosine receptor in rat hippocampal CA1 pyramidal neurons.

Cordycepin (known as 3-deoxyadenosine, CRD), a natural product from the valuable traditional Chinese medicine Cordyceps militaris, has been reported to improve cognitive function and modulate neuroprotective effects on the central nervous system (CNS). However, the modulating mechanisms of cordycepin on information processing in hippocampal CA1 pyramidal neurons are not fully understood. To clarify how cordycepin modulates synaptic responses of pyramidal neurons in rat hippocampal CA1 region, we conducted an electrophysiological experiment using whole-cell patch-clamp technique. The spontaneous and miniature excitatory postsynaptic currents (sEPSCs and mEPSCs, respectively) and the spontaneous and miniature inhibitory postsynaptic currents (sIPSCs and mIPSCs, respectively) recorded by this technique evaluated pure single or multi-synapse responses and enabled us to accurately quantify how cordycepin influenced the pre and postsynaptic aspects of synaptic transmission. The present results showed that cordycepin significantly decreased the frequency of both glutamatergic and GABAergic postsynaptic currents without affecting the amplitude, while these inhibitory effects were antagonized by the A adenosine receptor antagonist (DPCPX), but not the A (ZM 241385), A (MRS1754) and A (MRS1191) adenosine receptor antagonists. Taken together, our results suggested that cordycepin had a clear presynaptic effect on glutamatergic and GABAergic transmission, and provided novel evidence that cordycepin suppresses the synaptic transmission through the activation of AAR.
Jinxiu Wang, Yanchun Gong, Haoyuan Tan, Wenxi Li, Baiyi Yan, Chunfang Cheng, Juan Wan, Wei Sun, Chunhua Yuan, Li-Hua Yao

2795 related Products with: Cordycepin suppresses glutamatergic and GABAergic synaptic transmission through activation of A adenosine receptor in rat hippocampal CA1 pyramidal neurons.

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#34802248   2021/11/22 To Up

Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke.

Treatment with A1R/A3R (adenosine A1 and A3 receptor) agonists in rodent models of acute ischemic stroke results in significantly reduced lesion volume, indicating activation of adenosine A1R or A3R is cerebroprotective. However, dosing and timing required for cerebroprotection has yet to be established, and whether adenosine A1R/A3R activation will lead to cerebroprotection in a gyrencephalic species has yet to be determined.
Theodore E Liston, Aldric Hama, Johannes Boltze, Russell B Poe, Takahiro Natsume, Ikuo Hayashi, Hiroyuki Takamatsu, William S Korinek, James D Lechleiter

2416 related Products with: Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke.

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#34752329   2021/07/12 To Up

Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization.

We compare the GPCR-ligand interactions and highlight important residues for recognition in purinergic receptors-from both X-ray crystallographic and cryo-EM structures. These include A and A adenosine receptors, and P2Y and P2Y receptors that respond to ADP and other nucleotides. These receptors are important drug discovery targets for immune, metabolic and nervous system disorders. In most cases, orthosteric ligands are represented, except for one allosteric P2Y antagonist. This review catalogs the residues and regions that engage in contacts with ligands or with other GPCR protomers in dimeric forms. Residues that are in proximity to bound ligands within purinergic GPCR families are correlated. There is extensive conservation of recognition motifs between adenosine receptors, but the P2Y and P2Y receptors are each structurally distinct in their ligand recognition. Identifying common interaction features for ligand recognition within a receptor class that has multiple structures available can aid in the drug discovery process.
Veronica Salmaso, Shanu Jain, Kenneth A Jacobson

2883 related Products with: Purinergic GPCR transmembrane residues involved in ligand recognition and dimerization.