Introduction of ADORA1

The adenosine A₁ receptor (ADORA1) belongs to the adenosine receptor group of G protein-coupled receptors which use adenosine as endogenous ligand. The A1 receptor includes A2A, A2B, and A3 and displays high expression levels in the brain (cortex, cerebellum, hippocampus), dorsal horn of the spinal cord, eye and atria. ADORA1 is encoded by the ADORA1 gene. An important paralog of this gene is ADORA2A.

Function of ADORA1 Membrane Protein

A₁ receptors participate in sleep promotion by inhibiting arousal of cholinergic neurons in the basal forebrain and also present in the smooth muscle of the entire vascular system. Agonists activate adenosine A₁ receptors to cause binding of Gi1 / 2/3 or Go proteins, resulting in inhibition of adenylate cyclase and reduction of cAMP concentration. The increase in inositol triphosphate/diglyceride concentration is caused by the activation of phospholipase C. DAG lipase mediates elevated arachidonic acid levels, and DAG lipase cleaves DAG to form arachidonic acid. Several types of potassium channels are activated, but N-, P- and Q-type calcium channels are inhibited. Endogenous adenosine A₁ and A_2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow. Since the decrease in A₁ expression appears to prevent hypoxia-induced ventricular dilatation and white matter loss, the pharmacological blockade of A₁ may have clinical utility.

Fig.1 Adenosine formation and catabolism. (Sachdeva, 2013)

Application of ADORA1 Membrane Protein in Literature

1. El-Hashim A Z., et al. Central adenosine A₁ receptors inhibit cough via suppression of excitatory glutamatergic and tachykininergic neurotransmission. Br J Pharmacol. 2018, 175(15): 3162-3174. PubMed ID: 29767468

This article reveals that ADORA1 mediates several excitatory effects in the airways and has inhibitory effects in the central nervous system. ADORA1 may be useful in regulating cough and airway obstruction.

2. Beste A., et al. Mechanisms of acetylcholinesterase protection against sarin and soman by adenosine A₁ receptor agonist N⁶-cyclopentyladenosine. Comput Biol Chem. 2018, 75: 74-81. PubMed ID: 29747078

Authors in this group have demonstrated that alternative acute treatment with the adenosine A₁ receptor agonist N⁶-cyclopentyladensosine (CPA) could prevent AChE inhibition as well as to suppress neuronal activity. They try to explain the mechanisms of acetylcholinesterase protection against sarin and soman by ADORA1 agonist N⁶-cyclopentyladenosine.

3. Mitani T., et al. Theobromine suppresses adipogenesis through enhancement of CCAAT-enhancer-binding protein β degradation by adenosine receptor A1. Biochim Biophys Acta. 2017, 1864(12): 2438-2448. PubMed ID: 28965824

The article reports that theobromine selectively interacts with ADORA1 and ADORA1 knockdown inhibits theobromine-induced C/EBPβ degradation. The inhibition of ADORA1 signaling is essential for theobromine-induced C/EBPβ degradation.

4. Luan G., et al. Upregulation of Neuronal Adenosine A1 Receptor in Human Rasmussen Encephalitis. J Neuropathol Exp Neurol. 2017, 76(8): 720-731. PubMed ID: 28789481

This article focuses on the role adenosine A₁ receptor plays in human Rasmussen encephalitis. It shows that over-expression of adenosine kinase is a common pathologic hallmark of Rasmussen encephalitis, and that upregulation of neuronal A1R in Rasmussen encephalitis is crucial in preventing the spread of seizures.

5. Riff R., et al. Systemic inflammatory response syndrome-related lymphopenia is associated with adenosine A₁ receptor dysfunction. J Leukoc Biol. 2017, 102(1): 95-103. PubMed ID: 28495790

This article evaluates the role of adenosine in SIRS-mediated lymphopenia and impaired IL-15 production. They suggest that systemic inflammatory response syndrome-related lymphopenia is associated with adenosine A₁ receptor dysfunction and interference with adenosine signaling may thus be potentially beneficial for septic patients with leukopenia.

ADORA1 Preparation Options

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Reference

1. Sachdeva S and Gupta M. (2013). Adenosine and its receptors as therapeutic targets: An overview. Saudi Pharm J. 21(3), 245-53.

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