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Adenosine A1 receptor

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The correct title of this article is Adenosine A1 receptor. It appears incorrectly here because of technical restrictions.

Adenosine A1 receptor
Symbol(s) ADORA1; RDC7
External IDs OMIM: 102775 MGI99401 Homologene20165
RNA expression pattern



More reference expression data

Human Mouse Entrez 134 11539 Ensembl ENSG00000163485 ENSMUSG00000042429 Uniprot P30542 Q3URG8 Refseq NM_000674 (mRNA)
NP_000665 (protein)
NM_001008533 (mRNA)
NP_001008533 (protein)
Location Chr 1: 201.33 - 201.4 Mb Chr 1: 136.02 - 136.05 Mb
Pubmed search [1] [2]

The adenosine A1 receptor[1] is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand.


A1 receptors are implicated in sleep promotion by inhibiting wake promoting cholinergic neurons in the basal forebrain.[2] A1 receptors are also present in smooth muscle throughout the vascular system.[3]



Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an inhibition of adenylate cyclase and therefore a decrease in the cAMP concentration. An increase of the inositol triphosphate/diacylglycerol concentration is caused by an activation of phospholipase C while the elevated levels of arachidonic acid are mediated by phospholipase 2A Several types of potassium channels are activated but N-, P- and Q-type calcium channels are inhibited.[4]



Antagonism and agonismEdit

Caffeine, along with theophylline have been found to antagonize both A1 and A2a receptors in the brain. Specific antagonists include 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX), and Cyclopentyltheophylline‎ (CPT) or 8-cyclopentyl-1,3-dipropylxanthine‎ (CPX), while specific agonists include 2-chloro-N(6)-cyclopentyladenosine (CCPA).

In heartEdit



In neonatal medicineEdit

Adenosine antagonists are widely used in neonatal medicine;



However, we are unaware of clinical studies that have examined the incidence of periventricular leukomalacia (PVL) as related to neonatal caffeine use. Caffeine may reduce cerebral blood flow in premature infants, possibly by blocking vascular A2 ARs. Thus, it may prove more advantageous to use selective A1 antagonists to help reduce adenosine-induced brain injury.

References Edit

  1. Townsend-Nicholson A, Baker E, Schofield PR, Sutherland GR (1995). Localization of the adenosine A1 receptor subtype gene (ADORA1) to chromosome 1q32.1. Genomics 26 (2): 423–5.
  2. Elmenhorst D, Meyer PT, Winz OH, Matusch A, Ermert J, Coenen HH, Basheer R, Haas HL, Zilles K, Bauer A (2007). Sleep deprivation increases A1 adenosine receptor binding in the human brain: a positron emission tomography study. J. Neurosci. 27 (9): 2410–5.
  3. Tawfik HE, Schnermann J, Oldenburg PJ, Mustafa SJ (2005). Role of A1 adenosine receptors in regulation of vascular tone. Am. J. Physiol. Heart Circ. Physiol. 288 (3): H1411–6.

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