|Related Categories||Adenosines/P2 Nucleotide Receptor - Antagonists, Adenosines/P2 Nucleotide Receptors (Purinergics), Antagonists, Bioactive Small Molecules, Biochemicals and Reagents,|
|solubility||DMSO: >10 mg/mL|
|0.1 M NaOH: soluble2 mg/mL|
|ethanol: soluble4 mg/mL|
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)|
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Adora3(25370)
Selective A1 adenosine receptor antagonist.
Certificate of Analysis
|Precautionary statements||P261-P305 + P351 + P338|
|Personal Protective Equipment||dust mask type N95 (US), Eyeshields, Gloves|
|Hazard Codes (Europe)||Xi|
|Risk Statements (Europe)||36/37/38|
|Safety Statements (Europe)||26-36|
There are four known subtypes of adenosine receptors, referred to as A1, A2A, A2B and A3. All are members of the superfamily of G protein-coupled receptors and each bears the characteristic motif of ...
Keywords: Atomic absorption spectroscopy, Cancer, Cardiovascular, Diabetes, Diseases, Gene expression, Inflammation, Neurotransmitters, Substitutions, Transduction
G protein-coupled receptors (GPCRs) are the largest class of transmembrane proteins and the targets for almost half of the clinical drugs in the market today. Advances in X-ray crystallography and ot...
Mike Earley, Market Segment Manager, Sigma Life Science
Biofiles Vol. 8, No. 4
Keywords: Clinical, Confocal microscopy, Ligands, Microscopy
1,3-Dipropyl-8-cyclopentylxanthine (DPCPX) inhibition of [3H]N-ethylcarboxamidoadenosine (NECA) binding allows the visualization of putative non-A1 adenosine receptors. Lee, et al. Brain Res. 368, 394-398, (1986)
Antinociception by systemically-administered acetaminophen (paracetamol) involves spinal serotonin 5-HT7 and adenosine A1 receptors, as well as peripheral adenosine A1 receptors. Liu J, Reid AR, and Sawynok J Neurosci. Lett. 536, 64-8, (2013)
Angiotensin II contributes to glomerular hyperfiltration in diabetic rats independently of adenosine type I receptors. Patinha D, Fasching A, Pinho D, et al. Am. J. Physiol. Renal Physiol. 304(5), F614-22, (2013)
Thyroid hormones decrease the affinity of 8-cyclopentyl-1,3-dipropylxanthine (CPX), a competitive antagonist, for the guinea pig atrial A(1) adenosine receptor. Gesztelyi R, Kiss Z, Zsuga J, et al. Gen. Physiol. Biophys. 31(4), 389-400, (2012)
5'-Chloro-5'-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions. Luongo L, Petrelli R, Gatta L, et al. Molecules 17(12), 13712-26, (2012)
The effect of unpredictable chronic mild stress on depressive-like behavior and on hippocampal A1 and striatal A2A adenosine receptors. Crema LM, Pettenuzzo LF, Schlabitz M, et al. Physiol. Behav. 109, 1-7, (2013)
Spinal serotonin 5-HT7 and adenosine A1 receptors, as well as peripheral adenosine A1 receptors, are involved in antinociception by systemically administered amitriptyline. Liu J, Reid AR, and Sawynok J Eur. J. Pharmacol. 698(1-3), 213-9, (2013)
Inhibition of pre-ischeamic conditioning in the mouse caudate brain slice by NMDA- or adenosine A1 receptor antagonists. Chauhan NK, Young AM, Gibson CL, et al. Eur. J. Pharmacol. 698(1-3), 322-9, (2013)
A₁ adenosine receptor modulation of chemically and electrically evoked lumbar locomotor network activity in isolated newborn rat spinal cords. Taccola G, Olivieri D, D'Angelo G, et al. Neuroscience 222, 191-204, (2012)
Genetic inactivation of the adenosine A(2A) receptor exacerbates brain damage in mice with experimental autoimmune encephalomyelitis. Yao SQ, Li ZZ, Huang QY, et al. J. Neurochem. 123(1), 100-12, (2012)
Acute saline expansion increases nephron filtration and distal flow rate but maintains tubuloglomerular feedback responsiveness: role of adenosine A(1) receptors. Blantz RC, Singh P, Deng A, et al. Am. J. Physiol. Renal Physiol. 303(3), F405-11, (2012)
Noninvasive limb remote ischemic preconditioning contributes neuroprotective effects via activation of adenosine A1 receptor and redox status after transient focal cerebral ischemia in rats. Hu S, Dong H, Zhang H, et al. Brain Res. 1459, 81-90, (2012)
Factors mediating remote preconditioning of trauma in the rat heart: central role of the cytochrome p450 epoxygenase pathway in mediating infarct size reduction. Gross GJ, Hsu A, Gross ER, et al. J. Cardiovasc. Pharmacol. Ther. 18(1), 38-45, (2013)
Effects of ethanolic extract and naphthoquinones obtained from the bulbs of Cipura paludosa on short-term and long-term memory: involvement of adenosine A₁ and A₂A receptors. Lucena GM, Matheus FC, Ferreira VM, et al. Basic Clin Pharmacol Toxicol. 112(4), 229-35, (2013)
Genetically controlled upregulation of adenosine A(1) receptor expression enhances the survival of primary cortical neurons. Serchov T, Atas HC, Normann C, et al. Mol. Neurobiol. 46(2), 535-44, (2012)
Adenosine receptor activation is responsible for prolonged depression of synaptic transmission after spreading depolarization in brain slices. Lindquist BE and Shuttleworth CW Neuroscience 223, 365-76, (2012)
A novel dihydro-pyrazolo(3,4d)(1,2,4)triazolo(1,5a)pyrimidin-4-one (AJ23) is an antagonist at adenosine A(1) receptors and enhances consolidation of step-down avoidance. Harvey AL, Young LC, Kornisiuk E, et al. Behav. Brain Res. 234(2), 184-91, (2012)
Coadministration of cannabinoid CB1-receptor and adenosine A1-receptor antagonists improves the acquisition of spatial memory in mice: participation of glutamatergic neurotransmission Assini, F.L., et al. Behav. Pharmacol. 23(3), 292-301, (2012)
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