Istradefylline - CAS 155270-99-8
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Not Intended for Therapeutic Use. For research use only.
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Adenosine A2a | Adenosine Receptor
A very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM)
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Brife Description:
A very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM)
Pale Green Solid
KW-6002; 8-[(1E)-2-(2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
4 mg/mL < DMSO < 15mg/mL
Store at +4°C
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1.The safety of istradefylline for the treatment of Parkinson's disease.
Müller T1. Expert Opin Drug Saf. 2015 May;14(5):769-75. doi: 10.1517/14740338.2015.1014798. Epub 2015 Feb 13.
INTRODUCTION: Antagonism of the A2A receptor improves motor behavior in patients with Parkinson's disease (PD), according to results of clinical studies which confirm findings of previous experimental research. The xanthine derivative, istradefylline , has the longest half-life out of the available A2A receptor antagonists. Istradefylline easily crosses the blood-brain barrier and shows a high affinity to the human A2A receptor.
2.Purinergic signaling in Parkinson's disease. Relevance for treatment.
Navarro G1, Borroto-Escuela DO2, Fuxe K3, Franco R4. Neuropharmacology. 2015 Jul 23. pii: S0028-3908(15)30031-9. doi: 10.1016/j.neuropharm.2015.07.024. [Epub ahead of print]
Purinergic signaling modulates dopaminergic neurotransmission in health and disease. Classically adenosine A1 and A2A receptors have been considered key for the fine tune control of dopamine actions in the striatum, the main CNS motor control center. The main adenosine signaling mechanism is via the cAMP pathway but the future will tell whether calcium signaling is relevant in adenosinergic control of striatal function. Very relevant is the recent approval in Japan of the adenosine A2A receptor antagonist, istradefylline, for use in Parkinson's disease patients. Purine nucleotides are also regulators of striatal dopamine neurotransmission via P2 purinergic receptors. In parallel to the alpha-synuclein hypothesis of Parkinson's disease etiology, purinergic P2X1 receptors have been identified as mediators of accumulation of the Lewy-body enriched protein alpha-synuclein. Of note is the expression in striatum of purinergic-receptor-containing heteromers that are potential targets of anti-Parkinson's disease therapies and should be taken into account in drug discovery programs.
3.Clinical efficacy of istradefylline versus rTMS on Parkinson's disease in a randomized clinical trial.
Li ZJ1, Wu Q1, Yi CJ1. Curr Med Res Opin. 2015 Nov;31(11):2055-8. doi: 10.1185/03007995.2015.1086994. Epub 2015 Sep 22.
OBJECTIVE: To compare the efficacy of istradefylline (20 mg/day, 40 mg/day) and repetitive transcranial magnetic stimulation (rTMS) (1 Hz, 10 Hz) as an adjunct therapy to levodopa in the treatment of Parkinson's disease (PD).
4.Suppression of adenosine 2a receptor (A2aR)-mediated adenosine signaling improves disease phenotypes in a mouse model of amyotrophic lateral sclerosis.
Ng SK1, Higashimori H1, Tolman M2, Yang Y3. Exp Neurol. 2015 May;267:115-22. doi: 10.1016/j.expneurol.2015.03.004. Epub 2015 Mar 13.
Amyotrophic lateral sclerosis (ALS) is a rapidly progressing neurodegenerative disease in which the majority of upper and lower motor neurons are degenerated. Despite intensive efforts to identify drug targets and develop neuroprotective strategies, effective therapeutics for ALS remains unavailable. The identification and characterization of novel targets and pathways remain crucial in the development of ALS therapeutics. Adenosine is a major neuromodulator that actively regulates synaptic transmission. Interestingly, adenosine levels are significantly elevated in the cerebrospinal fluid (CSF) of progressing human ALS patients. In the current study, we showed that adenosine 2a receptor (A2aR), but not adenosine 1 receptor (A1R), is highly enriched in spinal (motor) neurons. A2aR expression is also selectively increased at the symptomatic onset in the spinal cords of SOD1G93A mice and end-stage human ALS spinal cords. Interestingly, we found that direct adenosine treatment is sufficient to induce embryonic stem cell-derived motor neuron (ESMN) cell death in cultures.
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