Chemistry:SCH-58261
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Short description: Chemical compound
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| Formula | C18H15N7O |
| Molar mass | 345.366 g·mol−1 |
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SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A2A, with more than 50x selectivity for A2A over other adenosine receptors.[1] It has been used to investigate the mechanism of action of caffeine, which is a mixed A1 / A2A antagonist, and has shown that the A2A receptor is primarily responsible for the stimulant and ergogenic effects of caffeine,[2] but blockade of both A1 and A2A receptors is required to accurately replicate caffeine's effects in animals.[3][4][5][6] SCH-58261 has also shown antidepressant,[7] nootropic and neuroprotective effects in a variety of animal models,[8][9][10][11][12][13] and has been investigated as a possible treatment for Parkinson's disease.[14][15]
See also
- CGS-15943
- Istradefylline (KW-6002)
References
- ↑ "The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist". The Journal of Pharmacology and Experimental Therapeutics 276 (2): 398–404. February 1996. PMID 8632302.
- ↑ "Neuronal adenosine A2A receptors signal ergogenic effects of caffeine". Scientific Reports 10 (1): 13414. August 2020. doi:10.1038/s41598-020-69660-1. PMID 32770138. Bibcode: 2020NatSR..1013414A.
- ↑ "Antagonism of adenosine A2A receptors underlies the behavioural activating effect of caffeine and is associated with reduced expression of messenger RNA for NGFI-A and NGFI-B in caudate-putamen and nucleus accumbens". Neuroscience 79 (3): 753–64. August 1997. doi:10.1016/S0306-4522(97)00046-8. PMID 9219939.
- ↑ "Adenosine A1 and A2A receptor antagonists stimulate motor activity: evidence for an increased effectiveness in aged rats". Neuroscience Letters 251 (3): 201–4. July 1998. doi:10.1016/S0304-3940(98)00533-3. PMID 9726378.
- ↑ "The stimulant effects of caffeine on locomotor behaviour in mice are mediated through its blockade of adenosine A(2A) receptors". British Journal of Pharmacology 129 (7): 1465–73. April 2000. doi:10.1038/sj.bjp.0703170. PMID 10742303.
- ↑ "Combination of adenosine A1 and A2A receptor blocking agents induces caffeine-like locomotor stimulation in mice". European Neuropsychopharmacology 16 (2): 129–36. February 2006. doi:10.1016/j.euroneuro.2005.07.001. PMID 16054807.
- ↑ "Adenosine A2A receptors and depression". Neurology 61 (11 Suppl 6): S82-7. December 2003. doi:10.1212/01.WNL.0000095220.87550.F6. PMID 14663017.
- ↑ "Blockade of adenosine A2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats". NeuroReport 9 (17): 3955–9. December 1998. doi:10.1097/00001756-199812010-00034. PMID 9875735.
- ↑ "Blockade of striatal adenosine A2A receptor reduces, through a presynaptic mechanism, quinolinic acid-induced excitotoxicity: possible relevance to neuroprotective interventions in neurodegenerative diseases of the striatum". The Journal of Neuroscience 22 (5): 1967–75. March 2002. doi:10.1523/jneurosci.22-05-01967.2002. PMID 11880527.
- ↑ "The selective A2A receptor antagonist SCH 58261 protects from neurological deficit, brain damage and activation of p38 MAPK in rat focal cerebral ischemia". Brain Research 1073-1074: 470–80. February 2006. doi:10.1016/j.brainres.2005.12.010. PMID 16443200.
- ↑ "Effects of the adenosine A2A receptor antagonist SCH 58621 on cyclooxygenase-2 expression, glial activation, and brain-derived neurotrophic factor availability in a rat model of striatal neurodegeneration". Journal of Neuropathology and Experimental Neurology 66 (5): 363–71. May 2007. doi:10.1097/nen.0b013e3180517477. PMID 17483693.
- ↑ "Adenosine A2A receptor blockade prevents synaptotoxicity and memory dysfunction caused by beta-amyloid peptides via p38 mitogen-activated protein kinase pathway". The Journal of Neuroscience 29 (47): 14741–51. November 2009. doi:10.1523/JNEUROSCI.3728-09.2009. PMID 19940169.
- ↑ "Memory deficits induced by chronic cannabinoid exposure are prevented by adenosine A2AR receptor antagonism". Neuropharmacology 155: 10–21. September 2019. doi:10.1016/j.neuropharm.2019.05.003. PMID 31103616.
- ↑ "Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease". The Journal of Neuroscience 21 (10): RC143. May 2001. doi:10.1523/JNEUROSCI.21-10-j0001.2001. PMID 11319241.
- ↑ "Dopamine and adenosine receptor interaction as basis for the treatment of Parkinson's disease". Journal of the Neurological Sciences 248 (1–2): 48–52. October 2006. doi:10.1016/j.jns.2006.05.038. PMID 16780890.
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