Chemistry:BQ-869
From HandWiki
BQ-869 is an NMDA receptor antagonist related to dizocilpine (MK-801).[1][2] It is described as a derivative of dizocilpine and has shown higher potency in comparison.[2] The drug shows neuroprotective effects in rodents, for instance against stroke and cerebral ischemia.[1][2] It is described as being "extremely potent" and was said to be "the most potent antagonist of NMDA receptors".[2] However, this was not based on standard affinity or functional assays for establishing potency.[2] BQ-869 was described in the scientific literature by Guo Yu and colleagues in Shanghai, China in 2015.[2]
See also
- Dextromethorphan (DXM)
References
- ↑ 1.0 1.1 "NMDA Receptor as a Molecular Target for Central Nervous System Disorders: The Advances and Contributions of Molecular Modeling". Frontiers in Clinical Drug Research - CNS and Neurological Disorders Volume 5. 5. UAE: Bentham Science Publishers Ltd.. 21 December 2017. pp. 211–249. doi:10.2174/97816810858521170501. ISBN 978-1-68108-585-2. "Also, BQ-869, a potent antagonist of NMDA receptors reduced Ca2+ influx induced by NMDA, decreased infarction size in focal cerebral ischemia and reduced stroke mortality in rats [77] [...]"
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "BQ-869, a novel NMDA receptor antagonist, protects against excitotoxicity and attenuates cerebral ischemic injury in stroke". International Journal of Clinical and Experimental Pathology 8 (2): 1213–1225. 2015. PMID 25973006. "[...] BQ-869, a potent NMDA receptor antagonist, blocked NMDA receptor in concentration-dependent and dose-dependent manner, attenuated NMDA-induced Ca2+ influx, inhabited NMDAR-mEPSC in hippocampal pyramidal neurons, improved athletic ability of rats with [middle cerebral artery occlusion (MACO)], decreased infarction size in focal cerebral ischemia rats and reduced stroke mortality. [...] the neuroprotective effect of BQ-869 might be through inhibiting NMDA-mediated excitotoxicity. These findings indicate that BQ-869 is the most potent antagonist of NMDA receptors, [...] BQ-869 is a derivative of NMDA receptor antagonist MK801, and the present study shows that it as an extremely potent neuroprotectant. [...] The different suppression capabilities suggests BQ-869 shows higher NMDA receptor inhibitory effects than MK-801, a commonly used antagonist of NMDA receptors, which suggested BQ-869 is a new NMDA receptor antagonist with higher appetency. [...]".
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