BQ-869

BQ-869
Clinical data
Other namesBQ869
Drug classNMDA receptor antagonist
ATC code
  • None
Chemical and physical data
FormulaC15H11ClN2
Molar mass254.72 g·mol−1
3D model (JSmol)
  • CNC1=CC2=C3C4=C1C=CC=C4NC3=C(Cl)C=C2
  • InChI=1S/C15H11ClN2/c1-17-12-7-8-5-6-10(16)15-13(8)14-9(12)3-2-4-11(14)18-15/h2-7,17-18H,1H3
  • Key:NFOBXMLDDAQTJH-UHFFFAOYSA-N

BQ-869 is an NMDA receptor antagonist related to dizocilpine (MK-801). It is described as a derivative of dizocilpine and has shown higher potency in comparison. The drug shows neuroprotective effects in rodents, for instance against stroke and cerebral ischemia. It is described as being "extremely potent" and was said to be "the most potent antagonist of NMDA receptors". However, this was not based on standard affinity or functional assays for establishing potency. BQ-869 was described in the scientific literature by Guo Yu and colleagues in Shanghai, China in 2015.

See also

References

  1. 1 2 Santana MV, Castro HC, Abreu PA (21 December 2017). "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. Vol. 5. UAE: Bentham Science Publishers Ltd. 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. 1 2 3 4 5 6 Yu G, Wu F, Wang ES (2015). "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. PMC 4396341. 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. [...]