Chemistry:NAS-181

From HandWiki

NAS-181, also known as MCOMM, is a selective rodent serotonin 5-HT1B receptor antagonist which is used in scientific research.[1][2]

In animals, NAS-181 has been found to strongly increase acetylcholine levels in the frontal cortex and hippocampus.[3][4] It has been found to block memory impairment induced by the antimuscarinic agent scopolamine and by the NMDA receptor antagonist dizocilpine (MK-801).[5][6] Injection of NAS-181 directly into the nucleus accumbens has also been found to reverse the prosocial behavior induced by the serotonin releasing agent MDMA in animals.[7]

NAS-181 was first described in the scientific literature by 1998.[8] The drug was discovered by researchers at Astra Arcus.[2]

See also

References

  1. ↑ "THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors". British Journal of Pharmacology 176 Suppl 1 (Suppl 1): S21–S141. December 2019. doi:10.1111/bph.14748. PMID 31710717. 
  2. ↑ 2.0 2.1 "Recent advances in 5-HT1B/1D receptor antagonists and agonists and their potential therapeutic applications". Current Topics in Medicinal Chemistry 2 (6): 559–574. June 2002. doi:10.2174/1568026023393903. PMID 12052194. 
  3. ↑ "The 5-HT1B receptor - a potential target for antidepressant treatment". Psychopharmacology 235 (5): 1317–1334. May 2018. doi:10.1007/s00213-018-4872-1. PMID 29546551. 
  4. ↑ "Effects of the 5-HT1B receptor antagonist NAS-181 on extracellular levels of acetylcholine, glutamate and GABA in the frontal cortex and ventral hippocampus of awake rats: a microdialysis study". European Neuropsychopharmacology 17 (9): 580–586. September 2007. doi:10.1016/j.euroneuro.2006.12.002. PMID 17234388. 
  5. ↑ "The role of serotonin in memory: interactions with neurotransmitters and downstream signaling". Experimental Brain Research 232 (3): 723–738. March 2014. doi:10.1007/s00221-013-3818-4. PMID 24430027. 
  6. ↑ "The 5-HT1B receptor: a novel target for the pathophysiology of depression". Current Drug Targets 10 (11): 1118–1138. November 2009. doi:10.2174/138945009789735192. PMID 19702551. 
  7. ↑ "Distinct neural mechanisms for the prosocial and rewarding properties of MDMA". Science Translational Medicine 11 (522). December 2019. doi:10.1126/scitranslmed.aaw6435. PMID 31826983. 
  8. ↑ "(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist". Journal of Medicinal Chemistry 41 (11): 1934–1942. May 1998. doi:10.1021/jm970806i. PMID 9599242. 



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