NAS-181 explained
| Class: | Serotonin 5-HT1B receptor antagonist |
| Cas Number: | 205242-61-1 |
| Pubchem: | 9955015 |
| Unii: | EB3GE9ZR8T |
| Chembl: | 1789131 |
| Synonyms: | NAS181; MCOMM |
| Iupac Name: | (2R)-2-3-(morpholin-4-ylmethyl)-2H-chromen-8-yloxymethyl]morpholine |
| C: | 19 |
| H: | 26 |
| N: | 2 |
| O: | 4 |
| Smiles: | C1CO[C@H](CN1)COC2=CC=CC3=C2OCC(=C3)CN4CCOCC4 |
| Stdinchi: | 1S/C19H26N2O4/c1-2-16-10-15(12-21-5-8-22-9-6-21)13-25-19(16)18(3-1)24-14-17-11-20-4-7-23-17/h1-3,10,17,20H,4-9,11-14H2/t17-/m1/s1 |
| Stdinchikey: | RTKDBEOSPDFLGD-QGZVFWFLSA-N |
NAS-181, also known as MCOMM, is a selective rodent serotonin 5-HT1B receptor antagonist which is used in scientific research.[1]
In animals, NAS-181 has been found to strongly increase acetylcholine levels in the frontal cortex and hippocampus.[2] [3] It has been found to block memory impairment induced by the antimuscarinic agent scopolamine and by the NMDA receptor antagonist dizocilpine (MK-801).[4] [5] 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.[6]
NAS-181 was first described in the scientific literature by 1998.[7]
Notes and References
- Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA . THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors . British Journal of Pharmacology . 176 Suppl 1 . Suppl 1 . S21–S141 . December 2019 . 31710717 . 6844580 . 10.1111/bph.14748 .
- Tiger M, Varnäs K, Okubo Y, Lundberg J . The 5-HT1B receptor - a potential target for antidepressant treatment . Psychopharmacology . 235 . 5 . 1317–1334 . May 2018 . 29546551 . 5919989 . 10.1007/s00213-018-4872-1 .
- Hu XJ, Wang FH, Stenfors C, Ogren SO, Kehr J . 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 . 17234388 . 10.1016/j.euroneuro.2006.12.002 .
- Seyedabadi M, Fakhfouri G, Ramezani V, Mehr SE, Rahimian R . The role of serotonin in memory: interactions with neurotransmitters and downstream signaling . Experimental Brain Research . 232 . 3 . 723–738 . March 2014 . 24430027 . 10.1007/s00221-013-3818-4 .
- Ruf BM, Bhagwagar Z . The 5-HT1B receptor: a novel target for the pathophysiology of depression . Current Drug Targets . 10 . 11 . 1118–1138 . November 2009 . 19702551 . 10.2174/138945009789735192 .
- Heifets BD, Salgado JS, Taylor MD, Hoerbelt P, Cardozo Pinto DF, Steinberg EE, Walsh JJ, Sze JY, Malenka RC . Distinct neural mechanisms for the prosocial and rewarding properties of MDMA . Science Translational Medicine . 11 . 522 . December 2019 . 31826983 . 7123941 . 10.1126/scitranslmed.aaw6435 .
- Slassi A . 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 . 12052194 . 10.2174/1568026023393903 .
- Berg S, Larsson LG, Rényi L, Ross SB, Thorberg SO, Thorell-Svantesson G . (R)-(+)-2-3-(Morpholinomethyl)-2H-chromen-8-yloxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist | journal = Journal of Medicinal Chemistry | volume = 41 | issue = 11 | pages = 1934–1942 | date = May 1998 | pmid = 9599242 | doi = 10.1021/jm970806i }} The drug was discovered by researchers at Astra Arcus.[7]
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