Neboglamine

Neboglamine (INN) (developmental code names CR-2249, XY-2401), formerly known as nebostinel, is a positive allosteric modulator of the glycine site of the NMDA receptor which is under investigation for Rottapharm for the treatment of schizophrenia and cocaine dependence.[1][2][3][4][5][6] It shows cognition- and memory-enhancing effects in animal models.[7][8][9] As of June 2015, it is in phase II clinical trials for both schizophrenia and cocaine abuse.[10]

Neboglamine
Clinical data
Other namesNebostinel; N-(4,4-Dimethylcyclohexyl)-L-α-glutamine
ATC code
  • None
Identifiers
IUPAC name
  • (4S)-4-Amino-5-[(4,4-dimethylcyclohexyl)amino]-5-oxopentanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard100.162.081
Chemical and physical data
FormulaC13H24N2O3
Molar mass256.346 g·mol−1
3D model (JSmol)
SMILES
  • CC1(CCC(CC1)NC(=O)C(CCC(=O)O)N)C
InChI
  • InChI=1S/C13H24N2O3/c1-13(2)7-5-9(6-8-13)15-12(18)10(14)3-4-11(16)17/h9-10H,3-8,14H2,1-2H3,(H,15,18)(H,16,17)/t10-/m0/s1
  • Key:VCRGLZYPNNAVRP-JTQLQIEISA-N

See also

References
  1. Chiusaroli R, Garofalo P, Espinoza S, Neri E, Caselli G, Lanza M (May 2010). "Antipsychotic-like effects of the N-methyl-D-aspartate receptor modulator neboglamine: an immunohistochemical and behavioural study in the rat". Pharmacological Research. 61 (5): 430–6. doi:10.1016/j.phrs.2009.12.010. PMID 20045056.
  2. Kantrowitz J, Javitt DC (March 2012). "Glutamatergic transmission in schizophrenia: from basic research to clinical practice". Current Opinion in Psychiatry. 25 (2): 96–102. doi:10.1097/YCO.0b013e32835035b2. PMC 5224527. PMID 22297716.
  3. "Drug Development in Schizophrenia: Summary and Table". Pharmaceutical Medicine. 28 (5): 265–271. 2014. doi:10.1007/s40290-014-0070-6. ISSN 1178-2595. S2CID 8513976.
  4. Santangelo RM, Acker TM, Zimmerman SS, Katzman BM, Strong KL, Traynelis SF, Liotta DC (November 2012). "Novel NMDA receptor modulators: an update". Expert Opinion on Therapeutic Patents. 22 (11): 1337–52. doi:10.1517/13543776.2012.728587. PMC 3677696. PMID 23009122.
  5. Zink M, Correll CU (May 2015). "Glutamatergic agents for schizophrenia: current evidence and perspectives". Expert Review of Clinical Pharmacology. 8 (3): 335–52. doi:10.1586/17512433.2015.1040393. PMID 25916667. S2CID 39547774.
  6. Köster LS, Carbon M, Correll CU (December 2014). "Emerging drugs for schizophrenia: an update". Expert Opinion on Emerging Drugs. 19 (4): 511–31. doi:10.1517/14728214.2014.958148. PMID 25234340. S2CID 42729570.
  7. Garofalo P, Colombo S, Lanza M, Revel L, Makovec F (December 1996). "CR 2249: a new putative memory enhancer. Behavioural studies on learning and memory in rats and mice". The Journal of Pharmacy and Pharmacology. 48 (12): 1290–7. doi:10.1111/j.2042-7158.1996.tb03938.x. PMID 9004193. S2CID 34902435.
  8. Lanza M, Bonnafous C, Colombo S, Revel L, Makovec F (August 1997). "Characterization of a novel putative cognition enhancer mediating facilitation of glycine effect on strychnine-resistant sites coupled to NMDA receptor complex". Neuropharmacology. 36 (8): 1057–64. doi:10.1016/S0028-3908(97)00092-0. PMID 9294970. S2CID 11958361.
  9. Lanza M, Makovec F (1997). "Cognition Enhancing Profile of CR 2249, a New NMDA-Glycine Site Modulator". CNS Drug Reviews. 3 (3): 245–259. doi:10.1111/j.1527-3458.1997.tb00326.x. ISSN 1080-563X.
  10. "Neboglamine". AdisInsight. Retrieved 2015-06-10.


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