From Wikipedia, the free encyclopedia
Chemical compound
Neboglamine
Other names Nebostinel; N -(4,4-Dimethylcyclohexyl)-L -α-glutamine
ATC code
(4S )-4-Amino-5-[(4,4-dimethylcyclohexyl)amino]-5-oxopentanoic acid
CAS Number
PubChem
CID
ChemSpider
UNII
CompTox Dashboard (
EPA )
ECHA InfoCard
100.162.081
Formula C 13 H 24 N 2 O 3
Molar mass 256.346 g·mol−1 3D model (
JSmol )
CC1(CCC(CC1)NC(=O)C(CCC(=O)O)N)C
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
Neboglamine (
INN Tooltip International Nonproprietary Name ) (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]
See also
References
^ 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 .
^ 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 .
^ "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 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .
^ 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 .
^
"Neboglamine" . AdisInsight . Retrieved 2015-06-10 .
External links
AMPAR Tooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KAR Tooltip Kainate receptor
NMDAR Tooltip N-Methyl-D-aspartate receptor