Neboglamine
Chemical compound
- None
- (4S)-4-Amino-5-[(4,4-dimethylcyclohexyl)amino]-5-oxopentanoic acid
- 163000-63-3
- 3074827
- 2333649
- 12EA34U5B8
- DTXSID2045787
- Interactive image
- 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
Neboglamine (INNTooltip 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
- Nebostinel - AdisInsight
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- Agonists: Main site agonists: 5-Fluorowillardiine
- Acromelic acid (acromelate)
- AMPA
- BOAA
- Domoic acid
- Glutamate
- Ibotenic acid
- Proline
- Quisqualic acid
- Willardiine; Positive allosteric modulators: Aniracetam
- Cyclothiazide
- CX-516
- CX-546
- CX-614
- Farampator (CX-691, ORG-24448)
- CX-717
- CX-1739
- CX-1942
- Diazoxide
- Hydrochlorothiazide (HCTZ)
- IDRA-21
- LY-392098
- LY-395153
- LY-404187
- LY-451646
- LY-503430
- Mibampator (LY-451395)
- Nooglutyl
- ORG-26576
- Oxiracetam
- PEPA
- Pesampator (BIIB-104, PF-04958242)
- Piracetam
- Pramiracetam
- S-18986
- Tulrampator (S-47445, CX-1632)
- Antagonists: ACEA-1011
- ATPO
- Becampanel
- Caroverine
- CNQX
- Dasolampanel
- DNQX
- Fanapanel (MPQX)
- GAMS
- Kaitocephalin
- Kynurenic acid
- Kynurenine
- Licostinel (ACEA-1021)
- NBQX
- PNQX
- Selurampanel
- Tezampanel
- Theanine
- Topiramate
- YM90K
- Zonampanel; Negative allosteric modulators: Barbiturates (e.g., pentobarbital, sodium thiopental)
- Cyclopropane
- Enflurane
- Ethanol (alcohol)
- Evans blue
- GYKI-52466
- GYKI-53655
- Halothane
- Irampanel
- Isoflurane
- Perampanel
- Pregnenolone sulfate
- Sevoflurane
- Talampanel; Unknown/unsorted antagonists: Minocycline
- Agonists: Main site agonists: 5-Bromowillardiine
- 5-Iodowillardiine
- Acromelic acid (acromelate)
- AMPA
- ATPA
- Domoic acid
- Glutamate
- Ibotenic acid
- Kainic acid
- LY-339434
- Proline
- Quisqualic acid
- SYM-2081; Positive allosteric modulators: Cyclothiazide
- Diazoxide
- Enflurane
- Halothane
- Isoflurane
- Antagonists: ACEA-1011
- CNQX
- Dasolampanel
- DNQX
- GAMS
- Kaitocephalin
- Kynurenic acid
- Licostinel (ACEA-1021)
- LY-382884
- NBQX
- NS102
- Selurampanel
- Tezampanel
- Theanine
- Topiramate
- UBP-302; Negative allosteric modulators: Barbiturates (e.g., pentobarbital, sodium thiopental)
- Enflurane
- Ethanol (alcohol)
- Evans blue
- NS-3763
- Pregnenolone sulfate
- Agonists: Main site agonists: AMAA
- Aspartate
- Glutamate
- Homocysteic acid (L-HCA)
- Homoquinolinic acid
- Ibotenic acid
- NMDA
- Proline
- Quinolinic acid
- Tetrazolylglycine
- Theanine; Glycine site agonists: β-Fluoro-D-alanine
- ACBD
- ACC (ACPC)
- ACPD
- AK-51
- Apimostinel (NRX-1074)
- B6B21
- CCG
- D-Alanine
- D-Cycloserine
- D-Serine
- DHPG
- Dimethylglycine
- Glycine
- HA-966
- L-687414
- L-Alanine
- L-Serine
- Milacemide
- Neboglamine (nebostinel)
- Rapastinel (GLYX-13)
- Sarcosine; Polyamine site agonists: Neomycin
- Spermidine
- Spermine; Other positive allosteric modulators: 24S-Hydroxycholesterol
- DHEATooltip Dehydroepiandrosterone (prasterone)
- DHEA sulfate (prasterone sulfate)
- Epipregnanolone sulfate
- Plazinemdor
- Pregnenolone sulfate
- SAGE-201
- SAGE-301
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- Antagonists: Competitive antagonists: AP5 (APV)
- AP7
- CGP-37849
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- CPP
- Kaitocephalin
- LY-233053
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- MDL-100453
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- NPC-12626
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- PBPD
- PEAQX
- Perzinfotel
- PPDA
- SDZ-220581
- Selfotel; Glycine site antagonists: 4-Cl-KYN (AV-101)
- 5,7-DCKA
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- ACC
- ACEA-1011
- ACEA-1328
- Apimostinel (NRX-1074)
- AV-101
- Carisoprodol
- CGP-39653
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- Kynurenine
- L-689560
- L-701324
- Licostinel (ACEA-1021)
- LU-73068
- MDL-105519
- Meprobamate
- MRZ 2/576
- PNQX
- Rapastinel (GLYX-13)
- ZD-9379; Polyamine site antagonists: Arcaine
- Co 101676
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- 3-HO-PCP
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- Rislenemdaz (CERC-301, MK-0657)
- Ro 8-4304
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- Traxoprodil (CP-101606); NR2A-selective antagonists: MPX-004
- MPX-007
- TCN-201
- TCN-213; Cations: Hydrogen
- Magnesium
- Zinc; Alcohols/volatile anesthetics/related: Benzene
- Butane
- Chloroform
- Cyclopropane
- Desflurane
- Diethyl ether
- Enflurane
- Ethanol (alcohol)
- Halothane
- Hexanol
- Isoflurane
- Methoxyflurane
- Nitrous oxide
- Octanol
- Sevoflurane
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- Trichloroethane
- Trichloroethanol
- Trichloroethylene
- Urethane
- Xenon
- Xylene; Unknown/unsorted antagonists: ARR-15896
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- D-αAA
- Dexanabinol
- Flufenamic acid
- Flupirtine
- FPL-12495
- FR-115427
- Furosemide
- Hodgkinsine
- Ipenoxazone (MLV-6976)
- MDL-27266
- Metaphit
- Minocycline
- MPEP
- Niflumic acid
- Pentamidine
- Pentamidine isethionate
- Piretanide
- Psychotridine
- Transcrocetin (saffron)
- Unsorted: Allosteric modulators: AGN-241751
- See also: Receptor/signaling modulators
- Metabotropic glutamate receptor modulators
- Glutamate metabolism/transport modulators
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