LY-235959
Chemical compound
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Formula | C11H20NO5P |
Molar mass | 277.257 g·mol−1 |
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LY-235959 is a competitive antagonist at the NMDA receptor.[1] It has analgesic and neuroprotective effects and causes hypothermia in animal models,[2] as well as reducing the development of tolerance to morphine and altering the reinforcing effects of cocaine.[3][4][5][6][7]
References
- ^ Allen RM, Dykstra LA (July 2001). "N-methyl-D-aspartate receptor antagonists potentiate the antinociceptive effects of morphine in squirrel monkeys". The Journal of Pharmacology and Experimental Therapeutics. 298 (1): 288–97. PMID 11408554.
- ^ Rawls SM, Cowan A, Tallarida RJ, Geller EB, Adler MW (October 2002). "N-methyl-D-aspartate antagonists and WIN 55212-2 [4,5-dihydro-2-methyl-4(4-morpholinylmethyl)-1-(1-naphthalenyl-carbonyl)-6H-pyrrolo[3,2,1-i,j]quinolin-6-one], a cannabinoid agonist, interact to produce synergistic hypothermia". The Journal of Pharmacology and Experimental Therapeutics. 303 (1): 395–402. doi:10.1124/jpet.102.037473. PMID 12235276. S2CID 18307764.
- ^ Allen RM, Carelli RM, Dykstra LA, Suchey TL, Everett CV (October 2005). "Effects of the competitive N-methyl-D-aspartate receptor antagonist, LY235959 [(-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid], on responding for cocaine under both fixed and progressive ratio schedules of reinforcement". The Journal of Pharmacology and Experimental Therapeutics. 315 (1): 449–57. doi:10.1124/jpet.105.086355. PMID 16024734. S2CID 15151429.
- ^ Allen RM, Dykstra LA, Carelli RM (April 2007). "Continuous exposure to the competitive N-methyl-D: -aspartate receptor antagonist, LY235959, facilitates escalation of cocaine consumption in Sprague-Dawley rats". Psychopharmacology. 191 (2): 341–51. doi:10.1007/s00213-006-0661-3. PMID 17225167. S2CID 20887004.
- ^ Fischer BD, Ward SJ, Henry FE, Dykstra LA (February 2010). "Attenuation of morphine antinociceptive tolerance by a CB(1) receptor agonist and an NMDA receptor antagonist: Interactive effects". Neuropharmacology. 58 (2): 544–50. doi:10.1016/j.neuropharm.2009.08.005. PMC 2813317. PMID 19699755.
- ^ Dykstra LA, Fischer BD, Balter RE, Henry FE, Schmidt KT, Miller LL (September 2011). "Opioid antinociception, tolerance and dependence: interactions with the N-methyl-D-aspartate system in mice". Behavioural Pharmacology. 22 (5–6): 540–7. doi:10.1097/FBP.0b013e328348ed08. PMC 3155647. PMID 21712708.
- ^ Bicca MA, Figueiredo CP, Piermartiri TC, Meotti FC, Bouzon ZL, Tasca CI, et al. (September 2011). "The selective and competitive N-methyl-D-aspartate receptor antagonist, (-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid, prevents synaptic toxicity induced by amyloid-β in mice". Neuroscience. 192: 631–41. doi:10.1016/j.neuroscience.2011.06.038. PMID 21756976. S2CID 36154501.
- v
- t
- e
Ionotropic glutamate receptor modulators
- 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
- SAGE-718
- Antagonists: Competitive antagonists: AP5 (APV)
- AP7
- CGP-37849
- CGP-39551
- CGP-39653
- CGP-40116
- CGS-19755
- CPP
- Kaitocephalin
- LY-233053
- LY-235959
- LY-274614
- MDL-100453
- Midafotel (d-CPPene)
- NPC-12626
- NPC-17742
- PBPD
- PEAQX
- Perzinfotel
- PPDA
- SDZ-220581
- Selfotel; Glycine site antagonists: 4-Cl-KYN (AV-101)
- 5,7-DCKA
- 7-CKA
- ACC
- ACEA-1011
- ACEA-1328
- Apimostinel (NRX-1074)
- AV-101
- Carisoprodol
- CGP-39653
- CNQX
- D-Cycloserine
- DNQX
- Felbamate
- Gavestinel
- GV-196771
- Harkoseride
- Kynurenic acid
- 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
- Diaminopropane
- Diethylenetriamine
- Huperzine A
- Putrescine; Uncompetitive pore blockers (mostly dizocilpine site): 2-MDP
- 3-HO-PCP
- 3-MeO-PCE
- 3-MeO-PCMo
- 3-MeO-PCP
- 4-MeO-PCP
- 8A-PDHQ
- 18-MC
- α-Endopsychosin
- Alaproclate
- Alazocine (SKF-10047)
- Amantadine
- Aptiganel
- Argiotoxin-636
- Arketamine
- ARL-12495
- ARL-15896-AR
- ARL-16247
- Budipine
- Coronaridine
- Delucemine (NPS-1506)
- Dexoxadrol
- Dextrallorphan
- Dextromethadone
- Dextromethorphan
- Dextrorphan
- Dieticyclidine
- Diphenidine
- Dizocilpine
- Ephenidine
- Esketamine
- Etoxadrol
- Eticyclidine
- Fluorolintane
- Gacyclidine
- Ibogaine
- Ibogamine
- Indantadol
- Ketamine
- Ketobemidone
- Lanicemine
- Levomethadone
- Levomethorphan
- Levomilnacipran
- Levorphanol
- Loperamide
- Memantine
- Methadone
- Methorphan
- Methoxetamine
- Methoxphenidine
- Milnacipran
- Morphanol
- NEFA
- Neramexane
- Nitromemantine
- Noribogaine
- Norketamine
- Orphenadrine
- PCPr
- PD-137889
- Pethidine (meperidine)
- Phencyclamine
- Phencyclidine
- Propoxyphene
- Remacemide
- Rhynchophylline
- Rimantadine
- Rolicyclidine
- Sabeluzole
- Tabernanthine
- Tenocyclidine
- Tiletamine
- Tramadol; Ifenprodil (NR2B) site antagonists:
- Besonprodil
- Buphenine (nylidrin)
- CO-101244 (PD-174494)
- Eliprodil
- Haloperidol
- Isoxsuprine
- Radiprodil (RGH-896)
- Rislenemdaz (CERC-301, MK-0657)
- Ro 8-4304
- Ro 25-6981
- Safaprodil
- 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
- Toluene
- Trichloroethane
- Trichloroethanol
- Trichloroethylene
- Urethane
- Xenon
- Xylene; Unknown/unsorted antagonists: ARR-15896
- Bumetanide
- Caroverine
- Conantokin
- 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