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Lu Ae58054 Information

Lu AE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.[1][2] As of February 2010 it is in phase II clinical trials.[2]

References

  1. ^ "U.S. Development Programs. - Lundbeck". http://www.lundbeckinc.com/usa/pipeline/default.asp.
  2. ^ a b "Search of: Lu AE58054 - List Results - ClinicalTrials.gov". http://clinicaltrials.gov/ct2/results?term=Lu+AE58054.

External links

Psychoanaleptics: Antidementia agents (N06D)
Anticholinesterases CymserineDonepezilGalantamineHuperzine A (Huperzia serrata) • LadostigilRivastigmineTacrine
Others BifemelaneBilobalide (Ginkgo biloba) • CerlapirdineEnsaculinLatrepirdineLecozotanLeteprinimMemantineSemagacestat

: PSO/PSI

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Nootropics (N06B)
Acetylcholinesterases DonepezilGalantamineHuperzine A (Huperzia Serrata) • LadostigilRivastigmineTacrine
Ampakines CX-516CX-546CX-614CX-691CX-717IDRA-21LY-404,187LY-503,430PEPASunifiramUnifiram
D1 Agonists 6-Br-APBA-77636DihydrexidineDinapsolineDoxanthrineSKF-81297
Eugeroics AdrafinilArmodafinilModafinil
GABAA α5 Inverse Agonists α5IAL-655,708PWZ-029SuritozoleTB-21007ZK-93426
H3 Antagonists A-349,821ABT-239CiproxifanGSK-189,254
mACh Agonists AlvamelineArecolineCevimelineCI-1017MilamelineSabcomelineTalsaclidineTazomelineXanomeline
nACh Agonists AR-R17779IsproniclineNicotinePNU-282,987SSR-180,711WAY-317,538
Racetams AniracetamBrivaracetamColuracetamEtiracetamFasoracetamLevetiracetamNebracetamNefiracetamOxiracetamPhenylpiracetamPiracetamPramiracetamRolziracetamSeletracetam
Others AcetylcarnitineAdafenoxateBifemelaneBilobalide (Ginkgo Biloba) • CarbenoxoloneCerlapirdineCholine (Lecithin) • CiticolineCyprodenateDimethylethanolamineEnsaculinFipexideIdebenoneIndeloxazineLatrepirdineLeteprinimLinopirdineMeclofenoxateNizofenonePirisudanolPyritinolS-17092SulbutiamineTaltirelinTeniloxazineTricyanoaminopropeneVinpocetine
Serotonergics
5-HT1 receptor ligands
5-HT1A Agonists: Azapirones: AlnespironeBinospironeBuspironeEnilospironeEptapironeGepironeIpsapironePerospironeRevospironeTandospironeTiospironeUmespironeZalospirone; Antidepressants: EtoperidoneNefazodoneTrazodoneVortioxetine; Antipsychotics: AripiprazoleAsenapineClozapineQuetiapineZiprasidone; Ergolines: DihydroergotamineErgotamineLisurideMethysergideLSD; Tryptamines: 5-CT5-MeO-DMT5-MTBufoteninDMTIndorenatePsilocinPsilocybin; Others: 8-OH-DPATAdatanserinBay R 1531BefiradolBMY-14802CannabidiolDimemebfeEbalzotanEltoprazine • F-11,461 • F-12,826 • F-13,714 • F-14,679 • F-15,063F-15,599FlesinoxanFlibanserinLesopitronLY-293,284 • LY-301,317 • MKC-242NBUMPOsemozotanOxaflozanePardoprunoxPiclozotanRauwolscineRepinotanRoxindoleRU-24,969 • S 14,506 • S-14,671S-15,535Sarizotan • SSR-181,507 • SunepitronU-92,016-AUrapidilVilazodoneXaliprodenYohimbine Antagonists: Antipsychotics: IloperidoneRisperidoneSertindole; Beta blockers: AlprenololCyanopindololIodocyanopindololOxprenolol • Pindobind • PindololPropranololTertatolol; Others: AV965 • BMY-7,378CSP-2503DotarizineFlopropione • GR-46611 • IsamoltaneLecozotanMefwayMetitepine/MethiothepinMPPFNAN-190PRX-00023RobalzotanS-15535SB-649,915 • SDZ 216-525 • SpiperoneSpiramideSpiroxatrineUH-301WAY-100,135WAY-100,635Xylamidine
5-HT1B Agonists: Lysergamides: DihydroergotamineErgotamineMethysergide; Piperazines: EltoprazineTFMPP; Triptans: AvitriptanEletriptanSumatriptanZolmitriptan; Tryptamines: 5-CT5-MT; Others: CGS-12066ACP-93,129CP-94,253CP-135,807RU-24,969Vortioxetine Antagonists: Lysergamides: Metergoline; Others: AR-A000002ElzasonanGR-127,935IsamoltaneMetitepine/MethiothepinSB-216,641 • SB-224,289 • SB-236,057 • Yohimbine
5-HT1D Agonists: Lysergamides: DihydroergotamineMethysergide; Triptans: AlmotriptanAvitriptanEletriptanFrovatriptanNaratriptanRizatriptanSumatriptanZolmitriptan; Tryptamines: 5-CT5-Ethyl-DMT5-MT5-(Nonyloxy)tryptamine; Others: CP-135,807 • CP-286,601 • GR-46611 • L-694,247 • L-772,405 • PNU-109,291 • PNU-142,633 Antagonists: Lysergamides: Metergoline; Others: AlniditanBRL-15,572ElzasonanGR-127,935KetanserinLY-310,762 • LY-367,642 • LY-456,219 • LY-456,220 • Metitepine/MethiothepinRitanserinYohimbineZiprasidone
5-HT1E Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: BRL-54443Tryptamine Antagonists: Metitepine/Methiothepin
5-HT1F Agonists: Triptans: EletriptanNaratriptanSumatriptan; Tryptamines: 5-MT; Others: BRL-54443LasmiditanLY-334,370 Antagonists: Metitepine/Methiothepin
5-HT2 receptor ligands
5-HT2A Agonists: Lysergamides: ALD-52ErgometrineLisurideLA-SS-AzLSDLSD-PipLysergic acid 2-butyl amideLysergic acid 3-pentyl amideMethysergide; Phenethylamines: 25I-NBF25I-NBMD25I-NBOH25I-NBOMe2C-B2C-B-FLY2CB-Ind2C-C-NBOMe2C-E2C-I2C-TFM-NBOMe2C-T-22C-T-72C-T-212CBCB-NBOMe2CBFly-NBOMeBromo-DragonFLYDOBDOCDOIDOMMDAMDMAMescalineTCB-2TFMFly; Piperazines: BZPQuipazineTFMPP; Tryptamines: 5-CT5-MeO-α-ET5-MeO-α-MT5-MeO-DET5-MeO-DiPT5-MeO-DMT5-MeO-DPT5-MTα-ETα-Methyl-5-HTα-MTBufoteninDETDiPTDMTDPTPsilocinPsilocybin; Others: AL-34662AL-37350ADimemebfeMedifoxamineOxaflozanePNU-22394RH-34 Antagonists: Atypical antipsychotics: AmperozideAripiprazoleCarpipramineClocapramineClorotepineClozapineGevotrolineIloperidoneMelperoneMosapramineOlanzapinePaliperidonePimozideQuetiapineRisperidoneSertindoleZiprasidoneZotepine; Typical antipsychotics: LoxapinePipamperone; Antidepressants: AmitriptylineAmoxapineAptazapineEtoperidoneMianserinMirtazapineNefazodoneTeniloxazineTrazodone; Others: 5-I-R911505-MeO-NBpBrT • AC-90179 • AdatanserinAltanserinAMDA • APD-215 • BlonanserinCinanserinCSP-2503CyproheptadineDeramciclaneDotarizineEplivanserinEsmirtazapineFananserinFlibanserinKetanserinKML-010LubazodoneMepiprazoleMetitepine/MethiothepinNanteninePimavanserinPizotifenPruvanserinRauwolscineRitanserinS-14,671SarpogrelateSetoperoneSpiperoneSpiramide • SR-46349B • VolinanserinXylamidineYohimbine
5-HT2B Agonists: Oxazolines: 4-MethylaminorexAminorex; Phenethylamines: ChlorphentermineCloforexDOBDOCDOIDOMFenfluramineMDAMDMANorfenfluramine; Tryptamines: 5-CT5-MTα-Methyl-5-HT; Others: BW-723C86CabergolinemCPPPergolidePNU-22394Ro60-0175 Antagonists: AgomelatineAsenapine • EGIS-7625 • KetanserinLisurideLY-272,015Metitepine/MethiothepinPRX-08066RauwolscineRitanserinRS-127,445Sarpogrelate • SB-200,646 • SB-204,741SB-206,553SB-215,505 • SB-221,284 • SB-228,357 • SDZ SER-082TegaserodYohimbine
5-HT2C Agonists: Phenethylamines: 2C-B2C-E2C-I2C-T-22C-T-72C-T-21DOBDOCDOIDOMMDAMDMAMescaline; Piperazines: AripiprazolemCPPTFMPP; Tryptamines: 5-CT5-MeO-α-ET5-MeO-α-MT5-MeO-DET5-MeO-DiPT5-MeO-DMT5-MeO-DPT5-MTα-ETα-Methyl-5-HTα-MTBufoteninDETDiPTDMTDPTPsilocinPsilocybin; Others: A-372,159AL-38022ACP-809,101DimemebfeLorcaserinMedifoxamine • MK-212 • Org 12,962ORG-37,684OxaflozanePNU-22394Ro60-0175Ro60-0213VabicaserinWAY-629WAY-161,503YM-348 Antagonists: Atypical antipsychotics: ClorotepineClozapineIloperidoneMelperoneOlanzapinePaliperidonePimozideQuetiapineRisperidoneSertindoleZiprasidoneZotepine; Typical antipsychotics: ChlorpromazineLoxapinePipamperone; Antidepressants: AgomelatineAmitriptylineAmoxapineAptazapineEtoperidoneFluoxetineMianserinMirtazapineNefazodoneNortriptylineTedatioxetineTrazodone; Others: AdatanserinCinanserinCyproheptadineDeramciclaneDotarizineEltoprazineEsmirtazapine • FR-260,010 • KetanserinKetotifenLatrepirdineMetitepine/MethiothepinMethysergidePizotifenRitanserinRS-102,221S-14,671 • SB-200,646 • SB-206,553 • SB-221,284 • SB-228,357 • SB-242,084 • SB-243,213 • SDZ SER-082Xylamidine
5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7 ligands
5-HT3 Agonists: Piperazines: BZPQuipazine; Tryptamines: 2-Methyl-5-HT5-CT; Others: ChlorophenylbiguanideButanolEthanolHalothaneIsofluraneRS-56812 • SR-57,227 • SR-57,227-A • TolueneTrichloroethaneTrichloroethanolTrichloroethyleneYM-31636 Antagonists: Antiemetics: AS-8112AlosetronAzasetronBatanoprideBemesetronCilansetronDazoprideDolasetronGranisetronLerisetronOndansetronPalonosetronRamosetronRenzaprideTropisetronZacoprideZatosetron; Atypical antipsychotics: ClozapineOlanzapineQuetiapine; Tetracyclic antidepressants: AmoxapineMianserinMirtazapine; Others: CSP-2503 • ICS-205,930 • MDL-72,222 • MemantineNitrous OxideRicasetronSevofluraneTedatioxetineThujoneVortioxetineXenon
5-HT4 Agonists: Gastroprokinetic Agents: CinitaprideCisaprideDazoprideMetoclopramideMosapridePrucaloprideRenzaprideTegaserodVelusetragZacopride; Others: 5-MTBIMU8CJ-033,466PRX-03140RS-67333 • RS-67506 • SL65.0155Antagonists: GR-113,808 • GR-125,487 • L-LysinePiboserod • RS-39604 • RS-67532 • SB-203,186 • SB-204,070
5-HT5A Agonists: Lysergamides: ErgotamineLSD; Tryptamines: 5-CT; Others: Valerenic Acid Antagonists: AsenapineLatrepirdineMetitepine/MethiothepinRitanserinSB-699,551 * Note that the 5-HT5B receptor is not functional in humans.
5-HT6 Agonists: Lysergamides: DihydroergotamineErgotamineLisurideLSDMesulergineMetergolineMethysergide; Tryptamines: 2-Methyl-5-HT5-BT5-CT5-MTBufoteninE-6801E-6837EMD-386,088EMDT • LY-586,713 • N-Methyl-5-HT • Tryptamine; Others: WAY-181,187WAY-208,466 Antagonists: Antidepressants: AmitriptylineAmoxapineClomipramineDoxepinMianserinNortriptyline; Atypical antipsychotics: AripiprazoleAsenapineClorotepineClozapineFluperlapineIloperidoneOlanzapineTiospirone; Typical antipsychotics: ChlorpromazineLoxapine; Others: BGC20-760 • BVT-5182 • BVT-74316 • CerlapirdineEGIS-12,233 • GW-742,457 • KetanserinLatrepirdineLu AE58054Metitepine/MethiothepinMS-245PRX-07034RitanserinRo04-6790 • Ro 63-0563 • SB-258,585SB-271,046SB-357,134SB-399,885SB-742,457
5-HT7 Agonists: Lysergamides: LSD; Tryptamines: 5-CT5-MTBufotenin; Others: 8-OH-DPATAS-19BifeprunoxE-55888LP-12LP-44RU-24,969Sarizotan Antagonists: Lysergamides: 2-Bromo-LSDBromocriptineDihydroergotamineErgotamineMesulergineMetergolineMethysergide; Antidepressants: AmitriptylineAmoxapineClomipramineImipramineMaprotilineMianserin; Atypical antipsychotics: AmisulprideAripiprazoleClorotepineClozapineOlanzapineRisperidoneSertindoleTiospironeZiprasidoneZotepine; Typical antipsychotics: ChlorpromazineLoxapine; Others: ButaclamolEGIS-12,233Ketanserin • LY-215,840 • Metitepine/MethiothepinPimozideRitanserinSB-258,719 • SB-258,741 • SB-269,970 • SB-656,104 • SB-656,104-A • SB-691,673 • SLV-313 • SLV-314 • Spiperone • SSR-181,507 • Vortioxetine
Reuptake inhibitors
SERT Selective serotonin reuptake inhibitors (SSRIs): AlaproclateCitalopramDapoxetineDesmethylcitalopramDesmethylsertralineEscitalopramFemoxetineFluoxetineFluvoxamineIndalpineIfoxetineLitoxetineLubazodonePanuramineParoxetinePirandamineRTI-353SeproxetineSertralineTedatioxetineVilazodoneVortioxetineZimelidine; Serotonin-norepinephrine reuptake inhibitors (SNRIs): BicifadineDesvenlafaxineDuloxetineEclanamineLevomilnacipranMilnacipranSibutramineVenlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors (SNDRIs): BrasofensineDiclofensineDOV-102,677DOV-21,947DOV-216,303NS-2359SEP-225289SEP-227,162Tesofensine; Tricyclic antidepressants (TCAs): AmitriptylineButriptylineCianopramineClomipramineDesipramineDosulepinDoxepinImipramineLofepramineNortriptylinePipofezineProtriptylineTrimipramine; Tetracyclic antidepressants (TeCAs): Amoxapine; Piperazines: NefazodoneTrazodone; Antihistamines: BrompheniramineChlorphenamineDiphenhydramineMepyramine/PyrilaminePheniramineTripelennamine; Opioids: PethidineMethadonePropoxyphene; Others: CocaineCP-39,332CyclobenzaprineDextromethorphanDextrorphanEXP-561FezolamineMesembrineNefopamPIM-35PridefineRoxindoleSB-649,915Ziprasidone
VMAT IbogaineReserpineTetrabenazine
Releasing agents
Aminoindanes: 5-IAIAMMIETAIMDAIMDMAIMMAITAI; Aminotetralins: 6-CAT8-OH-DPATMDATMDMAT; Oxazolines: 4-MethylaminorexAminorexClominorexFluminorex; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Methyl-MDA4-CAB4-FA4-FMA4-HA4-MTA5-APDB5-Methyl-MDA6-APDB6-Methyl-MDA • AEMMA • AmiflamineBDBBOHBrephedroneButyloneChlorphentermineCloforexAmfepramoneMetamfepramoneDCADFMDADMADMMAEBDBEDMAEthyloneEtolorexFenfluramine (Dexfenfluramine) • FlephedroneIAPIMPLophophineMBDBMDAMDEAMDHMAMDMAMDMPEAMDOHMDPEAMephedroneMethedroneMethyloneMMAMMDAMMDMA • MMMA • NAPNorfenfluramine • 4-TFMA • pBApCApIAPMAPMEAPMMATAP; Piperazines: 2C-B-BZP • 2-BZP • 3-MeOPP • BZP • DCPP • MBZPmCPPMDBZPMeOPPMepiprazolepCPPpFPPpTFMPPTFMPP; Tryptamines: 4-Methyl-αET4-Methyl-αMT5-CT5-MeO-αET5-MeO-αMT5-MTαETαMTDMTTryptamine (itself); Others: IndeloxazineTramadolViqualine
Enzyme inhibitors
Anabolism
TPH AGN-2979Fenclonine
AAAD BenserazideCarbidopaGenisteinMethyldopa
Catabolism
MAO Nonselective: BenmoxinCaroxazoneEchinopsidineFurazolidoneHydralazineIndantadolIproclozideIproniazidIsocarboxazidIsoniazidLinezolidMebanazineMetfendrazineNialamideOctamoxinParaxazonePhenelzinePheniprazinePhenoxypropazinePivalylbenzhydrazineProcarbazineSafrazineTranylcypromine; MAO-A Selective: AmiflamineBazinaprineBefloxatoneBefolBrofaromineCimoxatoneClorgilineEsuproneHarmala alkaloids (Harmine, Harmaline, Tetrahydroharmine, Harman, Norharman, etc) • Methylene BlueMetralindoleMinaprineMoclobemidePirlindoleSercloremineTetrindoleToloxatoneTyrima
Others
Precursors L-Tryptophan5-HTP
Cofactors Ferrous iron (Fe2+) • Magnesium (Mg2+) • TetrahydrobiopterinVitamin B3 (Niacin, NicotinamideNADPH) • Vitamin B6 (Pyridoxine, Pyridoxamine, PyridoxalPyridoxal phosphate) • Vitamin B9 (Folic AcidTetrahydrofolic acid) • Vitamin C (Ascorbic acid) • Zinc (Zn2+)
Others Activity enhancers: BPAPPPAP; Reuptake enhancers: Tianeptine

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