Aplindore

Aplindore
Clinical data

ATC code	none
Identifiers
IUPAC name (2S)-2-[(phenylmethylamino)methyl]-2,3,7,9-tetrahydro-[1,4]dioxino[3,2-e]indol-8-one
CAS Number	189681-71-8^Y
PubChem CID	6440763
ChemSpider	139676^Y
UNII	Q5O76TA0ML
KEGG	D03214^Y
ChEMBL	CHEMBL2110659^N
Chemical and physical data
Formula	C₁₈H₁₈N₂O₃
Molar mass	310.346 g/mol
3D model (JSmol)	Interactive image
SMILES c4ccccc4CNCC(CO2)Oc1c2ccc(N3)c1CC3=O
InChI InChI=1S/C18H18N2O3/c21-17-8-14-15(20-17)6-7-16-18(14)23-13(11-22-16)10-19-9-12-4-2-1-3-5-12/h1-7,13,19H,8-11H2,(H,20,21)/t13-/m0/s1^Y Key:DYJIKHYBKVODAC-ZDUSSCGKSA-N^Y
^NY (what is this?) (verify)

Aplindore (DAB-452) is a drug which acts as a partial agonist selective for the dopamine receptor D2.^[1] It is being developed by the pharmaceutical company Neurogen as a treatment for Parkinson's disease and restless legs syndrome.

On December 23rd 2009 Neurogen was acquired by Ligand Pharmaceuticals. Rights to Aplindore were given to Ligand around time of merger. As of 2008, Phase II was completed and Ligand.

Upon reviewing company website (Ligand.com) this drug is currently not listed at the moment due to several programs already partnered with GSK. GSK holds a significant share of the drug RLS drug programs on the market with Requip XR and the recent FDA approval of Horizant. To prevent any direct competition and losing strong ties with GSK, Aplindore is not listed at the moment on Lidgand website. If this medication were to reach phase III, this could adversely effect Ligand`s portfolio of partnered and unpartnered assets. By electing not to list the drug on company website, Ligand maintains the appearance that they are "currently actively seeking a partner" when a potential investor inquirers about drug development via email.

References

↑ Heinrich JN, Brennan J, Lai MH, Sullivan K, Hornby G, Popiolek M, Jiang LX, Pausch MH, Stack G, Marquis KL, Andree TH. Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist. European Journal of Pharmacology. 2006 Dec 15;552(1-3):36-45. PMID 17056032

Antiparkinson agents (N04)

Dopaminergics

DA precursors/prodrugs	Levodopa^# Melevodopa
DA receptor agonists	Apomorphine Bromocriptine Cabergoline Dihydroergocryptine Lisuride Pergolide Piribedil Pramipexole Ropinirole Rotigotine
MAO-B inhibitors	Rasagiline Selegiline
COMT inhibitors	Entacapone Opicapone Tolcapone
AAAD inhibitors	Benserazide Carbidopa^#

Anticholinergics

Others

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Dopamine receptor modulators

D₁-like

Agonists

Benzazepines 6-Br-APB Fenoldopam SKF-38,393 SKF-77,434 SKF-81,297 SKF-82,958 SKF-83,959 Trepipam Zelandopam
Ergolines Cabergoline CY-208,243 Dihydroergocryptine LEK-8829 Lisuride Pergolide Terguride
Dihydrexidine derivatives A-77636 A-86929 Adrogolide (ABT-431, DAS-431) Dihydrexidine Dinapsoline Dinoxyline Doxanthrine
Phenethylamines BCO-001 Deoxyepinephrine (N-methyldopamine, epinine) Dopexamine Etilevodopa Ibopamine L-DOPA (levodopa) Melevodopa L-Phenylalanine L-Tyrosine XP21279
Others A-68930 Apomorphine Isocorypalmine Nuciferine PF-6649751 PF 6669571 Propylnorapomorphine Rotigotine SKF-89,145 SKF-89,626 Stepholidine Tetrahydropalmatine

Antagonists

Typical antipsychotics Butaclamol Chlorpromazine Chlorprothixene Flupentixol (flupenthixol) (+melitracen) Fluphenazine Loxapine Perphenazine (+amitriptyline) Pifluthixol Thioridazine Thiothixene Trifluoperazine (+tranylcypromine) Zuclopenthixol
Atypical antipsychotics Asenapine Clorotepine Clotiapine Clozapine DHA-clozapine Fluperlapine Iloperidone Norclozapine Norquetiapine Olanzapine (++fluoxetine) Paliperidone Quetiapine Risperidone Tefludazine Zicronapine Ziprasidone Zotepine
Others Berupipam Ecopipam EEDQ Metitepine (methiothepin) Odapipam SCH-23390

D₂-like

Agonists

Adamantanes Amantadine Memantine Rimantadine
Aminotetralins 5-OH-DPAT 7-OH-DPAT 8-OH-PBZI Rotigotine UH-232
Ergolines Bromocriptine Cabergoline Dihydroergocryptine Epicriptine Lisuride LSD Pergolide Terguride
Dihydrexidine derivatives 2-OH-NPA Ciladopa Dihydrexidine Dinoxyline N,N-Propyldihydrexidine
Phenethylamines Deoxyepinephrine (N-methyldopamine, epinine) Dopexamine Etilevodopa Ibopamine L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Melevodopa XP21279
Atypical antipsychotics Alentemol (U-66444B) Aripiprazole (+sertraline) Aripiprazole lauroxil Bifeprunox Brexpiprazole Cariprazine F-15063 Lumateperone Norclozapine RP5063
Others A-412,997 ABT-670 ABT-724 Adrafinil Aplindore Apomorphine Arketamine Armodafinil BP-897 Captodiame CP-226,269 Dizocilpine Esketamine Flibanserin GSK-789,472 Ketamine Mesulergine Modafinil OSU-6162 Pardoprunox PD-128,907 PD-168,077 PF-219,061 PF-592,379 Phencyclidine Piribedil Pramipexole Propylnorapomorphine Pukateine Quinagolide Quinelorane Quinpirole RDS-127 Ro10-5824 Ropinirole Roxindole Salvinorin A SKF-83,959 Sumanirole Talipexole Umespirone WAY-100,635

Antagonists

Typical antipsychotics Acepromazine Acetophenazine Azaperone Benperidol Bromperidol Butaclamol Butaperazine Chloracizine Chlorproethazine Chlorpromazine Chlorprothixene Ciclindole Clopenthixol Clothixamide Clopimozide Droperidol Fluacizine Fluanisone Flucindole Fluotracen Flupentixol (flupenthixol) (+melitracen) Fluphenazine Fluprothixene Fluspirilene Haloperidol Homopipramol Lenperone Levomepromazine (methotrimeprazine) Levosulpiride Loxapine Mesoridazine Moperone Naranol Nemonapride Penfluridol Perathiepin Perazine Pericyazine (periciazine) Perphenazine (+amitriptyline) Piflutixol (pifluthixol) Pimozide Pipamperone Prochlorperazine Promazine Prothipendyl Spiperone (spiroperidol) Sulforidazine Sulpiride Sultopride Teflutixol Thiopropazate Thioproperazine Thioridazine Thiothixene Timiperone Trifluoperazine (+tranylcypromine) Triflupromazine Trifluperidol Zetidoline Zuclopenthixol
Atypical antipsychotics Amisulpride Asenapine BL-1020 Blonanserin Carpipramine Cinuperone Clocapramine Clorotepine Clotiapine (clothiapine) Clozapine Cyamemazine DHA-clozapine Dixyrazine Elopiprazole Flumezapine Fluperlapine Gevotroline Iloperidone Lurasidone Mazapertine Melperone Molindone Mosapramine Ocaperidone Olanzapine (+fluoxetine) Paliperidone Perospirone Piperacetazine Pipotiazine Piquindone Quetiapine Remoxipride Risperidone Sertindole Tefludazine Tenilapine Tiospirone Veralipride Zicronapine Ziprasidone Zotepine
Antiemetics/gastroprokinetics/sedatives Aceprometazine AS-8112 Alimemazine Alizapride Benzquinamide Bromopride Clebopride Domperidone Eticlopride Hydroxyzine Itopride Metoclopramide Metopimazine Promethazine Thiethylperazine Trimethobenzamide
Antidepressants Amoxapine Nefazodone Opipramol Propiomazine Trimipramine
Others Azapride Buspirone Desmethoxyfallypride EEDQ F-15063 Fallypride Fananserin Fenfluramine GSK-789,472 Iodobenzamide Isocorypalmine L-741,626 L-745,870 Levofenfluramine LEK-8829 Metergoline Metitepine (methiothepin) N-Methylspiperone Nafadotride Nuciferine PNU-99,194 Pridopidine Raclopride Sarizotan SB-277,011-A Seridopidine Sonepiprazole Spiroxatrine Stepholidine SV-293 Tetrahydropalmatine Tiapride UH-232 Yohimbine

See also: Receptor/signaling modulators

Adrenergics

Serotonergics

Monoamine reuptake inhibitors

Monoamine releasing agents

Monoamine metabolism modulators

Monoamine neurotoxins

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