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Wikipedia

Aplindore

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.

Aplindore
Clinical data
ATC code
  • none
Identifiers
  • (2S)-2-[(phenylmethylamino)methyl]-2,3,7,9-tetrahydro-[1,4]dioxino[3,2-e]indol-8-one
CAS Number
  • 189681-70-7 Y
  • fumarate: 189681-71-8 Y
PubChem CID
  • 6440763
ChemSpider
  • 139676 Y
UNII
  • Q5O76TA0ML
  • fumarate: P13TV5A758 Y
KEGG
  • D03214 Y
ChEMBL
  • ChEMBL2110659 N
Chemical and physical data
FormulaC18H18N2O3
Molar mass310.353 g·mol−1
3D model (JSmol)
  • Interactive image
  • c4ccccc4CNCC(CO2)Oc1c2ccc(N3)c1CC3=O
  • 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)

On December 23, 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 edit

  1. ^ Heinrich JN, Brennan J, Lai MH, Sullivan K, Hornby G, Popiolek M, Jiang LX, Pausch MH, Stack G, Marquis KL, Andree TH (December 2006). "Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist". European Journal of Pharmacology. 552 (1–3): 36–45. doi:10.1016/j.ejphar.2006.08.063. PMID 17056032.

aplindore, drug, which, acts, partial, agonist, selective, dopamine, receptor, being, developed, pharmaceutical, company, neurogen, treatment, parkinson, disease, restless, legs, syndrome, clinical, dataatc, codenoneidentifiersiupac, name, phenylmethylamino, m. 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 AplindoreClinical dataATC codenoneIdentifiersIUPAC name 2S 2 phenylmethylamino methyl 2 3 7 9 tetrahydro 1 4 dioxino 3 2 e indol 8 oneCAS Number189681 70 7 Yfumarate 189681 71 8 YPubChem CID6440763ChemSpider139676 YUNIIQ5O76TA0MLfumarate P13TV5A758 YKEGGD03214 YChEMBLChEMBL2110659 NChemical and physical dataFormulaC 18H 18N 2O 3Molar mass310 353 g mol 13D model JSmol Interactive imageSMILES c4ccccc4CNCC CO2 Oc1c2ccc N3 c1CC3 OInChI 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 YKey DYJIKHYBKVODAC ZDUSSCGKSA N Y N Y what is this verify On December 23 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 edit Heinrich JN Brennan J Lai MH Sullivan K Hornby G Popiolek M Jiang LX Pausch MH Stack G Marquis KL Andree TH December 2006 Aplindore DAB 452 a high affinity selective dopamine D2 receptor partial agonist European Journal of Pharmacology 552 1 3 36 45 doi 10 1016 j ejphar 2006 08 063 PMID 17056032 Retrieved from https en wikipedia org w index php title Aplindore amp oldid 1121721859, wikipedia, wiki, book, books, library,

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