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Indantadol

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Indantadol
Clinical data
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • N-(2,3-dihydro-1H-inden-2-yl)glycinamide
CAS Number
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC11H14N2O
Molar mass190.246 g·mol−1
3D model (JSmol)
  • NCC(=O)NC1Cc2ccccc2C1

Indantadol (CHF-3381,V-3381) is adrug which was formerly being investigated as ananticonvulsant andneuroprotective and is now under development for the treatment ofneuropathic pain andchronic cough inEurope byVernalis andChiesi.[1][2][3][4][5][6][7][8] It acts as acompetitive,reversible, and non-selectivemonoamine oxidase inhibitor,[5][6][9] and as a lowaffinity,non-competitiveNMDA receptor antagonist.[1][2][10] Apilot study of indantadol for chronic cough was initiated in October 2009 and in April 2010 it failed to achieve significant efficacy in neuropathic pain inphase IIbclinical trials.[7][8][11][12]

See also

[edit]

References

[edit]
  1. ^abVilletti G, Bregola G, Bassani F, et al. (June 2001). "Preclinical evaluation of CHF3381 as a novel antiepileptic agent".Neuropharmacology.40 (7):866–78.doi:10.1016/S0028-3908(01)00026-0.PMID 11378157.S2CID 23709155.
  2. ^abGandolfi O, Bonfante V, Voltattorni M, et al. (September 2001). "Anticonvulsant preclinical profile of CHF 3381: dopaminergic and glutamatergic mechanisms".Pharmacology Biochemistry and Behavior.70 (1):157–66.doi:10.1016/S0091-3057(01)00591-3.PMID 11566153.S2CID 24029988.
  3. ^Zucchini S, Buzzi A, Bergamaschi M, Pietra C, Villetti G, Simonato M (November 2002). "Neuroprotective activity of CHF3381, a putative N-methyl-D-aspartate receptor antagonist".NeuroReport.13 (16):2071–4.doi:10.1097/00001756-200211150-00016.PMID 12438928.S2CID 32235961.
  4. ^Villetti G, Bergamaschi M, Bassani F, et al. (August 2003). "Antinociceptive activity of the N-methyl-D-aspartate receptor antagonist N-(2-Indanyl)-glycinamide hydrochloride (CHF3381) in experimental models of inflammatory and neuropathic pain".The Journal of Pharmacology and Experimental Therapeutics.306 (2):804–14.doi:10.1124/jpet.103.050039.PMID 12750440.S2CID 12703264.
  5. ^ab"CHF 3381".Drugs in R&D.5 (1):28–30. 2004.doi:10.2165/00126839-200405010-00005.PMID 14725488.S2CID 29253197.
  6. ^abMattia C, Coluzzi F (September 2007). "Indantadol, a novel NMDA antagonist and nonselective MAO inhibitor for the potential treatment of neuropathic pain".IDrugs: The Investigational Drugs Journal.10 (9):636–44.PMID 17786847.
  7. ^ab"IN-STEP Phase IIb study results". Archived fromthe original on 2014-08-13.
  8. ^ab"Vernalis initiates Pilot Study of V3381 in patients with chronic cough". Archived fromthe original on 2014-08-13.
  9. ^Mathiesen O, Imbimbo BP, Hilsted KL, Fabbri L, Dahl JB (August 2006)."CHF3381, a N-methyl-D-aspartate receptor antagonist and monoamine oxidase-A inhibitor, attenuates secondary hyperalgesia in a human pain model".The Journal of Pain.7 (8):565–74.doi:10.1016/j.jpain.2006.02.004.PMID 16885013.
  10. ^Barbieri M, Bregola G, Buzzi A, et al. (August 2003)."Mechanisms of action of CHF3381 in the forebrain".British Journal of Pharmacology.139 (7):1333–41.doi:10.1038/sj.bjp.0705381.PMC 1573965.PMID 12890713.
  11. ^"V3381CC". Archived fromthe original on 2014-08-13.
  12. ^"Vernalis completes recruitment in V3381 Phase II IN-STEP study for neuropathic pain". Archived fromthe original on 2014-08-13.
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AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
Non-specific
AAADTooltip Aromatic L-amino acid decarboxylase
MAOTooltip Monoamine oxidase
Phenethylamines
(dopamine,epinephrine,
norepinephrine)
PAHTooltip Phenylalanine hydroxylase
THTooltip Tyrosine hydroxylase
DBHTooltip Dopamine beta-hydroxylase
PNMTTooltip Phenylethanolamine N-methyltransferase
COMTTooltip Catechol-O-methyl transferase
Tryptamines
(serotonin,melatonin)
TPHTooltip Tryptophan hydroxylase
AANATTooltip Serotonin N-acetyl transferase
ASMTTooltip Acetylserotonin O-methyltransferase
Histamine
HDCTooltip Histidine decarboxylase
HNMTTooltip Histamine N-methyltransferase
DAOTooltip Diamine oxidase
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