Imagabalin

Chemical compound
  • None
Identifiers
  • (3S,5R)-3-amino-5-methyloctanoic acid
CAS Number
  • 610300-07-7
    610300-00-0 (hydrochloride)
PubChem CID
  • 10236037
ChemSpider
  • 8411525
UNII
  • NDG6931B7H
KEGG
  • D09627
CompTox Dashboard (EPA)
  • DTXSID00976534 Edit this at Wikidata
Chemical and physical dataFormulaC9H19NO2Molar mass173.256 g·mol−13D model (JSmol)
  • Interactive image
  • O=C(O)C[C@@H](N)C[C@@H](CCC)C
InChI
  • InChI=1S/C9H19NO2/c1-3-4-7(2)5-8(10)6-9(11)12/h7-8H,3-6,10H2,1-2H3,(H,11,12)/t7-,8+/m1/s1
  • Key:JXEHXYFSIOYTAH-SFYZADRCSA-N

Imagabalin (INN, USAN; PD-0332334) was an investigational drug that acts as a ligand for the α2δ subunit of the voltage-dependent calcium channel,[1] with some selectivity for the α2δ1 subunit over α2δ2.[2] It was under development by Pfizer as a pharmaceutical medication due to its hypothesized anxiolytic, analgesic, hypnotic, and anticonvulsant-like activity. It reached phase-III clinical trials for treatment of generalized anxiety disorder; however, the trials were terminated by the manufacturer.[3][4][5][6] The drug is no longer under development.

See also

References

  1. ^ Quintero JE, Pomerleau F, Huettl P, Johnson KW, Offord J, Gerhardt GA (July 2011). "Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology". Brain Research. 1401: 1–9. doi:10.1016/j.brainres.2011.05.025. PMC 3197737. PMID 21664606.
  2. ^ Larry Ereshefsky (2008). "Therapies in the Pipeline for Sleep Disorders: Focus on Novel Mechanisms and Disease Models" (PDF) (Press release). p. 11. Retrieved 2012-04-22.
  3. ^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{cite journal}}: Cite journal requires |journal= (help)
  4. ^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study Of PD 0332334 And Paroxetine Evaluating The Efficacy And Safety Of PD 0332334 For The Treatment Of Generalized Anxiety Disorder". {{cite journal}}: Cite journal requires |journal= (help)
  5. ^ Pfizer (2012-11-09). "A Phase 3, Randomized, Double-Blind, Parallel Group, 10-Week Placebo Controlled Fixed Dose Study of PD 0332334 and Paroxetine Evaluating the Efficacy and Safety of PD 0332334 for the Treatment of Generalized Anxiety Disorder". {{cite journal}}: Cite journal requires |journal= (help)
  6. ^ Pfizer (2012-11-09). "A 52-Week Open-Label Safety Study of PD 0332334 in Subjects With Generalized Anxiety Disorder". {{cite journal}}: Cite journal requires |journal= (help)
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5-HT1ARTooltip 5-HT1A receptor agonistsGABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulatorsHypnoticsGabapentinoids
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Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
  • GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
KCaTooltip Calcium-activated potassium channel
Blockers
  • BKCa-specific: Ethanol (alcohol)
  • GAL-021
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
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Sodium
VGSCsTooltip Voltage-gated sodium channels
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ENaCTooltip Epithelial sodium channel
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ASICsTooltip Acid-sensing ion channel
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CaCCsTooltip Calcium-activated chloride channel
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CFTRTooltip Cystic fibrosis transmembrane conductance regulator
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Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
  • See here instead.
LGICsTooltip Ligand gated ion channels
  • See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators


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