• #LGM Pharma is a Gabapentin Enacarbil CAS# 478296-72-9 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
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  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 478296-72-9
  • AHFC code:
  • Synonyms: ASP 8825, ASP8825, Gabapentin enacarbil, GSK 1838262, GSK1838262, Horizant, Regnite, Solzira, UNII-75OCL1SPBQ, XP 13512, XP-13512, XP13512
  • ATC Code:
  • Chemical Formula: C16-H27-N-O6
  • Molecular Weight: 329.3903
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB08872
  • SMILES: CC(C)C(=O)OC(C)OC(=O)NCC1(CCCCC1)CC(=O)O
  • InChl: 1S/C16H27NO6/c1-11(2)14(20)22-12(3)23-15(21)17-10-16(9-13(18)19)7-5-4-6-8-16/h11-12H,4-10H2,1-3H3,(H,17,21)(H,18,19)
  • PubChem: 9883933
  • IUPAC: 1-(((alpha-isobutanoyloxyethoxy)carbonyl)aminomethyl)-1-cyclohexaneacetic acid

Additional Details

Indication:
For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Pharmacodynamics:
Since gabapentin enacarbil is a prodrug of gabapentin, it’s physiological effects are the same as gabapentin. Concerning PHN, gabapentin prevents allodynia and hyperalgesia.
Mode of Action:
Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Metabolism:
Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.
Toxicity:
Most common adverse reactions are headache, dizziness, and somnolence.
General Reference:
Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. [PubMed:15146029 ]
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