Gabapentin Inhibitor CAS No. 60142-96-3

Cat. No.	Name	Size	Price	Add Cart
KI0946	Gabapentin	25 mg	$112
KI0946	Gabapentin	100 mg	$336

Chemical Characteristic

Product Name	Gabapentin
Synonyms	CI-945, Neurontin
CAS No.	60142-96-3
Molecular Weight	171.24
Formula	C₉H₁₇NO₂
Chemical Structure

Biological activities

Gabapentin is a γ-aminobutyric acid-B (GABAB) receptor agonist. Gabapentin inhibits [³H] GABA binding in a GABAB receptor-selective binding assay. Gabapentin inhibits the high K⁺-evoked activation of voltage-dependent calcium channels in a murine mIL-tsA58 cell line. Gabapentin exhibits an efficacy at the GABA_{B(1a,2) heterodimer with an EC50 of 15 µM.^[1] Gabapentin is effective in the treatment of pain and sleep interference associated with postherpetic neuralgis (PHN). ^[2] Gabapentin can bind to the α_{2δ subunit of voltage-dependent calcium channels with an IC50 of 80 nM. ^[3] In vivo, gabapentin inhibits transient lower esophageal sphincter relaxations in Labrador retriever dogs. ^[1] In the rat formalin test, gabapentin (10 - 300 mg kg-1) dose-dependently inhibits the late phase of the nociceptive response with respective minimum effective doses (MED) of 10 and 30 mg kg-1, s.c. The intrathecal administration of gabapentin dose-dependently (1-100 µg/animal) blocks carrageenan- induced mechanical hyperalgesia. ^[3]}}

References

[1] Jensen AA, et al. The anticonvulsant gabapentin (neurontin) does not act through gamma-aminobutyric acid-B receptors. Mol Pharmacol. 2002, 61(6): 1377-1384. 閵嗏偓閵嗏偓 [2] Rowbotham M, et al. Gabapentin for the treatment of postherpetic neuralgia: a randomized controlled trial. JAMA. 1998, 280(21): 1837-1842. 閵嗏偓閵嗏偓 [3] Field MJ, Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents. Br J Pharmacol. 1997, 121(8): 1513-1522. 閵嗏偓閵嗏偓

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