Gabapentin (hydrochloride)

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mg
ArtNr HY-A0057A-10mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
CAS No.
60142-95-2
Purity
>98%
MW
2076977
Formula
C9H18ClNO2
Solubility
10 mM in DMSO
Biological Description
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.
IC50 Value: 140 nM (alpha2delta subunit of calcium channel) [1]
Target: Calcium Channel
in vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release [2]. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%). Significantly, the gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 microM), at least in neocortical neurons (IC50 about 4 microM) [3].
in vivo: Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-alpha, 316.0 +/- 69.7 pg/mL vs 88.8 +/- 24.4 pg/mL; IL-1beta, 1, 212.9 +/- 104.5 vs 577.4 +/- 97.1 pg/mL; IL-6, 254.0 +/- 64.8 pg/mL vs 125.5 +/- 44.1 pg/mL; IL-10, 532.1 +/- 78.7 pg/mL vs 918.9 +/- 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody [4].
Toxicity: No new safety signals or adverse event trends relating to GEn exposure were identified [5].
Clinical trial: N/A
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HY-A0057A-10mg.pdf

Menge: 10mg
Lieferbar: In stock
Listenpreis: 99,29 €
Rabatt: -10,0%
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