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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Neuronal Signaling>GABA Receptor agonists>Gabapentin (hydrochloride)
Gabapentin (hydrochloride)
  • Gabapentin (hydrochloride)

Gabapentin (hydrochloride)

Price $1
Package 1g
Min. Order: 1g
Supply Ability: 1ton
Update Time: 2020-01-13

Product Details

Product Name: Gabapentin (hydrochloride) CAS No.: 60142-95-2
EC-No.: 200-258-5 Min. Order: 1g
Purity: 99% Supply Ability: 1ton
Release date: 2020/01/13
contact: Mary@coreychem.com
Common Name
Gabapentin (hydrochloride)
CAS Number
60142-95-2
Molecular Weight
207.69800
Density
N/A
Boiling Point
314.4ºC at 760mmHg
Molecular Formula
C9H18ClNO2
Melting Point
148-151℃ (ethanol )
MSDS
N/A
Flash Point
144ºC

 Use of Gabapentin (hydrochloride)

 
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 (α2δ subunit of calcium channel) [1]Target: Calcium Channelin 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-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 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

 Names

Name
2-[1-(aminomethyl)cyclohexyl]acetic acid,hydrochloride
Synonym
More Synonyms

 Gabapentin (hydrochloride) Biological Activity

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 (α2δ subunit of calcium channel) [1]Target: Calcium Channelin 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-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 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
Related Catalog
Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel
Research Areas >> Neurological Disease
References

[1]. Receveur JM, et al. Synthesis and biological evaluation of conformationally restricted Gabapentin analogues. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2329-34.

[2]. Parker DA, et al. Gabapentin activates presynaptic GABAB heteroreceptors in rat cortical slices. Eur J Pharmacol. 2004 Jul 14;495(2-3):137-43.

[3]. Stefani A, et al. Gabapentin inhibits calcium currents in isolated rat brain neurons. Neuropharmacology. 1998;37(1):83-91.

[4]. Lee BS, et al. Intrathecal gabapentin increases interleukin-10 expression and inhibits pro-inflammatory cytokine in a rat model of neuropathic pain. J Korean Med Sci. 2013 Feb;28(2):308-14.

[5]. Harden RN, et al. A Phase 2a, Randomized, Crossover Trial of Gabapentin Enacarbil for the Treatment of Postherpetic Neuralgia inGabapentin Inadequate Responders. Pain Med. 2013 Sep 18.

 Chemical & Physical Properties

Boiling Point
314.4ºC at 760mmHg
Melting Point
148-151℃ (ethanol )
Molecular Formula
C9H18ClNO2
Molecular Weight
207.69800
Flash Point
144ºC
Exact Mass
207.10300
PSA
63.32000
LogP
2.87260

Company Profile Introduction

Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals. Mainly deals in the sales of: Pharmaceutical intermediates OLED intermediates: Pharmaceutical intermediates; OLED intermediates;

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