S85918 |
Gabapentin HCl |
源葉(MedMol) | ≥98% |
- 產(chǎn)品描述: Gabapentin hydrochloride is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain
- 靶點(diǎn): Calcium Channel;CalciumChannel;GABAReceptor
- 體外研究:
Gabapentin (0-300 μM) hydrochloride produces a concentration-dependent inhibition of the K+-induced [Ca2+]i?increase in synaptosomes (IC50=14?μM; maximal inhibition by 36%). Gabapentin (100? μM) hydrochloride decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively. Gabapentin (0-1000 μM) hydrochloride reduces the K+-evoked [3H]-noradrenaline release in neocortical slices (IC50=48?μM; maximal inhibition of 46%) but not from synaptosomes
- 體內(nèi)研究:
Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) hydrochloride has improving effects on spatial and emotional cognitive performance of naive mice in Morris water maze (MWM), passive avoidance (PA) and modified elevated plus maze (mEPM) tasks. Gabapentin (1-100 mg/kg; i.p.; once; male mice) hydrochloride has analgesic effect and reduces writhing in a dose-dependent manner. Animal Model: Male BALB/c mice (35-45 g) Dosage: 5 and 10 mg/kg Administration: Intraperitoneal injection; once Result: Increased the time spent in target quadrant and decreased the distance to platform in MWM test. Decreased the transfer latency on second day in mEPM test. Prolonged retention latency in PA test. Animal Model: Male mice (26-30 g) Dosage: 1, 5, 10, 50 and 100 mg/kg Administration: Intraperitoneal injection; once Result: Produced 45-70% inhibition of writhing.
- 參考文獻(xiàn):
1. Fink K, et, al. Inhibition of neuronal Ca(2+) influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices. Br J Pharmacol. 2000 Jun;130(4):900-6. 2. Celikyurt IK, et, al. Gabapentin, A GABA analogue, enhances cognitive performance in mice. Neurosci Lett. 2011 Apr 1;492(2):124-8. 3. Meymandi MS, et, al. Gabapentin action and interaction on the antinociceptive effect of morphine on visceral pain in mice. Eur J Anaesthesiol. 2008 Feb;25(2):129-34.
- 溶解性: Soluble in H2O
- 保存條件: -20°C
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 4.815 ml 24.073 ml 48.146 ml 5 mM 0.963 ml 4.815 ml 9.629 ml 10 mM 0.481 ml 2.407 ml 4.815 ml 50 mM 0.096 ml 0.481 ml 0.963 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)