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编 号:F402134
分子式:C9H18ClNO2
分子量:207.7
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10mg
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50mg
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100mg
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生物活性:
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.

体内研究:
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.

体外研究:
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.
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