Gabapentin HCl

SKU: orb1221984

Description

Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.(In Vitro):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.(In Vivo):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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 60142-95-2
• MW: 207.7
• Purity: >98% (HPLC)
• Formula: C₉H₁₇NO₂·HCl
• SMILES: Cl.NCC1(CC(O)=O)CCCCC1
• Target: GABAR
• Solubility: H2O : 50 mg/mL 240.73 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

GABAR