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Gabapentin

CAS No.: 60142-96-3
Product introduction:Gabapentin is a structurally unique pharmaceutical agent that was originally designed as a GABA (gamma-aminobutyric acid) mimetic but is now understood to exert its therapeutic effects through a completely different mechanism. It is a lipophilic analog of the inhibitory neurotransmitter GABA, with a cyclohexyl group that enables it to cross the blood-brain barrier effectively. Surprisingly, gabapentin does not bind to GABA-A, GABA-B, or benzodiazepine receptors, nor does it affect GABA synthesis, reuptake, or degradation. Instead, it binds with high affinity to the α2δ-1 subunit of voltage-gated calcium channels, reducing the influx of calcium ions into presynaptic neurons and thereby decreasing the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P. This unique mechanism of action makes gabapentin valuable for both neurological and psychiatric conditions, particularly neuropathic pain, epilepsy, and anxiety disorders.

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CAS No.:60142-96-3

Gabapentin is a white to off-white crystalline powder with the molecular formula C₉H₁₇NO₂ and a molecular weight of approximately 171.24 g/mol. Its chemical name is 1-(aminomethyl)cyclohexaneacetic acid. The compound is freely soluble in water and aqueous bases, soluble in acidic solutions, and slightly soluble in organic solvents such as ethanol. Gabapentin exhibits pH-dependent solubility, with maximum solubility in acidic conditions (pH 1-3). The compound has a characteristic bitter taste and is stable under normal storage conditions when kept in a tightly sealed container, protected from light and moisture. Gabapentin is typically available in pharmaceutical-grade purity (≥98% by HPLC) for oral formulation into capsules, tablets, and oral solutions.

Core Functions:

  • Active pharmaceutical ingredient (API) in oral formulations for the treatment of partial seizures (as adjunctive therapy) and neuropathic pain associated with postherpetic neuralgia

  • Treatment of moderate-to-severe restless legs syndrome and fibromyalgia (off-label indications with clinical evidence)

  • Management of various anxiety disorders, including social anxiety disorder and preoperative anxiety, as a potential alternative to benzodiazepines

  • Investigational application in alcohol and cocaine use disorder for withdrawal symptom reduction and relapse prevention

  • Research use in neurology and pharmacology studies of calcium channel modulation and neurotransmitter release

  • Reference standard for analytical method development and quality control in pharmaceutical testing

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