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60142-96-3 Usage


Gabapentin hydrochloride, also known as Neurontin, is a second-generation antiepileptic drug (AED) that was introduced in the UK in 1993 and in the USA in early 1994. It is a lipophilic analog of the neurotransmitter γ-Aminobutyric acid (GABA) and is designed to cross the blood-brain barrier. Gabapentin hydrochloride is a white crystalline solid that is used for various medical applications due to its multiple mechanisms of action, including modulating calcium influx, stimulating GABA biosynthesis, and competing for the biosynthesis of L-glutamic acid.


Used in Pharmaceutical Industry:
Gabapentin hydrochloride is used as an anticonvulsant for the treatment of refractory partial seizures and secondarily generalized tonic-clonic seizures. It exerts its anticonvulsive function through a GABA receptor-independent mechanism, possibly involving the L-system amino acid transporter protein.
Used in Neuropathic Pain Management:
Gabapentin hydrochloride is used as an analgesic for various neuropathic pain syndromes, such as Complex Regional Pain Syndrome type one (CRPS 1). It is also prescribed to multiple sclerosis patients to control dysesthesias and may be useful in reducing neuropathic pain caused by cancer and HIV infection.
Used in Restless Legs Syndrome (RLS) Treatment:
Gabapentin hydrochloride is used as an antipsychotic and 5HT2A antagonist for the treatment of adult Restless Legs Syndrome (RLS), a neurological disorder characterized by an uncontrollable urge to move the legs, often accompanied by uncomfortable sensations.
Used in Postherpetic Neuralgia (PHN) Treatment:
Gabapentin hydrochloride is used as a selective H1-receptor antagonist for the treatment of postherpetic neuralgia (PHN), a chronic pain condition that can follow an outbreak of shingles.
Used in Drug Delivery Systems:
Gabapentin hydrochloride is used in drug delivery systems to enhance its applications and efficacy against various medical conditions. Its high bioavailability and favorable pharmacokinetic profile make it an ideal candidate for combination therapies with other antiepileptic drugs, reducing the potential for drug interactions.

Generic formulation

MHRA/ CHM advice to minimize risk when switching patients with epilepsy between different manufacturers’ products (including generic products): It is usually unnecessary to ensure that patients are maintained on a specific manufacturer’s product unless there are specific concerns, such as patient anxiety and risk of confusion/ dosing error.


Epilepsy: monotherapy or adjunctive therapy of focal seizures with or without secondary generalization. Recommendations summarized from NICE (2012) Seizure types: adjunctive (focal seizures), contraindicated (generalized tonic- clonic seizures generalized tonic- clonic seizures if there are absence or myoclonic seizures, or if juvenile myoclonic epilepsy is suspected, tonic/ atonic seizures, absence seizures, myoclonic seizures). Epilepsy types: adjunctive (benign epilepsy with centrotemporal spikes, Panayiotopoulos syndrome, late- onset childhood occipital epilepsy), contraindicated (absence syndromes, juvenile myoclonic epilepsy, idiopathic generalized epilepsy, Dravet syndrome, Lennox– Gastaut syndrome) ?Psychiatry— treatment of anxiety disorders (unlicensed); treatment of alcohol withdrawal symptoms (unlicensed). ?Neurology— treatment of neuropathic pain and restless leg syndrome (unlicensed) and prophylaxis of migraine (unlicensed).


Gabapentin (Neurontin) significantly decreases pain scores and sleep interference associated with PHN. An initial dose of 300 mg/day is increased over 4 weeks (900, 1,800, 2,400, 3,600 mg/day divided t.i.d.) until efficacy is obtained or side effects become intolerable.

Dose titration

Monotherapy or adjunctive therapy 300 mg od for day 1300 mg bd for day 2300 mg td for day 3 (or 300 mg td for day 1), then increased by 300 mg every 2– 3 days, divided into three doses; usual maintenance 900– 3600 mg daily, divided into three doses (max. 4800 mg daily) If gabapentin has to be discontinued, it is recommended this should be done gradually over a minimum of 1?week, independent of the indication.


Patients with a history of psychotic illness. Patients with mixed seizures (including absences). Patients with diabetes mellitus. Elderly patients.


With AEDs Nil. With other drugs Patients who require concomitant treatment with opioids should be carefully observed for signs of respiratory depression and/ or sedation, and the dose of gabapentin or opioid should be reduced appropriately Co-administration of gabapentin with antacids containing aluminium and magnesium, reduces gabapentin bioavailability up to 24%, and it is therefore recommended that gabapentin be taken at the earliest 2 hours following antacid administration With alcohol/food There are no known specific interactions between alcohol and gabapentin and there are no specific foods that must be excluded from diet when taking gabapentin.

Special populations

Renal impairment Reduce maintenance dose according to degree of reduction in creatinine clearance. Pregnancy The dose of gabapentin should be monitored carefully during pregnancy and after birth, and adjustments made on a clinical basis. No definite conclusion can be made as to whether gabapentin is associated with an increased risk of congenital malformations when taken during pregnancy. Gabapentin should not be used during pregnancy unless the potential benefit to the mother clearly outweighs the potential risk to the foetus. Gabapentin is excreted in human milk. Because the effect on the breastfed infant is unknown, gabapentin should be used in breastfeeding mothers with caution and only if the benefits clearly outweigh the risks.

Behavioural and cognitive effects in patients with epilepsy

Gabapentin has a relatively favourable behavioural profile, although paradoxical hyperactivity, irritability and aggression have been occasionally reported, especially in patients with severe intellectual disabilities. The cognitive profile of gabapentin is equally favourable, as this AED has been associated with only minor cognitive difficulties (mainly in the attention domain).

Psychiatric use

Although gabapentin has no approved indications in psychiatry, it has shown efficacy in the treatment of anxiety disorders, especially social phobia. Other offlabel uses include other anxiety disorders (panic disorder, post- traumatic stress disorder), alcohol dependence and withdrawal, behavioural and psychological symptoms of dementia, and aggression. Gabapentin has also been proposed to be useful in the maintenance treatment of bipolar disorder as adjunctive therapy.


Warner-Lambert (U.S.A.)

Manufacturing Process

32.8 g 1,1-cyclohexane-diacetic anhydride are mixed with 7 g anhydrous methanol and heated under reflux for 1 hour. After evaporation of the reaction mixture in a vacuum, was obtained 37.5 g monomethyl 1,1-cyclohexanediacetate in the form of a yellowish oil. 5.6 ml triethylamine in 16 ml anhydrous acetone are added dropwise at 0°C to a solution of 7.28 g monomethyl 1,1-cyclohexane-diacetate, then a solution of 3.6 ml ethyl chloroformate in 16 ml anhydrous acetone is added thereto. The reaction mixture is further stirred for 30 min at 0°C and and then a solution of 3.4 g sodium azide in 12 ml water added dropwise thereto. The reaction mixture is stirred for 1 hour at 0°C, then poured into ice water and extracted three times with 50 ml amounts of ice-cold toluene. The combined extracts are dried over anhydrous sodium sulphate at 0°C and subsequently introduced drop-wise into a flask pre-heated to 100°C. The mixture is then heated for a further hour under reflux and thereafter evaporated in a vacuum. The crude methyl 1-isocyanatomethyl-1-cyclohexane-acetate which remains behind is heated under reflux for 3 hours with 50 ml 20% hydrochloric acid. After cooling the solution, it is extracted three times with 100 ml amounts of chloroform to remove the 1-amino-methyl-1-cyclohexane-acetic acid lactam formed as a by-product product and the aqueous hydrochloric acid solution evaporated in a vacuum, whereby 1-aminomethyl-1-cyclohexane-acetic acid crystallises as the hydrochloride; m.p. 117-118°C, after recrystallisation from acetone/methanol/ether. After recrystallization from methanol/ether the melting point of the product is 129-133°C. By treatment with a basic ion exchanger and crystallisation from ethanol/ether, there is obtained pure 1-amino-methyl-1-cyclohexane-acetic acid; melting point 162-166°C.

Therapeutic Function


Biological Functions

Gabapentin (Neurotonin) was initially designed to be a rigid analogue of GABA. When it was discovered to have antiepileptic properties, it was assumed that this activity was related to a GABAergic mechanism. However, subsequent studies have failed to show any GABAergic activity of gabapentin. Although it has not yet been possible to ascribe any definite mechanism to its antiepileptic activity, there is recent evidence that it may function as an agonist at GABAB receptors in the brain. Gabapentin is recommended as adjunctive therapy in the treatment of partial seizures in adults.When used with other drugs, it appears to be an effective AED; it is usually not effective when employed alone for patients with severe seizures. Gabapentin is generally well tolerated, with somnolence, dizziness, and ataxia the most commonly reported adverse effects. A low incidence of potentially serious side effects and no significant allergic reactions have been reported.

Biological Activity

Anticonvulsant with several possible mechanisms of action. Increases GABA in the brain and binds to a novel site associated with voltage-sensitive Ca 2+ channels. Prevents neuronal death and is antinociceptive and anxiolytic.

Biochem/physiol Actions

Primary Targetα2δ subunit of L-type voltage gated Ca2+ channels

Clinical Use

Antiepileptic: Adjunctive treatment of partial seizures with or without secondary generalisation Neuropathic pain Migraine prophylaxis (unlicensed)

Side effects

Dose-limiting adverse effects include somnolence, dizziness, ataxia, peripheral edema, and infection (22).

Side effects

Long-Term Side Effects of Gabapentin:Mood changes.Behavioral changes.Depression.Anxiety.Memory loss.Weakened muscles.

Veterinary Drugs and Treatments

Gabapentin may be useful as adjunctive therapy for refractory or complex partial seizures, or in the treatment of chronic pain in dogs or cats.

Drug interactions

Potentially hazardous interactions with other drugs Antacids: reduce absorption. Antidepressants: antagonism of anticonvulsive effect (convulsive threshold lowered); avoid with St John’s wort. Antimalarials: anticonvulsant effect antagonised by mefloquine. Antipsychotics: antagonism of anticonvulsive effect (convulsive threshold lowered). Orlistat: possible increased risk of convulsions.


There is no evidence of gabapentin metabolism in humans. Gabapentin is eliminated unchanged solely by renal excretion.


1) Cheng et al. (2004), Does gabapentin act as an agonist at native GABA(B) receptors?; J. Biomed. Sci., 11 346 2) Lanneau et al. (2001), Gabapentin is not a GABAB receptor agonist; Neuropharmacology 41 965 3) Hendrich et al. (2008), Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin; Proc. Natl. Acad. Sci. USA, 105 3628

Check Digit Verification of cas no

The CAS Registry Mumber 60142-96-3 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,0,1,4 and 2 respectively; the second part has 2 digits, 9 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 60142-96:
93 % 10 = 3
So 60142-96-3 is a valid CAS Registry Number.

60142-96-3 Well-known Company Product Price

  • Brand
  • (Code)Product description
  • CAS number
  • Packaging
  • Price
  • Detail
  • TCI America

  • (G0318)  Gabapentin  >98.0%(GC)(T)

  • 60142-96-3

  • 5g

  • 140.00CNY

  • Detail
  • TCI America

  • (G0318)  Gabapentin  >98.0%(GC)(T)

  • 60142-96-3

  • 25g

  • 380.00CNY

  • Detail
  • Sigma-Aldrich

  • (PHR1049)  Gabapentin  pharmaceutical secondary standard; traceable to USP

  • 60142-96-3

  • PHR1049-1G

  • 878.44CNY

  • Detail
  • Sigma-Aldrich

  • (Y0001280)  Gabapentin  European Pharmacopoeia (EP) Reference Standard

  • 60142-96-3

  • Y0001280

  • 1,880.19CNY

  • Detail
  • USP

  • (1287303)  Gabapentin  United States Pharmacopeia (USP) Reference Standard

  • 60142-96-3

  • 1287303-250MG

  • 4,662.45CNY

  • Detail
  • Sigma

  • (G154)  Gabapentin  solid

  • 60142-96-3

  • G154-10MG

  • 1,140.75CNY

  • Detail
  • Sigma

  • (G154)  Gabapentin  solid

  • 60142-96-3

  • G154-50MG

  • 4,910.49CNY

  • Detail
  • Cerilliant

  • (G-007)  Gabapentin solution  1.0 mg/mL in methanol, ampule of 1 mL, certified reference material

  • 60142-96-3

  • G-007-1ML

  • 716.04CNY

  • Detail



According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 16, 2017

Revision Date: Aug 16, 2017


1.1 GHS Product identifier

Product name gabapentin

1.2 Other means of identification

Product number -
Other names GABAPENTIN

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:60142-96-3 SDS

60142-96-3Relevant articles and documents

A Simple and Expedient Procedure for the Preparation of Gabapentin Lactam (2-Aza-spiro[4,5]decan-3-one)

Katuri, Jashuva V. P.,Ekkundi, Vadiraj S.,Nagarajan, Kuppuswamy

, p. 1828 - 1832 (2016)

A novel process has been described on 100 g scale for the preparation of gabapentin lactam which is a penultimate intermediate for the preparation of gabapentin, comprising a Hofmann reaction of 1,1-cyclohexanediacetic acid monoamide using chlorinating agents such as trichloroisocyanuric acid, sodium dichloroisocyanurate, 1,3-dichloro-5,5-dimethylhydantoin, and N-chlorosuccinimide, which have not been employed so far for making this molecule. Reactions done in aqueous alkali on the 1,1-cyclohexanediacetic acid monoamide led to a solution of gabapentin sodium salt which on heating led to the formation of the gabapentin lactam in good yield.

Process for the preparation of gabapentin


, (2019/09/17)

The present invention relates to an improved process for the preparation of Gabapentin. The process also relates to a new process for the preparation of 1, 1-cyclohexane diaceitic acid monoamide (CDMA), which is a key intermediate for the preparation of Gabapentin.

A process for synthesis of gabapentin


, (2016/11/24)

The invention discloses a gabapentin synthesis technology. The gabapentin synthesis technology comprises the following steps of 1, preparing 1,1-cyclohexane diacetic anhydride, 2, preparing 3,3-cyclopentaneglutaramic acid, 3, preparing gabapentin hydrochloride, 4, adding the gabapentin hydrochloride into an oxalic acid solution, adjusting a pH value to 2-5, carrying out stirring, carrying out pressure reduction condensation to obtain filter cake, dissolving the filter cake in ethanol, carrying out stirring for dissolution, and carrying out pressure reduction drying to obtain fined gabapentin oxalate, and 5, adding the fined gabapentin oxalate into absolute ethanol, adjusting a PH value to 7-8, carrying out stirring, adding active carbon into the mixture, carrying out heating reflux, carrying out filtration, carrying out pressure reduction drying to obtain a gabapentin hydrate, adding the gabapentin hydrate into absolute ethanol, carrying out heating dissolution, carrying out cooling, carrying out filtration, concentrating the filtrate, carrying out cooling for crystal precipitation, carrying out filtration, carrying out washing by absolute ethanol and carrying out drying to obtain gabapentin. Gabapentin obtained by the gabapentin synthesis technology has high content and a high yield.

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