Choose Your Country or Region

Gabapentin HCl

Name: Gabapentin HCl
Brand: Selleck Chemicals
SKU: S1338
Rating: 5 (3 reviews)

Synonyms: Neurontin HCl

Catalog No.S1338 Purity: 97%

Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

Gabapentin HCl Chemical Structure

CAS: 60142-95-2

Selleck's Gabapentin HCl has been cited by 3 publications

Purity & Quality Control

Batch: Purity: >97%

Other GABA Receptor Products

Related compound libraries

Choose Selective GABA Receptor Inhibitors

Biological Activity

Description

Gabapentin HCl(Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

Targets

GABA receptor ^[1]

In vitro
In vitro	Gabapentin suppresses ectopic afferent discharge activity generated from injured peripheral nerves. Gabapentin, in a range of 30 to 90 mg/kg, significantly attenuates allodynia in nerve-injured rats. Gabapentin dose-dependently inhibits the ectopic discharge activity of 15 injured sciatic afferent nerve fibers through an action on impulse generation. ^[1] Gabapentin inhibits KCl (30 mM)-evoked voltage-dependent Ca(2+) influx. Gabapentin potently inhibits the peak whole-cell Ca(2+) channel current (I(Ba)) in a dose-dependent manner with an estimated IC(50) value of 167 nM. Gabapentin inhibition is voltage-dependent, producing an approximately 7 mV hyperpolarizing shift in current voltage properties and reducing a non-inactivating component of whole-cell current activated at relatively depolarized potentials. ^[2] Gabapentin selectively activates heterodimeric GABAB1a-B2 receptors, but not GABAB1b-B2 or GABAB1c-B2 receptors. Gabapentin selectively activates presynaptic GABAB heteroreceptors on glutamatergic terminals, but not GABAB autoreceptors on GABAergic terminals. Gabapentin is found to inhibit both the excitatory synaptic transmission in vitro and the neuronal response to noxious electrical and mechanical stimulation in vivo mediated by α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), but not those mediated by N-methyl-D-asparate (NMDA) receptors. Gabapentin acts as an AMPA-receptor antagonist in the rat spinal cord to exert its spinal antinociceptive effect. Gabapentin depresses, but NMDA enhanced, the presynaptic fiber volley in the CA1 region of rat hippocampal slices. ^[3]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04613024	Not yet recruiting	Weight Loss\|Pain Postoperative	Stanford University	July 1 2023	Early Phase 1
NCT05276089	Not yet recruiting	Opioid Use	Dr Yu Fu\|Teesside University\|NIHR Applied Research Collaboration for North East and North Cumbria\|North East Academic Health Science Network\|Newcastle University	February 1 2023	Not Applicable
NCT05609682	Recruiting	Post Operative Pain	University of Oklahoma	November 29 2022	Early Phase 1
NCT05750875	Completed	Pruritus\|Uremia\|Chronic Kidney Diseases	King Edward Medical University	May 1 2022	Phase 4

References

Chemical lnformation & Solubility

Molecular Weight	207.7	Formula	C₉H₁₇NO₂.HCl
CAS No.	60142-95-2	SDF	Download Gabapentin HCl SDF
Smiles	C1CCC(CC1)(CC(=O)O)CN.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 42 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):