Name: Gabapentin
Brand: Selleck Chemicals
SKU: S2133
Rating: 5 (4 reviews)

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Quality Control

Batch: Purity: 99.41%

99.41

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor TRP Channel Cholinesterase (ChE) GluR
Other GABA Receptor Inhibitors	Dihydromyricetin CGP52432 Oxiracetam Ginkgolide A Pentylenetetrazol 4-Aminobutyric acid (GABA) Emamectin Benzoate Nefiracetam Piracetam Bemegride

Chemical Information, Storage & Stability

Molecular Weight	171.24	Formula	C₉H₁₇NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	60142-96-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CCC(CC1)(CC(=O)O)CN

Solubility

In vitro
Batch:

Water : 34.2 mg/mL

Ethanol : 3 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.15mg/ml (0.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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:

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

Mechanism of Action

Targets/IC₅₀/Ki	GABA receptor
In vitro	Gabapentin produces concentration-dependent inhibitions of the K(+)-induced [Ca(2+)](i) increase in fura-2-loaded human neocortical synaptosomes with IC50 of 17 mM and maximal inhibition of 37%. This compound may bind to the Ca(2+) channel alpha 2 delta subunit to selectively attenuate depolarization-induced Ca(2+) influx of presynaptic P/Q-type Ca(2+) channels; this results in decreased glutamate/aspartate release from excitatory amino acid nerve terminals leading to a reduced activation of AMPA heteroreceptors on noradrenergic nerve terminals. It produces alterations in the cytosolic and extracellular concentrations of several amino acids, including L-leucine, L-valine and L-phenylalanine, in rat cortical astrocytes and synaptosomes, effects that are postulated to be of pharmacological significance. This chemical reduces potassium-evoked calcium influx via voltage-gated calcium channels in a mouse pituitary cell line that constitutively expresses GABAB receptors comprising the functional gb1a–gb2 subunit heterodimer. It can increase N-methyl-d-aspartate (NMDA)-evoked currents in GABA-positive rat dorsal horn neurones in the presence of protein kinase C, possibly by increasing the glycine sensitivity of the NMDA receptor complex. This agent produces a delayed allosteric enhancement of an unspecified voltage-activated potassium current in rat dorsal root ganglion neurons.
In vivo	Gabapentin dose-dependently (10-100 mg/kg, p.o.) blocks both static and dynamic allodynia in the rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11804619/ [2] https://pubmed.ncbi.nlm.nih.gov/16376147/ [3] https://pubmed.ncbi.nlm.nih.gov/10204753/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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Gabapentin GABA Receptor agonist

Chemical Structure

Molecular Weight: 171.24