Engineering a GABA endowed with pharmacological CNS activity when given by an extracerebral route

Vamecq, Jòseph; Feutelais, Y.; Maurois, Pierre; Sghaier, Mehrez; Dichi, E.; German-Fattal, Michèle; Herrenknecht, Christine; Gressèns, Pierre; Cecchelli, Roméo; Dehouck, Lucie; Stables, James P.; Pagès, Nicole; Légendre, B.; Bac, Pierre

doi:10.1007/s00044-008-9124-1

Cited by 17 publications

(26 citation statements)

References 9 publications

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“…At low frequency, the impedances of the commercial GABA (361.2 kohm cm 2 ) and sublimated GABA (202.6 kohm cm 2 ) solutions were distinctly different, indicating that the mobility of sublimated GABA was greater than that of commercial GABA. Compared to the Nyquist curve for water, its impedance is 654.5 kohm cm 2 . The electronic transfer between the sublimated GABA in water and the platinum cell is easier than for commercial GABA.…”

Section: Resultsmentioning

confidence: 85%

“…2. They show that when administered intraperitoneally non-transformed GABA, even at a strong dose (100 mg/kg), is inactive at the level of the central nervous system.…”

Section: Discussionmentioning

confidence: 98%

“…This is a relatively low speed, given that it can reach 999.9 nm/s. The sublimation temperature was reduced from 250 2) to 190°C by changing the transformer and the evapora-…”

Section: Methodsmentioning

confidence: 99%

“…For several years, we have been carrying out a study on amino acid polymorphs synthesized by sublimation such as glycine, 1) g-amino butyric acid (GABA) 2) and leucine. The polymorphism exists in the crystal structures of amino acids with different packing arrangements and hydrogen bonding patterns of the zwitterions.…”

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confidence: 99%

“…Biological analyses 2) have demonstrated the therapeutic activity of sublimated GABA. When administered intraperitoneally, a dose of 25 mg/kg proved effective against audiogenic seizures, whereas for non-sublimated GABA, doses up to 100 mg/kg were unable to prevent audiogenic seizures.…”

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confidence: 99%

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Physico-Chemical Characterization of .GAMMA.-Amino n-Butyric Acid Nanoparticles

Dichi

Sghaier

Fraisse

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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This work deals with the preparation and characterization of high-purity nanoparticles of g g-amino n-butyric acid (GABA) in order to enhance the efficiency of this drug. A sublimation procedure at low pressure was applied to GABA after improving the experimental parameters of this physical transformation. The elaboration of the molecule is solvent-free. The process does not change the chemical formula of the compound but modifies its physico-chemical characteristics. In this work, we present the experimental parameters for preparing monoclinic GABA nanoparticles. Their identification and physico-chemical properties were determined with a large number of investigations: Powder X-ray diffraction (PXRD), density and purity measurements, differential scanning calorimetry (DSC), thermo-gravimetric analysis (TGA), calorimetric measurements (D DH dissolution and C p ), thermally stimulated current (TSC), and electrochemical impedance.

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Section: Resultsmentioning

confidence: 85%

“…2. They show that when administered intraperitoneally non-transformed GABA, even at a strong dose (100 mg/kg), is inactive at the level of the central nervous system.…”

Section: Discussionmentioning

confidence: 98%

“…This is a relatively low speed, given that it can reach 999.9 nm/s. The sublimation temperature was reduced from 250 2) to 190°C by changing the transformer and the evapora-…”

Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Physico-Chemical Characterization of .GAMMA.-Amino n-Butyric Acid Nanoparticles

Dichi

Sghaier

Fraisse

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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Additive‐Induced Selective Crystallization of the Elusive Form‐II of γ‐Aminobutyric Acid

Wang

Tang

et al. 2020

Chem Eng & Technol

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The impact of two structural factors of sodium carboxylate additives on their ability to induce the selective crystallization of g-aminobutyric acid (GABA) Form-II was investigated, namely, the number of -COOgroups and the types of R groups (chain alkyl, cyclic alkyl, or phenyl). It was found that the increase of -COOgroups caused the additives lose their inducing ability. This may be attributed to the fact that the increment of hydrophilic -COOgroups results in enhanced solvation and steric effect of additives, which makes additives unable to interact with GABA effectively. Additives with different R groups all can induce Form-II but they exhibited varying inducing abilities. This could be due to the distinct results of competition between the attachment and detachment of different additives on the GABA growth end.

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