Evaluation of Isonicotinoyl-γ-Aminobutyric Acid (GABA) and Nicotinoyl-GABA as Pro-drugs of GABA

Isonicotinoyl-γ-aminobutyric acid (GABA) (IG) and nicotinoyl-GABA (NG), candidate prodrugs of GABA, were assessed by measuring various pharmacological responses such as anticonvulsant effect, prolongation of pentobarbital sleeping time and depressive effect on rearing or ambulation in general behavi...

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Published inChemical & pharmaceutical bulletin Vol. 32; no. 10; pp. 4089 - 4095
Main Authors MATSUYAMA, KENJI, YAMASHITA, CHIKAMASA, NODA, ATSUKO, GOTO, SHIGERU, NODA, HIROSHI, ICHIMARU, YASUYUKI, GOMITA, YUTAKA
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 01.01.1984
Maruzen
Subjects
Animals
Behavior, Animal - drug effects
Biological and medical sciences
Brain - metabolism
Chemistry, Pharmaceutical
gamma-Aminobutyric Acid - analogs & derivatives
gamma-Aminobutyric Acid - metabolism
gamma-Aminobutyric Acid - pharmacology
GC-MS
General pharmacology
Male
Medical sciences
Mice
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
GABA
Purification
Prodrug
Structure activity relation
Preparation
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Abstract Isonicotinoyl-γ-aminobutyric acid (GABA) (IG) and nicotinoyl-GABA (NG), candidate prodrugs of GABA, were assessed by measuring various pharmacological responses such as anticonvulsant effect, prolongation of pentobarbital sleeping time and depressive effect on rearing or ambulation in general behavior, in relation to the GABA level in the mouse brain. The GABA level after the intraperitoneal administration of IG at a dose of 1000 mg/kg increased significantly from 2.30±0.02μmol/g wet wt. in the control to 2.93±0.05μmol/g wet wt., while NG caused only a slight increase in GABA level. IG showed a stronger anticonvulsant effect, greater prolongation of pentobarbital sleeping time and greater depressive effect on rearing in general behavior than NG did. The pharmacological effect of IG or NG corresponded well to the GABA level in the brain.
AbstractList Isonicotinoyl-γ-aminobutyric acid (GABA) (IG) and nicotinoyl-GABA (NG), candidate prodrugs of GABA, were assessed by measuring various pharmacological responses such as anticonvulsant effect, prolongation of pentobarbital sleeping time and depressive effect on rearing or ambulation in general behavior, in relation to the GABA level in the mouse brain. The GABA level after the intraperitoneal administration of IG at a dose of 1000 mg/kg increased significantly from 2.30±0.02μmol/g wet wt. in the control to 2.93±0.05μmol/g wet wt., while NG caused only a slight increase in GABA level. IG showed a stronger anticonvulsant effect, greater prolongation of pentobarbital sleeping time and greater depressive effect on rearing in general behavior than NG did. The pharmacological effect of IG or NG corresponded well to the GABA level in the brain.
Isonicotinoyl- gamma -aminobutyric acid (GABA) (IG) and nicotinoyl-GABA (NG), candidate pro-drugs of GABA, were assessed by measuring various pharmacological responses such as anticonvulsant effect, prolongation of pentobarbital sleeping time and depressive effect on rearing or ambulation in general behavior, in relation to the GABA level in the mouse brain. The GABA level after the intraperitoneal administration of IG at a dose of 1000 mg/kg increased significantly in the control, while NG caused only a slight increase in GABA level. IG showed a stronger anticonvulsant effect, greater prolongation of pentobarbital sleeping time and greater depressive effect on rearing in general behavior than NG did. The pharmacological effect of IG or NG corresponded well to the GABA level in the brain.
Author GOTO, SHIGERU
ICHIMARU, YASUYUKI
NODA, HIROSHI
GOMITA, YUTAKA
YAMASHITA, CHIKAMASA
NODA, ATSUKO
MATSUYAMA, KENJI
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Isonicotinoyl- gamma -aminobutyric acid (GABA) (IG) and nicotinoyl-GABA (NG), candidate pro-drugs of GABA, were assessed by measuring various pharmacological...
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SubjectTerms Animals
Behavior, Animal - drug effects
Biological and medical sciences
Brain - metabolism
Chemistry, Pharmaceutical
gamma-Aminobutyric Acid - analogs & derivatives
gamma-Aminobutyric Acid - metabolism
gamma-Aminobutyric Acid - pharmacology
GC-MS
General pharmacology
Male
Medical sciences
Mice
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Title Evaluation of Isonicotinoyl-γ-Aminobutyric Acid (GABA) and Nicotinoyl-GABA as Pro-drugs of GABA
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