Study of a GABA c receptor antagonist on sleep-waking behavior in rats

Arnaud, C.; Gauthier, Pierre; Gottesmann, Claude

doi:10.1007/s002130000653

Cited by 58 publications

(53 citation statements)

References 27 publications

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“…In contrast, guanidino compounds such as (S)-2-guanidino-3-methylbutyric acid (9), (2S,3R)-2-amino-3-hydroxybutyric acid (10), (S)-2-guanidino-2-(4-hydroxyphenyl) acetic acid (11) and creatine (12) were inactive or had Guanidinoacetic acid (1) caused a parallel shift in the concentration-response curve of GABA to the right over 4 antagonist concentrations indicating its competitive nature [ Fig. 3; K B = 7.75 lM (pA 2 or -logK B = 5.11 ± 0.06; Table 1)].…”

Section: Resultsmentioning

confidence: 95%

“…Guanidino analog (1)- (12) were evaluated for activity alone and in the presence of GABA (1 lM). These compounds had no effect alone when tested at 100 or 300 lM but in the presence of GABA (1 lM), compounds (1)-(8) inhibited the response in a concentration-dependent manner ( Fig.…”

Section: Resultsmentioning

confidence: 99%

“…Guanidino analogs, guanidinoacetic acid (1) 3-guanidinopropionic acid (2), 4-guanidinobutanoic acid (3), 2-guanidinoethanesulfinic acid (4) (S)-2-guanidinopropanoic acid (5), (±)-2-guanidinopropanoic acid (6), (S)-2-guanidino butyricacid (7), (S)-2-guanidino-3-hydroxypropanoic acid (8), (S)-2-guanidino-3-methylbutyric acid (9), (2S,3R)-2-amino-3-hydroxybutyric acid (10), (S)-2-guanidino-2-(4-hydroxyphenyl) acetic acid (11) and creatine (12) were synthesized in house using established methodologies [25][26][27]. All other chemicals were obtained from SigmaAldrich (St Louis, MO, USA) unless otherwise stated.…”

Section: Methodsmentioning

confidence: 99%

“…)-CAMP] [3] and 5-methyl imidazole-4-acetic acid [4], and blocked by (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid [TPMPA] [5,6], the cyclopentane phosphinic acids, cis-and trans-(3-aminocyclopentanyl)butylphosphinic acid [7][8][9] and the cyclopentene phosphinic acids, (R)-and (S)-4-amino-cyclopent-1-enyl phosphinic acids [10]. GABA C antagonists have been shown to prevent experimental myopia development, and inhibited the associated vitreous chamber elongation [9], enhance memory in chicks [11] and rats [9], and affect sleep-waking behavior in rats [12] suggesting that these receptors may also be involved in myopia, memory-related disorders and circadian rhythms [13]. GABA C receptors have also been found to be present in thyrotropin-secreting cells where they may be involved in the regulation of hormone secretion [14], as well as in the gut where they may have a role in regulating gut motility [15].…”

Section: Introductionmentioning

confidence: 99%

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Guanidino Acids Act as ρ1 GABAC Receptor Antagonists

et al. 2009

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GABA(C) receptors play a role in myopia, memory-related disorders and circadian rhythms signifying a need to develop potent and selective agents for this class of receptors. Guanidino analogs related to glycine, beta-alanine and taurine were evaluated at human rho(1)GABA(C) receptors expressed in Xenopus oocytes using 2-electrode voltage clamp methods. Of the 12 analogs tested, 8 analogs were active as antagonists and the remaining were inactive. (S)-2-guanidinopropionic acid (IC(50) = 2.2 microM) and guanidinoacetic acid (IC(50) = 5.4 microM; K (B) = 7.75 microM [pK (B) = 5.11 +/- 0.06]) were the most potent being competitive antagonists at this receptor. In contrast, the beta-alanine and GABA guanidino analogs showed reduced activity, indicating the distance between the carboxyl carbon and terminal nitrogen of the guanidino group is critical for activity. Substituting the C2-position of guanidinoacetic acid with various alkyl groups reduced activity indicating that steric effects may impact on activity. The results of this study contribute to the structure-activity-relationship profile required in developing novel therapeutic agents.

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Section: Resultsmentioning

confidence: 95%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Guanidino Acids Act as ρ1 GABAC Receptor Antagonists

et al. 2009

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“…GABA GABA-receptors GABA , GABA , , (Concas et al, 1994). , GABA (Arnaud et al, 2001), , (Declerck et. al., 1992).…”

Section: Gamma-amino Butyric Acid (Gaba)mentioning

confidence: 99%

Stress Relaxation and Sleep Induction Effect of Fermented Sea Tangle Saccharina japonica and Oyster Crassostrea gigas Powder

Woo¹,

Seo²

2013

Korean Journal of Fisheries and Aquatic Sciences

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Sleep is an essential biological process of which the underlying regulatory mechanisms involve numerous anatomical structures and biochemical substances that can be compromised by stress and the immune system. Gamma aminobutyric acid (GABA) is the main inhibitory neurotransmitter of the central nervous system (CNS). It is well established that activation of GABA A receptors promotes sleep. L. brevis BJ20 fermentation of sea tangle and oysters resulted in stress reduction and sleep inducing effects. This is the first study to report that GABA has the ability to induce sleep related hormones in mice; therefore, it has potential use as a natural sleep aid. These results suggested that sea tangle and oysters fermented by L. brevis BJ20 can be used as potential agents for stress reduction and sleep promotion.

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Multi‐messenger studies of γ‐ray bursts and their cosmic environment

Pintér

2018

Astron Nachr

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Recent results of the international High Energy Astronomy Research Team (HEART, a Czech, Japanese, American, and Hungarian collaboration) are presented. Our multi‐messenger investigations revealed the properties of γ‐ray bursts (GRB) and their host environments. We analyzed Fermi measurement data with our ADWO method, which appeared as a handy tool for identifying short and intermediate‐long GRBs, such as GRB170817. By studying the GRBs' spatial distribution, we discovered two of the largest known formations in the Universe: the Giant GRB Ring, and the Hercules‐Corona Borealis Great Wall. We used faar infrared imaging photometry data to resolve the fine structure and composition of the Galactic foreground interstellar medium (ISM) in the direction of GRBs. This resulted in an increase in the precision of calculating the column density of intrinsic ISM at the GRBs in their host galaxies.

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Study of a GABA c receptor antagonist on sleep-waking behavior in rats

Abstract: GABAC receptors are also involved in sleep-waking regulation. Since the sensitivity of GABAC receptors to GABA is much higher than that of GABAA and GABAB receptors, GABAC receptor modulators could be potential medications acting at low doses with fewer side effects.

Cited by 58 publications

References 27 publications

Guanidino Acids Act as ρ1 GABAC Receptor Antagonists

Guanidino Acids Act as ρ1 GABAC Receptor Antagonists

Stress Relaxation and Sleep Induction Effect of Fermented Sea Tangle Saccharina japonica and Oyster Crassostrea gigas Powder

Multi‐messenger studies of γ‐ray bursts and their cosmic environment

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