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Andrea Kragler et al.
European journal of medicinal chemistry, 43(11), 2404-2411 (2008-04-09)
A series of N-substituted aminomethylphenol derivatives was synthesized by reductive amination. To study the inhibitory potency of the target compounds at the murine GABA transporters (mGAT1-mGAT4), a [(3)H]GABA uptake test system in a 96-well format based on HEK cells stably
Philip M Duy et al.
Experimental physiology, 95(7), 774-787 (2010-04-27)
Hyperthermic prolongation of the laryngeal chemoreflex (LCR) in decerebrate piglets is prevented or reversed by GABA(A) receptor antagonists and adenosine A(2A) (Ad-A(2A)) receptor antagonists administered in the nucleus of the solitary tract (NTS). Therefore, we tested the hypothesis that enhanced
Khashayar Nassery et al.
Archives of oral biology, 52(7), 607-613 (2007-02-06)
The purpose of this study was to determine whether (a) an uptake system for gamma-aminobutyric acid (GABA) exists in human dental pulp, (b) GABA can be released from nerves in this tissue, and (c) GABA(B) autoreceptors modulate release of this
Hong Gao et al.
Neuropharmacology, 58(8), 1220-1227 (2010-03-17)
Zolpidem is a widely prescribed sleep aid with relative selectivity for GABA(A) receptors containing alpha1-3 subunits. We examined the effects of zolpidem on the inhibitory currents mediated by GABA(A) receptors using whole-cell patch-clamp recordings from DMV neurons in transverse brainstem
Michael P DeNinno et al.
Bioorganic & medicinal chemistry letters, 21(10), 3095-3098 (2011-04-05)
The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipophilicity to address metabolic liabilities uncovered an interesting diastereomer-dependent
Joanna R Dodd et al.
The Journal of biological chemistry, 282(21), 15528-15533 (2007-04-03)
The creatine transporter (CRT) is a member of a large family of sodium-dependent neurotransmitter and amino acid transporters. The CRT is closely related to the gamma-aminobutyric acid (GABA) transporter, GAT-1, yet GABA is not an effective substrate for the CRT.
Chia-Hui Wu et al.
Applied microbiology and biotechnology, 97(4), 1581-1587 (2012-03-31)
In the Candida antarctica lipase B-catalyzed hydrolysis of (R,S)-azolides derived from (R,S)-N-protected proline in water-saturated methyl tert-butyl ether (MTBE), high enzyme activity with excellent enantioselectivity (V (S) V (R) (-1) > 100) for (R,S)-N-Cbz-proline 1,2,4-triazolide (1) and (R,S)-N-Cbz-proline 4-bromopyrazolide (2) was
Fulvia Bongianni et al.
Brain research, 1090(1), 134-145 (2006-04-25)
The specific role of gamma-aminobutyric acid (GABA) and glycine receptors in respiratory rhythm generation and pattern formation was investigated in in vitro brainstem preparations from adult lampreys by analyzing the changes in respiratory activity induced by bath application of specific
Jianbin Zheng et al.
Bioorganic & medicinal chemistry letters, 16(1), 225-227 (2005-10-26)
Twenty novel N-diarylalkenyl-piperidinecarboxylic acid derivatives were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors. The biological assay showed that (R)-1-[4,4-bis(3-phenoxymethyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic hydrochloride possessed almost as strong GAT1 inhibitory activity as tiagabine. The synthesis and structure-activity relationships are discussed.
Murray B Herd et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 33(37), 14850-14868 (2013-09-13)
Thalamocortical circuits govern cognitive, sensorimotor, and sleep-related network processes, and generate pathological activities during absence epilepsy. Inhibitory control of thalamocortical (TC) relay neurons is partially mediated by GABA released from neurons of the thalamic reticular nucleus (nRT), acting predominantly via
Sayumi Fujimori et al.
European journal of pharmacology, 550(1-3), 24-32 (2006-10-07)
Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter in the brain, but widely distributed in different peripheral organs. We have previously shown the functional expression of GABA(B) receptors required for GABAergic signal input by cultured rat calvarial osteoblasts. This study focused
C J Watson et al.
Neuroscience, 144(1), 375-386 (2006-10-24)
Morphine, a mu-opioid receptor agonist, is a commonly prescribed treatment for pain. Although highly efficacious, morphine has many unwanted side effects including disruption of sleep and obtundation of wakefulness. One mechanism by which morphine alters sleep and wakefulness may be
Sabrina S Jedlicka et al.
International journal of neural systems, 19(3), 197-212 (2009-07-04)
In this work we quantified the in vitro calibration relationships between high frequency electrical stimulation and GABA and glutamate release in both mature retinoic acid differentiated P19 neurons and immortalized embryonic cortical cells engineered to express glutamic acid decarboxylase, GAD65.
Clarissa De Sampaio Schitine et al.
Neurotoxicity research, 12(2), 145-153 (2007-10-31)
GABA is the main inhibitory aminoacid transmitter present in neurons and glial cells. Its uptake is carried out by specific high-affinity Na(+)/Cl (-) dependent transporters (GATs). It has been reported in the past that, in the avian retina, [(3)H]GABA appears
Søren Skovstrup et al.
PloS one, 7(6), e39360-e39360 (2012-06-28)
The entire substrate translocation pathway in the human GABA transporter (GAT-1) was explored for the endogenous substrate GABA and the anti-convulsive drug tiagabine. Following a steered molecular dynamics (SMD) approach, in which a harmonic restraining potential is applied to the
Mark R Faust et al.
European journal of medicinal chemistry, 45(6), 2453-2466 (2010-03-12)
In this study azetidine derivatives representing conformationally constrained GABA or beta-alanine analogs were evaluated for their potency as GABA-uptake inhibitors. The study comprised derivatives substituted in 2- as well as in 3-position with either an acetic acid moiety or a
Jiange Zhang et al.
Bioorganic & medicinal chemistry letters, 17(13), 3769-3773 (2007-05-23)
A series of new (R)-1-(2-diarylmethylthio/sulfinyl)ethyl-piperidine-3-carboxylic acid hydrochlorides 5a-d/6a-d and (R)-1-(3-diarylmethylthio)propyl-piperidine-3-carboxylic acid hydrochlorides 5'a-d were synthesized and evaluated as gamma-aminobutyric acid uptake inhibitors through cultured cell lines expressing mouse GAT1. Biological screening results demonstrated that the compounds 6a-d with diarylmethylsulfinyl ethyl
Søren Skovstrup et al.
ChemMedChem, 5(7), 986-1000 (2010-05-22)
A homology model of the human GABA transporter (GAT-1) based on the recently reported crystal structures of the bacterial leucine transporter from Aquifex aeolicus (LeuT) was developed. The stability of the resulting model embedded in a membrane environment was analyzed
Ulrich Arnold et al.
Protein science : a publication of the Protein Society, 22(3), 274-279 (2012-12-15)
The introduction of non-natural modules could provide unprecedented control over folding/unfolding behavior, conformational stability, and biological function of proteins. Success requires the interrogation of candidate modules in natural contexts. Here, expressed protein ligation is used to replace a reverse turn
José Luiz Liberato et al.
Brain research, 1124(1), 19-27 (2006-11-11)
This study was aimed at determining the effects of FrPbAII (174 Da), a novel isolated component from Parawixia bistriata spider venom, in the CNS of Wistar rats. Considering that FrPbAII inhibits the high affinity GABAergic uptake in a dose-dependent manner
Moslem Mohammadi et al.
Toxicology, 244(1), 42-48 (2007-12-07)
A synaptosomal model was used to evaluate in vivo effects of paraoxon on the uptake of [(3)H]GABA in rat cerebral cortex and hippocampus. Male Wistar rats were given a single intraperitoneal injection of one of three doses of paraoxon (0.1
Ryo Shintani et al.
Organic letters, 11(2), 457-459 (2008-12-17)
A new synthetic method of multisubstituted nipecotic acid (piperidine-3-carboxylic acid) derivatives has been developed by way of palladium-catalyzed decarboxylative cyclization of gamma-methylidene-delta-valerolactones with imines. By employing the diethoxyphosphinoyl group as the N-protecting group for imines, the reaction proceeds smoothly with
Saori Ikeda et al.
American journal of physiology. Gastrointestinal and liver physiology, 303(3), G291-G297 (2012-06-09)
Taurine is essential for the hepatic synthesis of bile salts and, although taurine is synthesized mainly in pericentral hepatocytes, taurine and taurine-conjugated bile acids are abundant in periportal hepatocytes. One possible explanation for this discrepancy is that the active supply
Inhibition of the uptake of GABA and related amino acids in rat brain slices by the optical isomers of nipecotic acid.
G A Johnston et al.
Journal of neurochemistry, 26(5), 1029-1032 (1976-05-01)
Carmela Napolitano et al.
Molecules (Basel, Switzerland), 14(9), 3268-3274 (2009-09-29)
As a novel example of improved entry of poorly delivered drugs into the brain by means of nutrient conjugates, L-carnitine was conjugated to nipecotic acid and the capacity to antagonize PTZ-induced convulsions of this novel entity was evaluated.
Morteza Malakoutikhah et al.
Journal of medicinal chemistry, 53(6), 2354-2363 (2010-02-23)
Here we studied the capacity of N-MePhe-(N-MePhe)(3)-CONH(2), Cha-(N-MePhe)(3)-CONH(2), and 2Nal-(N-MePhe)(3)-CONH(2) to carry various drugs (cargos) in in vitro blood-brain barrier (BBB) models in order to determine the versatility of these peptides as BBB-shuttles for drug delivery to the brain. Using
O Kakinohana et al.
Neuroscience, 141(3), 1569-1583 (2006-06-27)
Transient spinal cord ischemia may lead to a progressive degeneration of spinal interneurons and subsequently to increased hind limb motor tone. In the present work we sought to characterize the rigidity and spasticity components of this altered motor function by:
Jana Mejía-Toiber et al.
Cell transplantation, 19(10), 1307-1323 (2010-06-25)
The cell line M213-2O CL-4 was derived from cell line M213-2O and further modified to express human glutamate decarboxylase (hGAD-67), the enzyme that synthesizes GABA. Brain transplants of this cell line in animal models of epilepsy have been shown to
Robert A Darnall et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 302(5), R551-R560 (2011-12-14)
Arousal is an important defense against hypoxia during sleep. Rat pups exhibit progressive arousal impairment (habituation) with multiple hypoxia exposures. The mechanisms are unknown. The medullary raphe (MR) is involved in autonomic functions, including sleep, and receives abundant GABAergic inputs.
Erica A Gelfuso et al.
Neuroscience letters, 543, 12-16 (2013-04-09)
The aims of the present work were to investigate the effects of the repeated administration of Parawixin2 (2-amino-5-ureidopentanamide; formerly FrPbAII), a novel GABA and glycine uptake inhibitor, in rats submitted to PTZ-induced kindling. Wistar rats were randomly divided in groups
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