Abstract：
:Structural analogues of ZAPA, Z-3-[(aminoiminomethyl)thio]prop-2-enoic acid, an isothiouronium analogue of GABA, are potent GABAA agonists as seen in the isolated guinea-pig ileum and in the facilitation of [3H]diazepam binding to rat brain membranes. Compounds with guanidino or amidine groups replacing the amino functionality of GABA were also found to be active. The highest activity was displayed by the isothiouronium salts in which the conformational flexibility of the molecule is restricted by a Z-substituted carbon-carbon double bond. A series of bis-isothiouronium compounds was prepared from aliphatic alpha, omega-bis-thioureas as mixtures of E and Z adducts. Maximum GABAA agonist activity for this series was found with a C6-C8 carbon chain, and the results were consistent with an interaction at the GABAA receptor with only one end of the molecule, rather than the more potent effect expected of a molecule bridging two active sites. GABAA antagonist/partial agonist activity was observed on the guinea pig isolated ileum for a number of different analogue types, with the most potent being bis-isothiouronium derivatives. None of the substituted derivatives of ZAPA was as active as ZAPA itself, and maximum GABAA activity was found in the n-pentyl and n-hexyl analogues.
journal_name
Neurochem Intjournal_title
Neurochemistry internationalauthors
Allan RD,Dickenson HW,Johnston GA,Kazlauskas R,Mewett KNdoi
10.1016/s0197-0186(96)00094-0subject
Has Abstractpub_date
1997-06-01 00:00:00pages
583-91issue
6eissn
0197-0186issn
1872-9754pii
S0197-0186(96)00094-0journal_volume
30pub_type
杂志文章abstract：:The effects of ?-amino-n-butyric acid (GABA), (+)bicuculline, isoguvacine and 3-(4-chlorophenyl)-4-aminobutyrate [(+/-)baclofen] on the K-induced release of [(3)H]acetylcholine (ACh) were studied in the superior cervical ganglia of the rat in vitro. GABA and isoguvacine inhibited [(3)H]ACh release and these inhibition...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(86)90193-2
更新日期：1986-01-01 00:00:00
abstract：:D-aspartate is present in significant concentrations throughout the nervous tissue but its physiological role is still under discussion. Here, we report the process of d-aspartate release in retinal cells. [(3)H]-d-aspartate release occurs through a glutamate/aspartate exchange mechanism using excitatory amino acid tr...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2011.03.001
更新日期：2011-06-01 00:00:00
abstract：:A purification procedure to obtain peroxisomes (microperoxisomes) from the brain of suckling rats is reported. A P2 fraction, (crude light mitochondria) frozen and thawed seven times, was subfractionated yielding a P4 fraction, 4-fold enriched in catalase activity with respect to the cytoplasmic extract S1. The P4 fra...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(93)90116-m
更新日期：1993-09-01 00:00:00
abstract：:Recent in vitro studies have revealed that benzodiazepines, opiates, barbiturates and ethanol might influence GABA binding to CNS membrane sites. Further studies of such interactions might be helpful for explaining both the mechanisms of action of these psychoactive agents and the tolerance/dependence that might resul...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(83)90062-1
更新日期：1983-01-01 00:00:00
abstract：:Several metabolic transformations of vitamin A have now been found in the pigment epithelium of cattle retina, leading to the hypothesis that there may be a vitamin A cycle in these cells. A retinol binding protein of MW ? 17,000 in pigment epithelial cytosol has been identified independently in several laboratories. ...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(80)90055-8
更新日期：1980-01-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(94)90010-8
更新日期：1994-06-01 00:00:00
abstract：:Glycine transporter GlyT1 plays important role in maintaining accurate glycine concentration in local brain microenvironment. Transporting efficiency of GlyT1 is strongly affected by the state of its distal C-terminus, which regulates transporter trafficking and cellular surface density. Using selected range of antibo...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2010.06.003
更新日期：2010-10-01 00:00:00
abstract：:This paper describes the background in experiment and theory on which present-day studies of the biochemistry of learning and memory are based. It then reviews specifically the use of passive avoidance training in the day-old chick as a model for the analysis of the cellular events associated with memory-formation. It...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(89)90055-7
更新日期：1989-01-01 00:00:00
abstract：:Resistance to inhibitors of cholinesterase (RIC) -3 promotes the maturation (folding and assembly) of neuronal nicotinic acetylcholine receptors (nAChRs) as a molecular chaperone. The modulation effects of RIC-3 on homomeric α7 nAChRs are always positive, but its effects on heteromeric subtypes are inconsistent among ...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2017.10.007
更新日期：2018-05-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(85)90156-1
更新日期：1985-01-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/s0197-0186(02)00137-7
更新日期：2003-04-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(80)90021-2
更新日期：1980-01-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2019.104548
更新日期：2019-12-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2019.104479
更新日期：2019-10-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(81)90008-5
更新日期：1981-01-01 00:00:00
abstract：:Glutamate is an excitotoxin responsible for causing neuronal damage associated with mitochondria dysfunction. We have analyzed the relationship between the mitochondrial respiratory rate, the membrane potential (delta psi) and the activity of mitochondrial complexes in retinal cells in culture, used as neuronal models...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/s0197-0186(99)00107-2
更新日期：2000-02-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/s0197-0186(98)00013-8
更新日期：1998-08-01 00:00:00
abstract：:Lithium is well established as a treatment of manic-depressive illness. As for the mechanism of action of lithium, it is proposed that lithium has effects on intracellular calcium ion (Ca2+) movement. But there are few reports in which the effects of lithium on intracellular Ca2+ movement are observed in the mammalian...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(94)00130-m
更新日期：1995-03-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(94)90093-0
更新日期：1994-05-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
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更新日期：1991-01-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(92)90183-r
更新日期：1992-10-01 00:00:00
abstract：:Streptozotocin (STZ) is a glucosamine-nitrosourea commonly used to induce long-lasting models of diabetes mellitus and Alzheimer's disease. Direct toxicity of STZ on the pancreas and kidneys has been well characterized, but the acute effect of this compound on brain tissue has received less attention. Herein, we inves...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2019.04.013
更新日期：2019-09-01 00:00:00
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journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(84)90045-7
更新日期：1984-01-01 00:00:00
abstract：:Alpha-synuclein (ASN), a 140-amino acid protein, is richly expressed in presynaptic terminals in the central nervous system, where it plays a role in synaptic vesicle function. However, if it is altered and accumulated it is involved in neurodegeneration as Parkinson's disease (PD). ASN contained 35-amino acid domain ...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2006.01.025
更新日期：2006-09-01 00:00:00
abstract：:The presence of corticotropin-releasing hormone (CRH) receptors has been previously demonstrated in corticotrophs from normal pituitaries using a method combining immunocytochemistry and liquid emulsion autoradiography. The aim of this study was to compare the characteristics of the 125I-Tyr0-hCRH binding in corticotr...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/s0197-0186(96)00102-7
更新日期：1997-03-01 00:00:00
abstract：:The turnover of phospholipids was compared in peripheral nerves of Trembler dysmelinating mutant and control mice, after intraperitoneal and local injection of labeled ethanolamine. In the mutant sciatic nerve, neurochemical analysis showed that [(14)C]ethanolamine is incorporated into EGP (ethanolamine glycerophospho...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(90)90045-u
更新日期：1990-01-01 00:00:00
abstract：:The developmental profiles of the neurotransmitter recognition site, labeled by [(3)H]muscimol, and of the two main modulatory sites, labeled by [(3)H]flunitrazepam and [ (35)S ]t- butylbicyclophosphorothionate , respectively, within the GABA(A) receptor complex, have been determined in chick tectal lobes between embr...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(87)90032-5
更新日期：1987-01-01 00:00:00
abstract：:Oxidative stress (OS) has been related to cocaine's actions and also to numerous nervous system pathologies, including seizures. The purpose of this work was to determine the alterations in glutathione (GSH) content, nitrite/nitrate and MDA levels after cocaine-induced toxicity. Male Swiss mice were injected (i.p.) wi...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/j.neuint.2009.10.001
更新日期：2010-01-01 00:00:00
abstract：:Human atrial natriuretic peptide (Ser 99-Tyr 126) was rapidly degraded by both choroid plexus and hypothalamic membranes with a complex pattern of cleavage. The use of protease inhibitors allowed a preliminary characterization of the enzymes involved in the hydrolysis of the Ser-Phe and Phe-Arg bonds of iodine-labelle...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(88)90176-3
更新日期：1988-01-01 00:00:00
abstract：:Ethanol (15% v/v) was administered in the drinking water to male Wistar rats over period of 3 months. Binding properties of muscarinic receptors were studied in synaptosomes from selected brain areas using [(3)H]quinuclidinyl benzilate and its displacement by the selective antagonist, pirenzepine and the agonist, carb...
journal_title：Neurochemistry international
pub_type： 杂志文章
doi：10.1016/0197-0186(88)90027-7
更新日期：1988-01-01 00:00:00
