Abstract：
:In slices of cerebral cortex from rat preloaded with [3H]GABA, muscimol produced a concentration-related inhibition of K(+)-evoked release of tritium with a pIC25 value of 7.80 +/- 0.39. Dimethylbarbituric acid (10 and 100 microM) and pentobarbitone (100 microM) significantly increased this value to 8.31 +/- 0.09, 9.91 +/- 0.21 and 8.50 +/- 0.21, respectively, whereas the steroid ligands alphaxalone (1 microM) and 5 beta-pregnane-3 alpha-ol-20-one (10 nM) had no significant effect. The 5 beta-pregnane-3 alpha-ol-20-one and 5 beta-pregnane-3,20-dione produced a concentration-related increase in K(+)-evoked release of tritium alone. These data suggest that the GABAA-like autoreceptor may be modulated by barbiturates but not by steroids and thus may be different from the postsynaptic GABAA receptor.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Ennis C,Minchin MCdoi
10.1016/0028-3908(93)90156-wsubject
Has Abstractpub_date
1993-04-01 00:00:00pages
355-7issue
4eissn
0028-3908issn
1873-7064journal_volume
32pub_type
杂志文章abstract：:Nimodipine is a 1,4-dihydropyridine (DHP) calcium channel blocker which is used in the treatment of neurological deficits associated with subarachnoid hemorrhage. Small angle x-ray diffraction, differential scanning calorimetry, and equilibrium and kinetic binding techniques were used to study the interaction of nimod...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(94)90015-9
更新日期：1994-02-01 00:00:00
abstract：:Alcohol use disorder (AUD) is a serious public health problem that results in tremendous social, legal and medical costs to society. Unlike other addictive drugs, there is no specific molecular target for ethanol (EtOH). Here, we report a novel molecular target that mediates EtOH effects at concentrations below those ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.01.021
更新日期：2019-05-01 00:00:00
abstract：:The pharmacotherapy for the treatment of pain is an active area of investigation. There are effective drugs to treat this problem, but there is also a need to find alternative treatments free of undesirable side effects. In the present work the capacity of a series of flavonoids to bind to the μ opioid receptor was ev...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.04.020
更新日期：2013-09-01 00:00:00
abstract：:The dorsal striatum plays a key role in motor control and cognitive processes. Proper functioning of the striatum relies on the fine dynamic balance between the direct pathway projection medium spiny neurons (MSNs) that express D1 dopamine receptor (D1 MSNs) and indirect pathway projection MSNs that express D2 dopamin...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.03.037
更新日期：2016-08-01 00:00:00
abstract：:Granule cell axon terminals of rat cerebellum possess benzodiazepine-insensitive GABA(A) receptors mediating glutamate release. We have investigated the ability of benzodiazepines, ethanol and furosemide to modulate the function of these receptors in the cerebellum of alcohol-tolerant (AT) and alcohol-nontolerant (ANT...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(99)00025-8
更新日期：1999-09-01 00:00:00
abstract：:The effect of drugs which down-regulate the function of GABA at the level of the GABA/benzodiazepine receptor complex was studied on the conflict test in the rat. The GABA receptor antagonist, bicuculline, and the blockers of the GABA-receptor-coupled chloride channel, picrotoxin and pentylenetetrazol, produced a dose...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(86)90181-4
更新日期：1986-05-01 00:00:00
abstract：:Ethylcholine mustard aziridinium ion (AF64A), or vehicle, was infused bilaterally (3 nmol/3 microliter per side) into the lateral ventricles of rats. The effect of such treatment on various cholinergic responses was measured in the hippocampus, cortex and striatum. Potassium-stimulated release of acetylcholine from su...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(85)90031-0
更新日期：1985-05-01 00:00:00
abstract：:Administration of stimulant and non-stimulant drugs that inhibit monoamine reuptake is known to improve cognitive and behavioral symptoms of attention deficit hyperactivity disorder (ADHD). Although this may reflect acute actions of these drugs, clinical observations suggest that prolonged treatment with these agents ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2009.08.007
更新日期：2009-12-01 00:00:00
abstract：:Following intraperitoneal administration, the selective cAMP phosphodiesterase (PDE) inhibitors rolipram, ICI 63 197 and Ro 20-1724 were investigated in mice in comparison with imipramine for their effectiveness in two classical test models for prediction of clinical antidepressant activity: antagonism of reserpine-in...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(83)90239-3
更新日期：1983-03-01 00:00:00
abstract：:Excessive glutamate-mediated synaptic transmission and secondary excitotoxicity have been proposed as key determinants of neurodegeneration in many neurological diseases. Soluble mediators of inflammation have recently gained attention owing to their ability to enhance glutamate transmission and affect synaptic sensit...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2014.09.022
更新日期：2015-09-01 00:00:00
abstract：:This paper evaluates the involvement of hippocampal ATP-sensitive potassium channels (K(ATP)) in learning and memory. After confirming expression of the Kir6.2 subunit in the CA3 region of C57BL/6J mice, we performed intra-hippocampal pharmacological injections of specific openers and blockers of K(ATP) channels. The ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2008.11.001
更新日期：2009-03-01 00:00:00
abstract：:In the rat subthalamic nucleus, which plays a critical role in the control of motor behaviour, specific binding of [3H]-prazosin was detected by radioligand binding to homogenates and by autoradiography in slices. [3H]-Prazosin binding to homogenates (Bmax 71 +/- 5 fmol/mg protein; Kd 0.27 +/- 0.05 nM) was competed fo...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(03)00315-0
更新日期：2003-12-01 00:00:00
abstract：:Aberrant increases in NMDA receptor (NMDAR) signaling contributes to central nervous system sensitization and chronic pain by activating neuronal nitric oxide synthase (nNOS) and generating nitric oxide (NO). Because the scaffolding protein postsynaptic density 95kDA (PSD95) tethers nNOS to NMDARs, the PSD95-nNOS comp...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.05.038
更新日期：2015-10-01 00:00:00
abstract：:Intracerebroventricular administration of neurotensin (NT) suppresses locomotor activity. However, the brain regions that mediate the locomotor depressant effect of NT and receptor subtype-specific mechanisms involved are unclear. Using a brain-penetrating, selective NT receptor type 1 (NTS1) agonist PD149163, we inve...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2014.05.046
更新日期：2014-10-01 00:00:00
abstract：:The homotrimeric P2X3 receptor, one of the seven members of the ATP-gated P2X receptor family, plays a crucial role in sensory neurotransmission. P2X3 receptor antagonists have been identified as promising drugs to treat chronic cough and are suggested to offer pain relief in chronic pain such as neuropathic pain. Her...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2019.107749
更新日期：2019-11-01 00:00:00
abstract：:Tryptophan (Trp) availability for the kynurenine pathway (KP) across the life span is discussed. Free (non-albumin-bound) plasma Trp is the major determinant of the flux of Trp down the KP. Flux is the major determinant of kynurenine metabolite formation and is more effective than induction of hepatic Trp 2,3-dioxygen...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2015.11.015
更新日期：2017-01-01 00:00:00
abstract：:The selective benzodiazepine antagonist RO 15-1788, labelled with carbon 11 [11C] RO 15-1788, as a specific marker, together with positron emission tomography, allows the in vivo study of benzodiazepine receptors in primates. In addition, when coupled with recordings of electroencephalographic activity, this method of...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(87)90171-7
更新日期：1987-10-01 00:00:00
abstract：:Exposure to ethanol (EtOH) during fetal development can lead to long-lasting alterations, including deficits in fine motor skills and motor learning. Studies suggest that these are, in part, a consequence of cerebellar damage. Cerebellar granule neurons (CGNs) are the gateway of information into the cerebellar cortex....
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.11.020
更新日期：2014-04-01 00:00:00
abstract：:Depression is a polygenic and highly complex psychiatric disorder that is currently a major burden on society. Depression is highly heterogeneous in presentation and frequently exhibits high comorbidity with other psychiatric and somatic disorders. Commonly used treatments, such as selective serotonin reuptake inhibit...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2011.02.017
更新日期：2011-09-01 00:00:00
abstract：:The modulation of insect behavior for the purpose of controlling the spread of infectious diseases has been the task of a few insect repellents for which the mechanistic modes of action on odorant receptors (ORs) are unclear. Here, we study the effects of the repellents DEET and IR3535, and a novel OR co-receptor (Orc...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2012.01.004
更新日期：2012-04-01 00:00:00
abstract：:L-AP4 is an agonist at the presynaptic metabotropic receptor subtypes mGluR4, mGluR6 and mGluR7. In vitro, L-AP4 has been shown to reduce glutamate release and thereby suppress hippocampal excitatory transmission. Little data is available with regard to the actions of this compound in vivo. This study examined the eff...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(95)00081-g
更新日期：1995-08-01 00:00:00
abstract：:The efficacy of antidepressant drugs with serotonergic, noradrenergic, or dual reuptake inhibition was evaluated in reversing carrageenan-induced thermal hyperalgesia and mechanical allodynia in rats. Duloxetine (1-30mg/kg, i.p.), a balanced serotonergic-noradrenergic reuptake inhibitor (SNRI), was equiefficacious and...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2006.08.005
更新日期：2006-12-01 00:00:00
abstract：:In the solitary tract nucleus, neuronal responsiveness to synaptic input from peripheral afferent fibres has been found to decrease as the frequency of that input is increased. The present study investigated the possibility that glycine and gamma-aminobutyric acid (GABA) are (1) involved in this phenomenon of "frequen...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(91)90149-6
更新日期：1991-03-01 00:00:00
abstract：:Benzodiazepines (BZDs) and barbiturates exert their CNS actions by binding to GABA-A receptors (GABARs). The structural mechanisms by which these drugs allosterically modulate GABAR function, to either enhance or inhibit GABA-gated current, are poorly understood. Here, we used the substituted cysteine accessibility me...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2010.11.009
更新日期：2011-02-01 00:00:00
abstract：:Methylphenidate (MPH, Ritalin©) is widely used in the treatment of Attention Deficit Hyperactivity Disorder and recently as a drug of abuse. Although the effect of MPH has been studied in brain regions such as striatum and prefrontal cortex (PFC), the hippocampus has received relatively little attention. It is known t...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.07.003
更新日期：2015-12-01 00:00:00
abstract：:Opiates addiction is characterized by its long-term persistence. In order to study the enduring changes in long-term memory in hippocampus, a pivotal region for this process, we used suppression subtractive hybridization to compare hippocampal gene expression in morphine and saline-treated rats. Animals were subjected...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2006.08.012
更新日期：2007-02-01 00:00:00
abstract：:Mutations in LRRK2 (leucine-rich repeat kinase 2) are found associated with both sporadic and familial Parkinson's disease (PD). Pathogenic mutations are localized to the catalytic domains of LRRK2, including kinase and GTPase domains. Altered catalytic activity correlates with neurotoxicity, indicating that targeting...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2014.05.020
更新日期：2014-10-01 00:00:00
abstract：:Electrophysiological studies suggest that 5-HT autoreceptor desensitization may be responsible for the delayed clinical efficacy of some antidepressant drugs, such as selective 5-HT reuptake inhibitors (SSRI) and certain MAO inhibitors (MAOI). In the present study we have used in vivo microdialysis to test this hypoth...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(94)90062-0
更新日期：1994-03-01 00:00:00
abstract：:Serotonin (5-HT) neurons are involved in wake promotion and exert a strong inhibitory influence on rapid eye movement (REM) sleep. Such effects have been ascribed, at least in part to the action of 5-HT at post-synaptic 5-HT1A receptors (5-HT1AR) in the brainstem, a major wake/REM sleep regulatory center. However, the...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.06.014
更新日期：2018-08-01 00:00:00
abstract：:The majority of existing research on the function of metabotropic glutamate (mGlu) receptor 1 focuses on G protein-mediated outcomes. However, similar to other G protein-coupled receptors (GPCR), it is becoming apparent that mGlu1 receptor signaling is multi-dimensional and does not always involve G protein activation...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2015.02.007
更新日期：2015-06-01 00:00:00
