Abstract：
:Ionic currents from non-inactivating Shaker K(+)-channels were expressed in Xenopus oocytes and recorded with the cut-open oocyte voltage clamp technique. Kinetic properties of ionic currents were studied between 1.4 and 19 degrees C. The forward step of the last transition (...C --> O) of the activation pathway, just before the channel opening, was studied by the recovery of the ionic current after a short interval (< 500 microseconds) at a hyperpolarized potential (-90 mV) between two identical depolarizing pulses (0, 40 or 100 mV). Ionic currents under these experimental conditions are described by at least three kinetic components. The predominant kinetic component (corresponding to the ...C --> O transition) has a low temperature dependence (activation energy, Ea, around -5 kcal/mol) and it is voltage independent, suggesting that this step does not carry charge and has a mainly entropic energy barrier. The backward step (O --> C...) was studied from ionic tail currents at -120 mV after pulsing to 40 mV. The closure of the channel has a high temperature dependence (Q10 > 4), having an Ea of 24-25 kcal/mol. The closure of the channel also is voltage dependent, having a valence times fraction of the electric field, z beta of 0.5 eo. We conclude that the transition from the closed to the opened state has a net decrease in entropy and enthalpy, suggesting that the channel gets more ordered when it is open.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Rodríguez BM,Bezanilla Fdoi
10.1016/0028-3908(96)00111-6subject
Has Abstractpub_date
1996-01-01 00:00:00pages
775-85issue
7eissn
0028-3908issn
1873-7064pii
0028390896001116journal_volume
35pub_type
杂志文章abstract：:An infusion of dopamine for 13 days into the nucleus accumbens of rat caused biphasic peaks of hyperactivity responding during infusion and an enhanced locomotor responsiveness to the dopamine agonist (-)N-n-propylnorapomorphine [(-)NPA] after the infusion when rats where initially preselected as low activity responde...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(85)90073-5
更新日期：1985-03-01 00:00:00
abstract：:The gender difference in behavioral and hormonal response to stress is well known, but the underlying mechanism remains elusive. Arginine-vasopressin (AVP) and corticotrophin-releasing hormone (CRH) are two major regulatory peptides in the brain involved in stress regulation. Their response to stress has been shown to...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2008.03.016
更新日期：2008-06-01 00:00:00
abstract：:The roles of recognition sites for central neurotransmitters in the mediation of the behavioural effects of the putative 5-hydroxytryptamine (5-HT1) receptor agonist, RU 24969 [5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)1H indole] in the rat have been examined. The drug RU 24969 was found to have high affinity for 5-H...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(86)90014-6
更新日期：1986-08-01 00:00:00
abstract：:The stable transcription factor ΔFosB is induced in the nucleus accumbens (NAc) by chronic exposure to several drugs of abuse, and transgenic expression of ΔFosB in the striatum enhances the rewarding properties of morphine and cocaine. However, the mechanistic basis for these observations is incompletely understood. ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2011.08.046
更新日期：2011-12-01 00:00:00
abstract：:Despite evidence of local glycinergic circuits in the mature cerebellar nuclei the result of their activation remains unknown. Here, using whole cell recordings in rat cerebellar slices we demonstrated that after postnatal day 17 (>P17) glycinergic IPSCs can be readily evoked in large deep cerebellar nuclear neurons (...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.12.005
更新日期：2008-04-01 00:00:00
abstract：:24S-hydroxycholesterol (24S-HC) is a brain-derived product of lipid metabolism present in the systemic circulation, where its level can change significantly in response to physiological and pathophysiological conditions. Here, using electrophysiological and optical approaches, we have found a high sensitivity to 24S-H...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.01.030
更新日期：2017-05-01 00:00:00
abstract：:High concentrations of diazepam-binding inhibitor (DBI) mRNA have been detected in astrocytoma, suggesting that DBI-derived peptides may play a role in glial cell proliferation. In the present study, we have investigated the effect of a processing product of DBI, the octadecaneuropeptide ODN, on DNA synthesis in cultu...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(98)00231-7
更新日期：1999-05-01 00:00:00
abstract：:Depolarizing, hyperpolarizing and biphasic muscarinic responses have been described in hippocampal inhibitory interneurons, but the receptor subtypes and activity patterns required to synaptically activate muscarinic responses in interneurons have not been completely characterized. Using optogenetics combined with who...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.05.026
更新日期：2013-10-01 00:00:00
abstract：:Maternal behavior and anxiety are potently modulated by the brain corticotropin-releasing factor (CRF) system postpartum. Downregulation of CRF in limbic brain regions is essential for appropriate maternal behavior and an adaptive anxiety response. Here, we focus our attention on arguably the most important brain regi...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.02.019
更新日期：2018-05-01 00:00:00
abstract：:Serotonin (5-HT)1A and σ1 receptors have been implicated in psychiatric disorders. We previously found that combined 5-HT reuptake inhibition and σ1 receptor activation has a synergistic effect on prefrontal dopaminergic transmission in adrenalectomized/castrated mice lacking circulating steroid hormones. In the prese...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.06.026
更新日期：2013-12-01 00:00:00
abstract：:Brain injury generates the release of a multitude of factors including extracellular nucleotides, which exhibit bi-functional properties and contribute to both detrimental actions in the acute phase and also protective and reparative actions in the later recovery phase to allow neuroregeneration. A promising strategy ...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2015.09.002
更新日期：2016-05-01 00:00:00
abstract：:The basic unsolved questions concerning GABAA receptors are: "How many receptor subtypes exist?", "What subtypes are used by which types of neuron and where are they located on the cell?", and "What are the functions of the different subtypes?" As described in this Review, the cerebellum is an ideal vertebrate brain r...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/s0028-3908(96)00076-7
更新日期：1996-01-01 00:00:00
abstract：:The hippocampus may be functionally differentiated along its dorsoventral axis. In contrast to the wealth of data available on synaptic plasticity mechanisms in the dorsal hippocampus, little is known about synaptic plasticity processes in the intermediate hippocampus. Behavioral data suggest that this structure may p...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.02.017
更新日期：2013-11-01 00:00:00
abstract：:In urethane-chloralose anesthetized, neuromuscularly blocked, ventilated rats, microinjection of NMDA (12 pmol) into the right fourth thoracic segment (T4) spinal intermediolateral nucleus (IML) immediately increased ipsilateral brown adipose tissue (BAT) sympathetic nerve activity (SNA; peak +492% of control), expire...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.10.019
更新日期：2008-03-01 00:00:00
abstract：:Chronic administration of desipramine resulted in a significant decrease in the degree of stimulation of production of cyclic AMP by noradrenaline, isoproterenol and forskolin in slices of the cerebral cortex of the rat. In preparations of membranes from similarly treated animals, GppNHp- and forskolin-stimulated aden...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(87)90258-9
更新日期：1987-08-01 00:00:00
abstract：:Conantokin-G (con-G), conantokin-T (con-T), a truncated conantokin-R (con-R[1-17]), that functions the same as wild-type con-R, and variant sequences of con-T, were chemically synthesized and employed to investigate their selectivities as antagonists of glutamate/glycine-evoked ion currents in human embryonic kidney-2...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.04.016
更新日期：2007-07-01 00:00:00
abstract：:NMDA receptors have been known to play a central role in long-term potentiation at glutamatergic synapses in principal cells for thirty years. In contrast, their roles in the development and activity-dependent plasticity of synapses in inhibitory circuits have only recently begun to be understood. Progress has, to a g...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2013.03.004
更新日期：2013-11-01 00:00:00
abstract：:Trazodone is one of the most commonly prescribed medicines for treating depression and insomnia. However, the pharmacological mechanism of action underlying trazodone's unique effects is unclear. Despite its nanomolar affinity for 5HT(2A) receptors, histamine(1) receptors and alpha(1) adrenoceptors the drug is given a...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2007.05.011
更新日期：2007-08-01 00:00:00
abstract：:Although selective activation of the M1 muscarinic acetylcholine receptor (mAChR) subtype has been shown to improve cognitive function in animal models of neuropsychiatric disorders, recent evidence suggests that enhancing M4 mAChR function can also improve memory performance. Positive allosteric modulators (PAMs) tar...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2017.07.013
更新日期：2018-01-01 00:00:00
abstract：:Using the technique of microelectrophoresis on spinal neurones in pentobarbitone-anaesthetized rats, (1S,3R)-1-aminocyclo-pentane-1,3-dicarboxylate (1S,3R-ACPD) reversibly and dose-dependently enhanced responses to alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate (AMPA), kainate, N-methyl-D-aspartate (NMDA) and L...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(95)00046-9
更新日期：1995-08-01 00:00:00
abstract：:Cholecystokinin octapeptide (CCK-8), caerulein and seven out of ten analogues of caerulein produced in mice, after subcutaneous administration, a dose-dependent drop in rectal temperature. For the hypothermic effect, i.e. a decrease in temperature by at least 1.5 degree C, ED50's were estimated with these peptides and...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(82)90067-3
更新日期：1982-08-01 00:00:00
abstract：:Acetylcholine-induced currents were measured in partially depolarized mouse soleus muscles, denervated for 3-6 days by using a point voltage clamp. When 0.25 microM d-tubocurarine (d-Tc) was used, the weak currents provoked by 0.1 microM ACh, at a holding potential of -20 mV, were barely affected, while the large curr...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(90)90070-8
更新日期：1990-06-01 00:00:00
abstract：:Traumatic injuries to peripheral nerves are frequent, however, specific pharmacological treatments are currently lacking. Curcumin has antioxidant, anti-inflammatory and neuroprotective properties but high oral doses are required for therapeutic use, particularly due to its low bioavailability. The aim of the present ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2018.07.001
更新日期：2018-09-01 00:00:00
abstract：:There has been increasing interest in the rostromedial tegmental nucleus (RMTg), given its potential regulatory role in many aversion-related behaviors. The RMTg contains mostly GABAergic neurons, sends a dense inhibitory projection to dopamine neurons in the midbrain, and is rich with μ-opioid receptors (MOR). Like m...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2016.02.027
更新日期：2016-08-01 00:00:00
abstract：:Of the ionotropic glutamatergic receptors, the NMDA receptor is clearly implicated in the acute and chronic effects of ethanol; however, the role of the AMPA receptor in mediating the effects of ethanol in vivo is as yet unclear. Using mice deficient in the AMPA receptor subunit GluR1 (GluR1-/- mice), we investigated ...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/s0028-3908(03)00174-6
更新日期：2003-09-01 00:00:00
abstract：:Acromelic acid, a kainate derivative of natural origin, markedly increased intracellular Ca2+ concentration ([Ca2+]i) in cultured rat spinal neurons in a concentration dependent manner; the half effective concentration (EC50) was 1.3 microM. Acromelic acid was more potent in increasing [Ca2+]i than any other glutamate...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/0028-3908(94)90146-5
更新日期：1994-09-01 00:00:00
abstract：:There is increasing evidence that N-methyl-D-aspartate (NMDA) receptor blockade in the neonatal period has a long-lasting influence on brain and behavior development and has been linked to an increased risk for neuropsychiatric disorders in later life. We sought to determine whether postnatal NMDA receptor blockade ca...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2013.04.056
更新日期：2013-10-01 00:00:00
abstract：:The kynurenine pathway (KP) of tryptophan metabolism has emerged in recent years as a key regulator of the production of both neuroprotective (e.g. kynurenic and picolinic acid, and the essential cofactor NAD+) and neurotoxic metabolites (e.g. quinolinic acid, 3-hydroxykynurenine). The balance between the production o...
journal_title：Neuropharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.neuropharm.2016.03.024
更新日期：2017-01-01 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：:C57BL/6J mice were introduced to a nine arm radial maze without prior habituation and trained in the acquisition of a working memory task in 16 sessions, one session per day. In this maze mice need to climb onto an upward inclined bridge in order to reach and cross onto an arm. They received in each session an i.p. in...
journal_title：Neuropharmacology
pub_type： 杂志文章
doi：10.1016/j.neuropharm.2011.06.027
更新日期：2011-10-01 00:00:00
