Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460

Buldakova, Svetlana; Vorobjev, Vladimir S.; Шаронова, И. Н.; Samoilova, Marina; Lg, Magazanik

doi:10.1016/s0006-8993(99)01970-8

Cited by 55 publications

(45 citation statements)

References 62 publications

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“…We did not observe any significant effects of CaMKI or inactCaMKI infusion of mEPSC frequency (data not shown). To assess the potential involvement of CP-AMPARs in mEPSC potentiation, we used IEM-1460, a well characterized rapid and reversible inhibitor, which shows greater selectivity than philanthotoxin-433 for CPAMPARs versus GluR2-containing AMPARs and NMDARs (Magazanik et al, 1997;Buldakova et al, 1999Buldakova et al, , 2007Samoilova et al, 1999;Gray et al, 2007). For example, IEM has no effect on basal AMPA EPSCs from CA1 pyramidal neurons, which do not contain CP-AMPARs (Monyer et al, 1991;Craig et al, 1993;Geiger et al, 1995;Wenthold et al, 1996;Sans et al, 2003), whereas IEM partially suppresses AMPA EPSCs of CA1 interneurons (Buldakova et al, 2007), which do contain some CPAMPARs (Racca et al, 1996;Laezza and Dingledine, 2004).…”

Section: Cam-kinase I Activity Promotes Synaptic Incorporation Of Cp-mentioning

confidence: 99%

Recruitment of Calcium-Permeable AMPA Receptors during Synaptic Potentiation Is Regulated by CaM-Kinase I

Guire¹,

Oh²,

Soderling³

et al. 2008

Journal of Neuroscience

142

154

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Ca2ϩ -permeable AMPA receptors (CP-AMPARs) at central glutamatergic synapses are of special interest because of their unique biophysical and signaling properties that contribute to synaptic plasticity and their roles in multiple neuropathologies. However, intracellular signaling pathways that recruit synaptic CP-AMPARs are unknown, and involvement of CP-AMPARs in hippocampal region CA1 synaptic plasticity is controversial. Here, we report that intracellular infusion of active CaM-kinase I (CaMKI) into cultured hippocampal neurons enhances miniature EPSC amplitude because of recruitment of CP-AMPARs, likely from an extrasynaptic pool. The ability of CaMKI, which regulates the actin cytoskeleton, to recruit synaptic CP-AMPARs was blocked by inhibiting actin polymerization with latrunculin A. CaMK regulation of CP-AMPARs was also confirmed in hippocampal slices. CA1 long-term potentiation (LTP) after theta bursts, but not high-frequency tetani, produced a rapid, transient expression of synaptic CP-AMPARs that facilitated LTP. This component of TBS LTP was blocked by inhibition of CaM-kinase kinase (CaMKK), the upstream activator of CaMKI. Our calculations show that adding CP-AMPARs numbering Ͻ5% of existing synaptic AMPARs is sufficient to account for the potentiation observed in LTP. Thus, synaptic expression of CP-AMPARs is a very efficient mechanism for rapid enhancement of synaptic strength that depends on CaMKK/ CaMKI signaling, actin dynamics, and the pattern of synaptic activity used to induce CA1 LTP.

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Section: Cam-kinase I Activity Promotes Synaptic Incorporation Of Cp-mentioning

confidence: 99%

Recruitment of Calcium-Permeable AMPA Receptors during Synaptic Potentiation Is Regulated by CaM-Kinase I

Guire¹,

Oh²,

Soderling³

et al. 2008

Journal of Neuroscience

142

154

View full text Add to dashboard Cite

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“…106,179 Because of their marked sensitivity to the presence of GluR2 subunits, PCCs have been used to characterize AMPAR in native neurons. Magazanik and colleagues have used dicationic adamantane and phenylcyclohexyl derivatives to indicate the relative presence of GluR2 subunits in AMPAR of acutely dissociated neurons of several types, from the sensorimotor cortex, hippocampus, striatum, and cerebellum, 102,180,181 and from hypoglossal motoneurons in brainstem slices. 182 Also by analyzing the maximum inhibition of AMPAR responses, it is possible to indicate where distinct populations of GluR2-lacking and GluR2-containing AMPAR co-exist within the same neuron.…”

Section: A Open Channel Blockmentioning

confidence: 99%

“…182 Also by analyzing the maximum inhibition of AMPAR responses, it is possible to indicate where distinct populations of GluR2-lacking and GluR2-containing AMPAR co-exist within the same neuron. 180 PhTX-433 (20) has been used to identify distinct populations of AMPAR on hippocampal interneurons, with PhTX-433 (20) sensitive receptors being localized at synapses from mossy fibers while insensitive AMPAR were localized to synapses from CA3 pyramidal neurons. 183 The voltage-dependence of AMPAR antagonism by externally applied polyamines sometimes takes on an unusual profile.…”

Section: A Open Channel Blockmentioning

confidence: 99%

AMPA receptor ligands: Synthetic and pharmacological studies of polyamines and polyamine toxins

Strømgaard

Mellor

2004

Medicinal Research Reviews

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Alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors (AMPAR), subtype of the ionotropic glutamate receptors (IGRs), mediate fast synaptic transmission in the central nervous system (CNS), and are involved in many neurological disorders, as well as being a key player in the formation of memory. Hence, ligands affecting AMPARs are highly important for the study of the structure and function of this receptor, and in this regard polyamine-based ligands, particularly polyamine toxins, are unique as they selectively block Ca2+ -permeable AMPARs. Indeed, endogenous intracellular polyamines are known to modulate the function of these receptors in vivo. In this study, recent developments in the medicinal chemistry of polyamine-based ligands are given, particularly focusing on the use of solid-phase synthesis (SPS) as a tool for the facile generation of libraries of polyamine toxin analogues. Moreover, the recent development of highly potent and very selective AMPAR ligands is described. Additionally, we provide a detailed account on the mechanism and site of action of AMPAR blockade by polyamine-based ligands, including examples of how these ligands are used as tools to study AMPAR, and a comparison with their action on other ionotropic receptors.

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“…The CluA2 lacking CP AMPA glutamate receptors were blocked by bath application of 100 μM IEM 1460 (IC 50 = 2.6 μM for CP AMPA, 1.1 mM for Ca imper meable AMPA, and more than 300 μM for NMDA [6].…”

Section: Resultsmentioning

confidence: 99%

“…Such cal cium permeable AMPARs (CP AMPARs) are wide spread in mammalian neurons at the earliest stages of ontogenesis, whereas in adult animals they are found mainly in the populations of spineless neurons [3], e.g., cortical GABAergic interneurons, giant cholin ergic neurons in the striatum, etc. [4][5][6]. Physiologi 1 The text was translated by the authors.…”

mentioning

confidence: 99%

The role of calcium-permeable AMPA receptors in disynaptic feedforward inhibition in the rat prefrontal cortex

Zaitsev

Kim

2012

Biochem. Moscow Suppl. Ser. A

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Calcium permeable AMPA receptors (CP AMPARs) play an important role in synaptic trans mission and plasticity, but they also can induce neuronal death under certain pathological conditions. The involvement of CP AMPARs in the pathogenesis of many diseases of the central nervous system makes them an attractive target for selective pharmacological blockade, to prevent and relieve pathological processes. However, the practical application of selective CP AMPAR channel blockers requires a thorough study of their effects on the functioning of neural networks under the normal conditions. The goal of this study was to clarify the role of CP AMPARs in the regulation of firing thresholds in different types of cortical neurons, as well as their involvement in maintaining the excitation/inhibition balance in the cortex. To do this, we have investigated the effects of CP AMPARs blockade on the amplitude of excitatory postsynaptic potentials (EPSPs) and the threshold of action potentials evoked by extracellular stimulation. Whole cell current clamp recordings were carried out from pyramidal cells and fast spiking interneurons in the slices of rat medial prefrontal cortex. CP AMPARs were blocked with a selective channel blocker IEM 1460 (100 µM), the dicationic derivative of adamantane. It was found that the blockade of CP AMPARs reduced the ampli tude EPSPs in interneurons but not in pyramidal cells. In addition, it reduced the firing threshold in pyrami dal cells via partial suppression of feedforward inhibition. Thus, the blockade of CP AMPA receptors shifts the balance between cortical excitation and inhibition toward excitation.

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Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460

Cited by 55 publications

References 62 publications

Recruitment of Calcium-Permeable AMPA Receptors during Synaptic Potentiation Is Regulated by CaM-Kinase I

Recruitment of Calcium-Permeable AMPA Receptors during Synaptic Potentiation Is Regulated by CaM-Kinase I

AMPA receptor ligands: Synthetic and pharmacological studies of polyamines and polyamine toxins

The role of calcium-permeable AMPA receptors in disynaptic feedforward inhibition in the rat prefrontal cortex

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