Protein Information

Name GABA B receptors
Synonyms GABA B R1; GABA B receptor; GABA B receptor 1; GABAB(1e); GABABR 1; GABABR1; GABBR 1; GABBR1…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
11247993 Traub RD, Bibbig R, Piechotta A, Draguhn R, Schmitz D: Synaptic and nonsynaptic contributions to giant ipsps and ectopic spikes induced by 4-aminopyridine in the hippocampus in vitro. J Neurophysiol. 2001 Mar;85(3):1246-56.

Experiments show that, indeed, the gap junction blocking compound carbenoxolone does suppress spontaneous large IPSCs, occurring in 4-AP plus ionotropic glutamate blockers, together with a GABA (B) receptor blocker; carbenoxolone also suppresses large, fast inward currents, corresponding to ectopic spikes, which occur in 4-AP.
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18992811 Engelmann J, van den Burg E, Bacelo J, de Ruijters M, Kuwana S, Sugawara Y, Grant K: Dendritic backpropagation and synaptic plasticity in the mormyrid electrosensory lobe. J Physiol Paris. 2008 Jul-Nov;102(4-6):233-45. Epub 2008 Oct 17.


Coincidence of backpropagating action potentials with parallel fibre input produces a strong local depolarisation that could be sufficient to cause local secretion of GABA, which might then cause plastic change through an action on presynaptic GABA (B) receptors.
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19535226 Wahab A, Heinemann U, Albus K: Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure like events in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23. Epub 2009 Jun 16.


PURPOSE: Seizure like events (SLEs) induced by low magnesium or 4-aminopyridine in organotypic hippocampal slice cultures (OHSCs) are resistant to standard antiepileptic drugs including phenobarbital, and 1,4-benzodiazepines [Albus, K., Wahab, A., Heinemann, U., 2008.
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12438533 Motalli R, D'Antuono M, Louvel J, Kurcewicz I, D'Arcangelo G, Tancredi V, Manfredi M, Pumain R, Avoli M: Epileptiform synchronization and GABA (B) receptor antagonism in the juvenile rat hippocampus. J Pharmacol Exp Ther. 2002 Dec;303(3):1102-13.

The GABA (B) receptor agonist baclofen enhances the epileptiform activity induced by 4-aminopyridine (4AP) in juvenile rat hippocampal slices.
85(1,1,1,5) Details
11530219 Louvel J, Papatheodoropoulos C, Siniscalchi A, Kurcewicz I, Pumain R, Devaux B, Turak B, Esposito V, Villemeure JG, Avoli M: GABA-mediated synchronization in the human neocortex: elevations in extracellular potassium and presynaptic mechanisms. Neuroscience. 2001;105(4):803-13.

Our data indicate that human neocortical networks challenged with 4-aminopyridine generate glutamatergic-independent, GABA-mediated potentials that are modulated by mu-opioid and GABA (B) receptors presumably located on interneuron terminals.
83(1,1,1,3) Details
18538357 Salah A, Perkins KL: Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology. 2008 Jul;55(1):47-54. Epub 2008 Apr 23.

Co-application of the convulsant 4-aminopyridine (4-AP) and the GABA (B) receptor antagonist CGP 55845 to adult guinea pig hippocampal slices elicits giant GABA-mediated postsynaptic potentials (GPSPs) and epileptiform discharges.
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16887273 Chen Q, Pan HL: Regulation of synaptic input to hypothalamic presympathetic neurons by GABA (B) receptors. Neuroscience. 2006 Oct 13;142(2):595-606. Epub 2006 Aug 2.

However, the inhibitory effect of baclofen on the frequency of mIPSCs and mEPSCs persisted in the presence of either Cd2+, a voltage-gated Ca2+ channel blocker, or 4-aminopyridine, a blocker of voltage-gated K+ channels.
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19176980 Inaba Y, D'Antuono M, Bertazzoni G, Biagini G, Avoli M: Diminished presynaptic GABA (B) receptor function in the neocortex of a genetic model of absence epilepsy. Neurosignals. 2009;17(2):121-31. Epub 2009 Jan 29.

We also obtained similar evidence by comparing the effects of baclofen on the rate of occurrence of synchronous GABAergic events recorded by WAG/Rij and NEC neocortical slices treated with 4-aminopyridine + glutamatergic receptor antagonists.
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15979855 Thuault SJ, Brown JT, Calver AR, Collingridge GL, Randall A, Davies CH: Mechanisms contributing to the exacerbated epileptiform activity in hippocampal slices expressing a C-terminal truncated GABA (B2) receptor subunit. Epilepsy Res. 2005 Jun;65(1-2):41-51.

We have previously shown that global loss of GABA (B) receptor function due to transgenic deletion of the GABA (B1) receptor subunit exacerbates epileptiform activity induced by pharmacological manipulations in hippocampal slices.
Furthermore, synchronous GABA (A) receptor-mediated potentials recorded in the presence of the potassium channel blocker 4-aminopyridine (4-AP, 100muM) and the ionotropic glutamate receptor antagonists NBQX (20muM) and D-AP5 (50muM) were significantly prolonged in duration in DeltaGB2-Ct versus WT slices.
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14654096 Avoli M, Benini R, de Guzman P, Omar A: GABA (B) receptor activation and limbic network ictogenesis. Neuropharmacology. 2004 Jan;46(1):43-51.

Rat brain slices containing interconnected hippocampus and entorhinal cortex (EC) responded to 4-aminopyridine (50 microM) application by generating: (i) CA3-driven interictal discharges that propagated to the EC; and (ii) N-methyl-D-aspartic (NMDA) acid receptor-dependent ictal events originating in EC (cf.
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15590725 Kantrowitz JT, Francis NN, Salah A, Perkins KL: Synaptic depolarizing GABA Response in adults is excitatory and proconvulsive when GABAB receptors are blocked. J Neurophysiol. 2005 May;93(5):2656-67. Epub 2004 Dec 8.

In the presence of 4-aminopyridine, interneurons fire synchronously, causing giant GABA-mediated postsynaptic potentials (GPSPs; GPSCs in voltage clamp) in CA3 pyramidal cells in hippocampal slices from adult guinea pigs.
We propose that GABA (B) receptors exert control over the postsynaptic depolarizing GABA response.
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16709723 Moldavan MG, Irwin RP, Allen CN: Presynaptic GABA (B) receptors regulate retinohypothalamic tract synaptic transmission by inhibiting voltage-gated Ca2+ channels. J Neurophysiol. 2006 Jun;95(6):3727-41.

Neither Ba2+ nor high extracellular K+ modified the baclofen-induced inhibition. 4-Aminopyridine (4-AP) significantly increased the EPSC amplitude and the charge transfer, and dramatically reduced the baclofen effect.
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14698756 Takeda M, Tanimoto T, Ikeda M, Kadoi J, Matsumoto S: Activaton of GABAB receptor inhibits the excitability of rat small diameter trigeminal root ganglion neurons. Neuroscience. 2004;123(2):491-505.

Baclofen-sensitive I (A) and I (K) currents were antagonized by K (+) channel blockers, 4-aminopyridine (4-AP) and tetraethylammonium (TEA).
A selective GABA (B) receptor agonist, baclofen, is known to suppress neuropathic pain.
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11011003 Wagner EJ, Reyes-Vazquez C, Ronnekleiv OK, Kelly MJ: The role of intrinsic and agonist-activated conductances in determining the firing patterns of preoptic area neurons in the guinea pig. Brain Res. 2000 Oct 6;879(1-2):29-41.

A smaller percentage of POA neurons (29%) expressed a transient outward, A-type K (+) current that was antagonized by a high concentration of 4-aminopyridine (3 mM).
Moreover, POA neurons responded to bath application of the mu-opioid receptor agonist DAMGO (93%) or the GABA (B) receptor agonist baclofen (83%) with a membrane hyperpolarization or an outward current.
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10670420 Jarolimek W, Baurle J, Misgeld U: Impaired inhibition of epileptiform activity by baclofen, but not by adenosine in the weaver hippocampus. Neuropharmacology. 2000 Jan 4;39(2):246-53.


Therefore, we investigated the affinity of GABA (B) receptors for the antagonist CGP55845A in wv/wv and +/+ hippocampi.
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