Protein Information

Name glutamate receptors (protein family or complex)
Synonyms Glutamate receptor; Glutamate receptors

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
14770276 Wejksza K, Rzeski W, Parada-Turska J, Zdzisinska B, Rejdak R, Kocki T, Okuno E, Kandefer-Szerszen M, Zrenner E, Turski WA: Kynurenic acid production in cultured bovine aortic endothelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Mar;369(3):300-4. Epub 2004 Feb 10.

Kynurenic acid (KYNA) is a broad-spectrum antagonist at all subtypes of ionotropic glutamate receptors, but is preferentially active at the strychnine-insensitive glycine allosteric site of the N-methyl-D-aspartate (NMDA) receptor and is also a non-competitive antagonist at the alpha7 nicotinic receptor.
31(0,1,1,1) Details
16457470 Zielinska E, Kocki T, Saran T, Borbely S, Kuc D, Vilagi I, Urbanska EM, Turski WA: Effect of pesticides on kynurenic acid production in rat brain slices. Ann Agric Environ Med. 2005;12(2):177-9.

Kynurenic acid (KYNA) is a broad spectrum antagonist of ionotropic glutamate receptors, preferentially active at the strychnine-insensitive glycine allosteric site of the N-methyl-D-aspartate (NMDA) receptor, and a noncompetitive antagonist of alpha7 nicotinic receptor.
31(0,1,1,1) Details
14523604 Taccola G, Marchetti C, Nistri A: Effect of metabotropic glutamate receptor activity on rhythmic discharges of the neonatal rat spinal cord in vitro. Exp Brain Res. 2003 Dec;153(3):388-93. Epub 2003 Oct 2.

To extend our understanding of the network-based properties which enable a neuronal circuit to produce sustained electrical oscillations, we explored the potential contribution of metabotropic glutamate receptors (mGluRs) to generation of rhythmic discharges.
The regular, synchronous bursting emerging in the presence of strychnine and bicuculline was accelerated by t-ACPD with a commensurate decrease in single burst length, an effect antagonized by MCPG which per se did not affect bursting.
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18805436 Yang CR, Svensson KA: Allosteric modulation of NMDA receptor via elevation of brain glycine and D-serine: the therapeutic potentials for schizophrenia. Pharmacol Ther. 2008 Dec;120(3):317-32. Epub 2008 Aug 27.

Ionotropic AMPA and NMDA glutamate receptors are ligand-gated ion channels that mediate fast synaptic transmission in the brain and play a crucial role in learning and memory.
Endogenous glycine and D-serine both act as co-agonists on the strychnine-insensitive GlyB site on the NMDA receptor, and along with glutamate, co-activate the NMDA receptor.
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11118498 Smith AJ, Owens S, Forsythe ID: Characterisation of inhibitory and excitatory postsynaptic currents of the rat medial superior olive. J Physiol. 2000 Dec 15;529 Pt 3:681-98.

Following blockade of glutamate receptors, a monosynaptic strychnine-sensitive response was evoked on stimulation of the MNTB, indicative of a glycine receptor-mediated IPSC.
31(0,1,1,1) Details
8103091 Zhou ZJ, Fain GL, Dowling JE: The excitatory and inhibitory amino acid receptors on horizontal cells isolated from the white perch retina. J Neurophysiol. 1993 Jul;70(1):8-19.

The results demonstrated the existence of an inhomogeneous distribution of strychnine-sensitive glycine receptors and a homogeneous distribution of non-NMDA type glutamate receptors among the four types of white perch horizontal cells.
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8624016 Onaka M, Minami T, Nishihara I, Ito S: Involvement of glutamate receptors in strychnine- and bicuculline-induced allodynia in conscious mice. Anesthesiology. 1996 May;84(5):1215-22.
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9765506 Weaver CD, Partridge JG, Yao TL, Moates JM, Magnuson MA, Verdoorn TA: Activation of glycine and glutamate receptors increases intracellular calcium in cells derived from the endocrine pancreas. Mol Pharmacol. 1998 Oct;54(4):639-46.

GK-P3 cells express the first strychnine-sensitive glycine receptors reported in a permanent cell line.
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9266432 Fossom LH, Skolnick P: Chronic administration of a partial agonist at strychnine-insensitive glycine receptors: a novel experimental approach to the treatment of ischemias. J Neural Transm Suppl. 1997;49:235-44.

Pharmacological studies indicate that activation of both ionotropic and metabotropic glutamate receptors can substantially contribute to excitotoxic cell damage (Choi, 1992; Pizzi et al., 1993; Sheardown et al., 1993; Xue et al., 1994).
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16876205 Wagner J, Luhmann HJ: Activation of metabotropic glutamate receptors induces propagating network oscillations in the intact cerebral cortex of the newborn mouse. Neuropharmacology. 2006 Sep;51(4):848-57. Epub 2006 Jul 28.

Blockade of GABA-A receptors with gabazine did not influence the ACPD-induced network activity, but the glycine antagonist strychnine caused a significant decrease in the frequency, amplitude and duration of the oscillations.
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11741402 Basile AS, Koustova E, Ioan P, Rizzoli S, Rogawski MA, Usherwood PN: IgG isolated from LP-BM5 infected mouse brain activates ionotropic glutamate receptors. Neurobiol Dis. 2001 Dec;8(6):1069-81.

Glycine-dependent and -independent currents were unaffected by tetrodotoxin, strychnine, the transmembrane Cl- gradient or d-tubocurare.
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14530208 Rouaud E, Billard JM: D-cycloserine facilitates synaptic plasticity but impairs glutamatergic neurotransmission in rat hippocampal slices. Br J Pharmacol. 2003 Nov;140(6):1051-6. Epub 2003 Oct 6.

We found that DCS decreased neurotransmission mediated by alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainate subtypes of glutamate receptors.
This inhibition was not prevented by the gamma-aminobutyric acid GABAA antagonist bicuculline, but was antagonized by the glycine antagonist strychnine. 4.
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14622220 Marchetti C, Taccola G, Nistri A: Distinct subtypes of group I metabotropic glutamate receptors on rat spinal neurons mediate complex facilitatory and inhibitory effects. Eur J Neurosci. 2003 Oct;18(7):1873-83.

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9498236 Hantzschel A, Andreas K: Efficacy of glutamate receptor antagonists in the management of functional disorders in cytotoxic brain oedema induced by hexachlorophene. Pharmacol Toxicol. 1998 Feb;82(2):80-8.

In order to examine whether glutamate receptors are involved in mediating functional disorders due to neurotoxic brain damage, we have studied the protective effects of several competitive and non-competitive antagonists using adult male Wistar rats in a simple "ladder-test" for assessing coordinative motor behaviour.
Similar effects were observed with 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) in the dose of 0.8 mg/kg intraperitoneally, an antagonist interacting both with the strychnine-insensitive binding site for glycine within the NMDA receptor complex and with the kainate (+/-)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor complex.
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11600626 Frech MJ, Perez-Leon J, Wassle H, Backus KH: Characterization of the spontaneous synaptic activity of amacrine cells in the mouse retina. J Neurophysiol. 2001 Oct;86(4):1632-43.

Only four amacrine cells showed glycinergic sIPSCs that were inhibited by strychnine (1 microM).
In addition to ionotropic glutamate receptors, amacrine cells express two types of inhibitory receptors, GABA (A) receptors (GABA (A) Rs) and glycine receptors (GlyRs).
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11952420 Menzikov SA, Menzikova OV: Effect of activators and blockers of ligand-regulated ion channels on the activity of the Cl-stimulated Mg2+-ATPase of the plasma membrane fraction from bream (Abramis brama L.) brain. Biochemistry. 2002 Feb;67(2):233-9.

Effects of GABA, glycine, acetylcholine, and glutamate (agonists of the GABAa/benzodiazepine, glycine, choline, and glutamate receptors, respectively) at concentrations in the range 10 (-8)-10 (-4) M on the activity of "basal" Mg (2+)-ATPase of the plasma membrane fraction from bream brain and on its activation by Cl (-) were investigated.
The activation of "basal" Mg (2+)-ATPase by neuromediators was decreased by blockers of the corresponding receptors (picrotoxin, strychnine, benztropine mesylate, and D-2-amino-5-phosphonovaleric acid).
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9671104 Garcia MC, Celuch SM, Adler-Graschinsky E: Involvement of GABA and glutamate receptors in the blood pressure responses to intrathecally injected sodium nitroprusside in anesthetized rats. Eur J Pharmacol. 1998 May 22;349(2-3):245-52.

The blood pressure responses to sodium nitroprusside were not modified by blockade of muscarinic receptors with methyl atropine (164 nmol, i.t.), or of nicotinic receptors with hexamethonium (211 nmol, i.t.), of alpha1-adrenoceptors with prazosin (3.1 nmol, i.t.), of alpha2-adrenoceptors with yohimbine (2.8 micromol/kg, i.v.), of 5-HT receptors with methysergide (5.1 micromol/kg, i.v.), or of glycine receptors with strychnine (65 nmol, i.t.).
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9080374 Russo RE, Nagy F, Hounsgaard J: Modulation of plateau properties in dorsal horn neurones in a slice preparation of the turtle spinal cord. J Physiol. 1997 Mar 1;499 ( Pt 2):459-74.

All ACPD-induced effects were blocked by alpha-methyl-4-carboxyphenylglycine (MCPG, 0.5-1 mM), a selective antagonist of metabotropic glutamate receptors.
The tetanic stimulus facilitated wind-up and after-discharges even when fast synaptic transmission was blocked by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX, 10-20 microM), (+/-)-2-amino-5-phosphonopentanoic acid (AP5, 100 microM), bicuculline (10-20 microM) and strychnine (5-20 microM). 2.
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15555633 Ran I, Mathers DA, Puil E: Pentobarbital induces thalamic oscillations in brain slices, modulated by GABA and glycine receptors. Neuropharmacology. 2004 Dec;47(7):985-93.

Kynurenate-sensitive glutamate receptors were essential for oscillations.
GABA (B) antagonism (CGP 35348, 100 nM), or antagonism of glycine receptors (strychnine, 1 microM) suppressed oscillations at 1-4 and 11-15 Hz.
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11564428 Fontana G, Taccola G, Galante J, Salis S, Raiteri M: AMPA-evoked acetylcholine release from cultured spinal cord motoneurons and its inhibition by GABA and glycine. Neuroscience. 2001;106(1):183-91.

The glutamate receptors involved are AMPA type since the AMPA-evoked [(3) H] acetylcholine release was blocked by LY303070 and was potentiated by the antidesensitizing agent cyclothiazide.
Glycine, acting at strychnine-sensitive receptors, also inhibited the effect of AMPA, but only in part.
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8809837 Haji A, Pierrefiche O, Foutz AS, Champagnat J, Denavit-Saubie M, Takeda R: Pharmacological properties of peripherally induced postsynaptic potentials in bulbar respiratory neurons of decerebrate cats. Neurosci Lett. 1996 Jun 14;211(1):17-20.

Inhibitory postsynaptic potentials (IPSPs) evoked by stimulation of the superior laryngeal nerve or vagus nerve were depressed by bicuculline in all 22 neurons tested, but not modified by strychnine.
The present results suggest that the peripherally induced IPSPs are mediated through gamma-aminobutyric acid (GABA) A receptors and the EPSPs through non-NMDA glutamate receptors in bulbar respiratory neurons.
1(0,0,0,1) Details
10367956 Jensen RJ: Responses of directionally selective retinal ganglion cells to activation of AMPA glutamate receptors. Vis Neurosci. 1999 Mar-Apr;16(2):205-19.

Pretreatment of retinas with the glycine receptor antagonist strychnine (1-2 microM) did not alter the effects of AMPA.
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11020764 Cheng G, Kendig JJ: Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors. Anesthesiology. 2000 Oct;93(4):1075-84.

Block of inhibitory gamma-aminobutyric acid A and glycine receptors by bicuculline (20 micrometer) or strychnine (2 micrometer) or both did not significantly reduce the effects of enflurane on glutamate-evoked currents.
This study was designed to test the hypothesis that enflurane acts directly on motor neurons to inhibit excitatory synaptic transmission at glutamate receptors.
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10899215 Schwartz NE, Alford S: Physiological activation of presynaptic metabotropic glutamate receptors increases intracellular calcium and glutamate release. J Neurophysiol. 2000 Jul;84(1):415-27.

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11134626 Zhong J, Gerber G, Kojic L, Randic M: Dual modulation of excitatory synaptic transmission by agonists at group I metabotropic glutamate receptors in the rat spinal dorsal horn. Brain Res. 2000 Dec 29;887(2):359-77.

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14984404 Taccola G, Marchetti C, Nistri A: Modulation of rhythmic patterns and cumulative depolarization by group I metabotropic glutamate receptors in the neonatal rat spinal cord in vitro. Eur J Neurosci. 2004 Feb;19(3):533-41.

Disinhibited bursting induced by strychnine + bicuculline was accelerated by DHPG, slowed down by AIDA (which prevented the action of DHPG), unaffected by MPEP and counteracted by the selective group II agonist (2S,2'R,3'R)-2-(2',3'-dicarboxycyclopropyl) glycine.
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12200222 Bough KJ, Gudi K, Han FT, Rathod AH, Eagles DA: An anticonvulsant profile of the ketogenic diet in the rat. Epilepsy Res. 2002 Aug;50(3):313-25.


All animals began diet treatment at age P37 and each was subjected to one of five chemically-induced seizure tests: bicuculline (BIC; s.c.), picrotoxin (PIC; s.c.), kainate (KA, i.p. or s.c.) and gamma-butyrolactone (GBL, i.p.), strychnine (s.c.).
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10604951 Snell LD, Claffey DJ, Ruth JA, Valenzuela CF, Cardoso R, Wang Z, Levinson SR, Sather WA, Williamson AV, Ingersoll NC, Ovchinnikova L, Bhave SV, Hoffman PL, Tabakoff B: Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization. J Pharmacol Exp Ther. 2000 Jan;292(1):215-27.


These compounds were shown to act in a use-dependent manner as antagonists of VSNaCs and to act as selective competitive antagonists at the strychnine-insensitive glycine recognition site of NMDA receptors.
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9861707 Zhao FY, Roberts A: Assessing the roles of glutamatergic and cholinergic synaptic drive in the control of fictive swimming frequency in young Xenopus tadpoles. J Comp Physiol A. 1998 Dec;183(6):753-8.


The components of synaptic drive were revealed by the local microperfusion of strychnine together with different excitatory antagonists.
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19017536 Zhang HM, Chen SR, Pan HL: Effects of activation of group III metabotropic glutamate receptors on spinal synaptic transmission in a rat model of neuropathic pain. Neuroscience. 2009 Jan 23;158(2):875-84. Epub 2008 Oct 30.

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7834343 Ball EF, Shaw PJ, Ince PG, Johnson M: The distribution of excitatory amino acid receptors in the normal human midbrain and basal ganglia with implications for Parkinson's disease: a quantitative autoradiographic study using [3H] MK-801, [3H] glycine, [3H] CNQX and [3H] kainate. Brain Res. 1994 Sep 26;658(1-2):209-18.

Detailed knowledge of the anatomy and subtype specificity of glutamate receptors is important both in understanding the normal physiology of basal ganglia neurotransmission and the pathophysiological changes occurring in diseases affecting the basal ganglia such as Parkinson's disease (PD).
In the substantia nigra relatively high densities of [3H] MK-801 and strychnine-insensitive [3H] glycine binding sites representing NMDA receptors were present, whereas only moderate densities of [3H] CNQX and [3H] kainate binding sites were present, compared to other regions.
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15548213 Rosato-Siri MD, Zoccolan D, Furlan F, Ballerini L: Interneurone bursts are spontaneously associated with muscle contractions only during early phases of mouse spinal network development: a study in organotypic cultures. Eur J Neurosci. 2004 Nov;20(10):2697-710.

Conversely, bursting recorded in the presence of strychnine and bicuculline became increasingly regular with time in vitro.
We also demonstrated that spontaneous bursts of interneurone action potentials strongly correlate with muscular contractions only during the first week in vitro and that this is due to the activation of motoneurones via AMPA-type glutamate receptors.
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17365101 Maile RA, Morgan E, Bagust J, Walker RJ: Effects of amino acid antagonists on spontaneous dorsal root activity and evoked dorsal horn field potentials in an isolated preparation of rat spinal cord. Int J Neurosci. 2007 Jan;117(1):85-106.

The GABA antagonist, bicuculline, and the glycine antagonist, strychnine, while having no effect on the fast S1 and slow components of the field potential, reduced both the fast S2 component of the field potential and spontaneous dorsal root activity.
These results suggest that non-NMDA glutamate receptors are involved in low and high threshold transmission to dorsal horn neurones while NMDA and metabotropic glutamate receptors are primarily involved in high threshold transmission and both GABA and glycine have roles in the transmission or modulation of sensory information within the dorsal horn of the cord.
1(0,0,0,1) Details
10381800 Wang MY, Rampil IJ, Kendig JJ: Ethanol directly depresses AMPA and NMDA glutamate currents in spinal cord motor neurons independent of actions on GABAA or glycine receptors. J Pharmacol Exp Ther. 1999 Jul;290(1):362-7.

This study was designed to test the hypothesis that ethanol acts directly on motor neurons to inhibit excitatory synaptic transmission at glutamate receptors.
Block of inhibitory gamma-aminobutyric acidA and glycine receptors by bicuculline (50 microM) and strychnine (5 microM), respectively, did not significantly reduce the effects of ethanol on glutamate currents.
1(0,0,0,1) Details
9183739 Withers MD, St John PA: Embryonic rat spinal cord neurons change expression of glycine receptor subtypes during development in vitro. J Neurobiol. 1997 Jun 5;32(6):579-92.


However, the extent to which responses to glycine were blocked by the antagonist strychnine differed significantly between the first few days and 8 days in culture.
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7588967 Tegtmeyer-Metzdorf H, Roth B, Gunther M, Theisohn M, Heinemann U, Adams HA, Sticht G: Ketamine and strychnine treatment of an infant with nonketotic hyperglycinaemia. Eur J Pediatr. 1995 Aug;154(8):649-53.

Glycine is a major inhibitory neurotransmitter in the CNS, but has also modulating effects at one of the glutamate receptors, the N-methyl-D-aspartate-(NMDA) receptor.
1(0,0,0,1) Details
10974307 Chen J, Heinke B, Sandkuhler J: Activation of group I metabotropic glutamate receptors induces long-term depression at sensory synapses in superficial spinal dorsal horn. Neuropharmacology. 2000 Sep;39(12):2231-43.

In the presence of bicuculline and strychnine, bath application of (1S,3R)-1-aminocyclopentane-1, 3-dicarboxylic acid ((1S,3R)-ACPD) or the specific group I mGluR agonist (S)-3,5-dihydroxyphenylglycine ((S)-3,5-DHPG) but not the specific group II mGluR agonist (2S,2'R,3'R)-2-(2', 3'-dicarboxycyclopropyl) glycine (DCG-IV) for 20 min produced an acute and a long-term depression of synaptic strength.
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7953730 Baran H, Loscher W, Mevissen M: The glycine/NMDA receptor partial agonist D-cycloserine blocks kainate-induced seizures in rats. Brain Res. 1994 Aug 1;652(2):195-200.

The data demonstrate that pharmacological manipulation of the strychnine-insensitive glycine site is a powerful means of protecting against kainate-induced seizures.
Since kainate increases the release of excitatory amino acid neurotransmitters such as glutamate, this syndrome is thought to be due, at least in part, to excessive activation of glutamate receptors, particularly of the N-methyl-D-aspartate (NMDA) subtype.
1(0,0,0,1) Details
8120580 Floeter MK, Lev-Tov A: Excitation of lumbar motoneurons by the medial longitudinal fasciculus in the in vitro brain stem spinal cord preparation of the neonatal rat. J Neurophysiol. 1993 Dec;70(6):2241-50.

The short-latency MLF EPSP was reversibly blocked by 6-cyano-7-nitroquinoxaline (CNQX), an antagonist of non-N-methyl-D-aspartate glutamate receptors, with a small CNQX-resistant component.
Longer-latency components of the MLF EPSP were also blocked by CNQX, and some late components of the PSP were sensitive to strychnine.
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10845755 Ballanyi K, Onimaru H, Homma I: Respiratory network function in the isolated brainstem-spinal cord of newborn rats. Prog Neurobiol. 1999 Dec;59(6):583-634.

In particular non-NMDA type glutamate receptors constitute excitatory synaptic connectivity between respiratory neurons.
Respiratory rhythm is not blocked upon inhibition of IPSPs with bicuculline, strychnine and saclofen.
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15888962 Leewanich P, Tohda M, Takayama H, Sophasan S, Watanabe H, Matsumoto K: Corymine potentiates NMDA-induced currents in Xenopus oocytes expressing NR1a/NR2B glutamate receptors. J Pharmacol Sci. 2005 May;98(1):58-65. Epub 2005 May 12.

Previous studies demonstrated that corymine, an indole alkaloid isolated from the leaves of Hunter zeylanica, dose-dependently inhibited strychnine-sensitive glycine-induced currents.
1(0,0,0,1) Details
8234367 Sladeczek F, Momiyama A, Takahashi T: Presynaptic inhibitory action of a metabotropic glutamate receptor agonist on excitatory transmission in visual cortical neurons. Proc Biol Sci. 1993 Sep 22;253(1338):297-303.


A family of metabotropic glutamate receptors (mGluRs) has been elucidated by molecular cloning.
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15548203 Pierobon P, Sogliano C, Minei R, Tino A, Porcu P, Marino G, Tortiglione C, Concas A: Putative NMDA receptors in Hydra: a biochemical and functional study. Eur J Neurosci. 2004 Nov;20(10):2598-604.

These results, together with the decrease in response duration produced by d-serine, support the hypothesis that NMDA-like glutamate receptors may occur in Hydra tissues where they are involved in modulation of the response to GSH with opposite actions to those of GABA and glycine.
Simultaneous administration of ineffective doses of NMDA and strychnine, glycine or d-serine, an agonist at the glycine binding site of the NMDA receptor in vertebrate CNS, resulted in a strong reduction of response duration.
1(0,0,0,1) Details
11738262 Tapia JC, Mentis GZ, Navarrete R, Nualart F, Figueroa E, Sanchez A, Aguayo LG: Early expression of glycine and GABA (A) receptors in developing spinal cord neurons. Neuroscience. 2001;108(3):493-506.

This suggests that glycine and GABA (A) receptors provide a fundamental regulation of both neuronal excitability and intracellular Ca (2+) at this early time of development.The neurotrophic effects of agonists and antagonists for glycine, GABA (A) and glutamate receptors were examined in neurons cultured for 2 or 5 DIV.
The use of various receptor antagonists (strychnine, bicuculline, DL-2-amino-5-phosphonovalerate [APV], 6-cyano-7-nitroquinoxaline-2,3-dione [CNQX]) revealed that this activity was predominantly glycinergic, and to a smaller extent, GABAergic.
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10934271 Snead OC 3rd, Banerjee PK, Burnham M, Hampson D: Modulation of absence seizures by the GABA (A) receptor: a critical rolefor metabotropic glutamate receptor 4 (mGluR4). J Neurosci. 2000 Aug 15;20(16):6218-24.

The release of both glutamate and GABA is regulated by group III metabotropic glutamate receptors (mGluRs).
No differences were observed between mGluR4 (-/-) and mGluR4 (+/+) mice in threshold to clonic or tonic seizures induced by higher doses of GABA (A) R antagonists, strychnine, or electroshock, indicating that seizure resistance in the mGluR4 (-/-) mice was restricted solely to absence seizures.
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9209115 Jenei Z, Varga V, Janaky R, Saransaari P, Oja SS: Role of histidyl residues in the binding of ligands to the porcine N-methyl-D-aspartate receptor. Neurosci Lett. 1997 Jun 6;228(2):127-30.

Possible involvement of histidyl residues in the binding of ligands to ionotropic glutamate receptors and to modulatory sites on the N-methyl-D-aspartate (NMDA) receptor was assessed in porcine cortical synaptic plasma membranes after covalent modification with diethyl pyrocarbonate (DEPC).
DEPC reduced the strychnine-insensitive binding of [3H] glycine and the glycine- and glutamate-activated binding of [3H] dizocilpine.
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7887983 Forray MI, Andres ME, Bustos G, Gysling K: Regulation of endogenous noradrenaline release from the bed nucleus of stria terminalis. Biochem Pharmacol. 1995 Mar 1;49(5):687-92.

N-Methyl-D-aspartate (NMDA), a specific agonist of NMDA-type glutamate receptors, evoked the release of NA from vBNST minislices.
However, glycine exhibited a significant effect by itself, suggesting the existence of strychnine-sensitive glycine receptors in vBNST.
1(0,0,0,1) Details
9714868 Zhao FY, Wolf E, Roberts A: Longitudinal distribution of components of excitatory synaptic input to motoneurones during swimming in young Xenopus tadpoles: experiments with antagonists. J Physiol. 1998 Sep 15;511 ( Pt 3):887-901.


Different antagonists (10 microM dihydro-beta-erythroidine (DHbetaE) for nicotinic ACh receptors (nAChRs), 2 mM kynurenate (Kyn) for glutamate receptors (GluRs), and 100 microM Cd2+ for all chemical synapses) were microperfused very locally to unmask the relative contributions of these components to the total excitatory drive, and their distribution along the spinal cord during swimming. 3.
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7796124 Nowak G, Ordway GA, Paul IA: Alterations in the N-methyl-D-aspartate (NMDA) receptor complex in the frontal cortex of suicide victims. Brain Res. 1995 Mar 27;675(1-2):157-64.

This adaptation consists of a reduction in the potency of glycine to displace [3H] 5,7-dichlorokynurenic acid from strychnine-insensitive glycine receptors and a reduction in high affinity, glycine-displaceable [3H] CGP-39653 binding to glutamate receptors.
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8401927 Ishida M, Saitoh T, Shimamoto K, Ohfune Y, Shinozaki H: A novel metabotropic glutamate receptor agonist: marked depression of monosynaptic excitation in the newborn rat isolated spinal cord. Br J Pharmacol. 1993 Aug;109(4):1169-77.

Depression of monosynaptic excitation caused by DCG-IV was not affected by any known pharmacological agents, including 2-amino-3-phosphonopropanoic acid (AP3), diazepam, 2-hydroxysaclofen, picrotoxin and strychnine. 6.
DCG-IV has the potential of providing further useful information on the physiological function of metabotropic glutamate receptors.
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19321640 Bonnot A, Chub N, Pujala A, O'Donovan MJ: Excitatory actions of ventral root stimulation during network activity generated by the disinhibited neonatal mouse spinal cord. J Neurophysiol. 2009 Jun;101(6):2995-3011. Epub 2009 Mar 25.


Collectively, our data indicate that VR stimulation can entrain disinhibited spinal network activity and trigger locomotor-like activity through a mechanism dependent on activation of both ionotropic and metabotropic glutamate receptors.
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9851655 Rodriguez-Ithurralde D, Maruri A, Rodriguez X: Motor neurone acetylcholinesterase release precedes neurotoxicity caused by systemic administration of excitatory amino acids and strychnine. J Neurol Sci. 1998 Oct;160 Suppl 1:S80-6.

We investigated histochemical and histopathological changes in cell populations of the mouse spinal ventral horn upon in vivo stimulation of glutamate receptors with L-aspartate (ASP, 10-50 mg/kg, intraperitoneal: i.p.), or blockade of glycine receptors with strychnine (STRY, 2 mg/kg, i.p.).
81(1,1,1,1) Details
16806506 Martineau M, Baux G, Mothet JP: D-serine signalling in the brain: friend and foe. Trends Neurosci. 2006 Aug;29(8):481-91. Epub 2006 Jun 30.

One such glia-derived modulator is D-serine, an amino acid that serves as an endogenous ligand for the strychnine-insensitive glycine-binding site of NMDA glutamate receptors.
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16613054 Polina IuA, Amakhin DV, Kozhakov VM, Kurchavyi GG, Veselkin NP: [Three types of miniature inhibitory potentiaes in the frog spinal cord motoneurons: the possibility of GABA and glycine co-release]. Ross Fiziol Zh Im I M Sechenova. 2006 Jan;92(1):18-26.

Miniature inhibitory postsynaptic potentials (mlPSPs) were recorded from motoneurons of the frog isolated spinal cord after blocking action potentials and ionotropic glutamate receptors (TTX 1 mcm: CNQX 25 mcm, D-AP5 50 mcm).
The GlyR antagonist strychnine (1 mcm) reduced the frequency of fast mlPSPs and increased this parameter of slow mlPSPs.
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7830058 Widdowson PS, Trainor A, Lock EA: NMDA receptors in rat cerebellum and forebrain: subtle differences in pharmacology and modulation. J Neurochem. 1995 Feb;64(2):651-61.

Binding of [3H] glutamate, [3H] glycine, and the glutamate antagonist [3H] CGS-19755 to NMDA-type glutamate receptors was examined in homogenates of rat forebrain and cerebellum.
In the cerebellum, however, [3H] glycine bound to a second site with a 10-fold lower affinity and with a pharmacology that resembled that of the glycine/strychnine chloride channel. [3H]-Glutamate binding was not affected by glycine agonists or antagonists, nor was [3H] glycine binding affected by glutamate agonists in either forebrain or cerebellum.
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9593880 Miyazaki T, Kobayashi H, Tosaka T: Presynaptic inhibition by noradrenaline of the EPSC evoked in neonatal rat sympathetic preganglionic neurons. Brain Res. 1998 Apr 20;790(1-2):170-7.

Monosynaptic excitatory postsynaptic currents (EPSCs) were evoked by electrical stimulation of the nucleus intercalatus in the presence of strychnine (5 microM) and bicuculline (10 microM).
These EPSCs were abolished by the antagonist of AMPA-type glutamate receptors, 6-cyano-7-nitro-quinoxaline-2,3-dione (CNQX; 10 microM).
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16836978 Jung SJ, Kim SJ, Park YK, Oh SB, Cho K, Kim J: Group I mGluR regulates the polarity of spike-timing dependent plasticity in substantia gelatinosa neurons. Biochem Biophys Res Commun. 2006 Aug 25;347(2):509-16. Epub 2006 Jun 30.

However, how group I metabotropic glutamate receptors (mGluRs) may operate spinal plasticity remains essentially unexplored.
In the presence of bicuculline and strychnine, long-term potentiation (LTP) was blocked by AP-5 and Ca2+ chelator BAPTA-AM.
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19194159 Nguyen HT, Li KY, daGraca RL, Delphin E, Xiong M, Ye JH: Behavior and cellular evidence for propofol-induced hypnosis involving brain glycine receptors. Anesthesiology. 2009 Feb;110(2):326-32.

Propofol-induced LORR was examined in the presence and absence of strychnine (a glycine receptor antagonist), GABAzine (a gamma-aminobutyric acid A receptor antagonist), as well as ketamine (an antagonist of N-methyl-D-aspartic acid subtype of glutamate receptors).
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8899663 Rodriguez-Ithurralde D, Olivera S, La Paz A, Vincent O, Rondeau A: Glycine effects on glutamate-receptor elicited acetylcholinesterase release from slices and synaptosomes of the spinal ventral horn. J Neurol Sci. 1996 Aug;139 Suppl:76-82.

After the 28th postnatal day, nearly all the AChE secreted was released either after the activation of non-NMDA glutamate receptors or by strychnine-sensitive GLY-evoked AChE release mechanisms.
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17294103 Polina YA, Amakhin DV, Kozhanov VM, Kurchavyi GG, Veselkin NP: Three types of inhibitory miniature potentials in frog spinal cord motoneurons: possible GABA and glycine cotransmission. Neurosci Behav Physiol. 2007 Mar;37(3):271-6.

Miniature inhibitory postsynaptic potentials (mIPSP) of motoneurons in isolated frog spinal cord were recorded in conditions of blockade of the conduction of nerve spikes and ionotropic glutamate receptors (TTX, 1 microM, CNQX, 25 microM, D-AP5, 50 microM).
Strychnine (1 microM), a blocker of glycine receptors, led to a reduction in the number of fast receptors and an increase in the number of slow potentials.
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8003681 Chiba C, Saito T: APB (2-amino-4-phosphonobutyric acid) activates a chloride conductance in ganglion cells isolated from newt retina. Neuroreport. 1994 Jan 12;5(4):489-92.

In vertebrate retinae, APB (2-amino-4-phosphonobutyrate) selectively activates glutamate receptors of ON-bipolar cells.
Strychnine, a glycine receptor blocker, inhibited the APB response.
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8883856 Matsuoka N, Aigner TG: The glycine/NMDA receptor antagonist HA-966 impairs visual recognition memory in rhesus monkeys. Brain Res. 1996 Aug 26;731(1-2):72-8.

Recent studies have shown that strychnine-insensitive glycine binding sites positively modulate the N-methyl-D-asparate (NMDA) subclass of glutamate receptors, which are important in neural pathways involved in cognitive function.
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15031290 Ju P, Aubrey KR, Vandenberg RJ: Zn2+ inhibits glycine transport by glycine transporter subtype 1b. J Biol Chem. 2004 May 28;279(22):22983-91. Epub 2004 Mar 18.

In the central nervous system, glycine is a co-agonist with glutamate at the N-methyl-D-aspartate subtype of glutamate receptors and also an agonist at inhibitory, strychnine-sensitive glycine receptors.
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9707286 Lingenhohl K, Pozza MF: Reevaluation of ACEA 1021 as an antagonist at the strychnine-insensitive glycine site of the N-methyl-D-aspartate receptor. Neuropharmacology. 1998 Jun;37(6):729-37.

Electrophysiological experiments were performed in vitro and in vivo to characterize the inhibitory effects of 6,7-dichloro-5-nitro-1,4-dihydro-2,3-quinoxalinedione (ACEA 1021; licostinel) on rat brain glutamate receptors.
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8836233 Hartveit E: Membrane currents evoked by ionotropic glutamate receptor agonists in rod bipolar cells in the rat retinal slice preparation. J Neurophysiol. 1996 Jul;76(1):401-22.

Coapplication of the non-NMDA receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione blocked the response to kainate and AMPA, indicating that the response was mediated by conventional ionotropic glutamate receptors. 6.
The conductance increase evoked by non-NMDA receptor agonists could not be blocked by a combination of 100 microM picrotoxin and 10 microM strychnine.
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15758056 Wong KY, Dowling JE: Retinal bipolar cell input mechanisms in giant danio. J Neurophysiol. 2005 Jul;94(1):265-72. Epub 2005 Mar 9.

Specific agonists were puffed in the presence of cobalt, picrotoxin, and strychnine to identify glutamate receptors on these cells.
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7477740 Fossom LH, Von Lubitz DK, Lin RC, Skolnick P: Neuroprotective actions of 1-aminocyclopropanecarboxylic acid (ACPC): a partial agonist at strychnine-insensitive glycine sites. Neurol Res. 1995 Aug;17(4):265-9.

1-Aminocyclopropanecarboxylic acid is a high affinity ligand with partial agonist properties at strychnine-insensitive glycine sites associated with the N-methyl-D-aspartate subtype of glutamate receptors.
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18497354 Petit-Jacques J, Bloomfield SA: Synaptic regulation of the light-dependent oscillatory currents in starburst amacrine cells of the mouse retina. J Neurophysiol. 2008 Aug;100(2):993-1006. Epub 2008 May 21.

Strychnine, the blocker of glycine receptors did not affect the initial peak but strongly decreased the oscillations frequency.
The synaptic pathway responsible for the light responses was blocked by AP4, an agonist of metabotropic glutamate receptors that hyperpolarize on-center bipolar cells on activation.
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9704598 Jenei Z, Janaky R, Varga V, Saransaari P, Oja SS: Interference of S-alkyl derivatives of glutathione with brain ionotropic glutamate receptors. Neurochem Res. 1998 Aug;23(8):1085-91.

The strychnine-insensitive binding of the NMDA coagonist [3H] glycine was attenuated only by oxidized glutathione and glutathione sulfonate.
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8558453 Standaert DG, Testa CM, Rudolf GD, Hollingsworth ZR: Inhibition of N-methyl-D-aspartate glutamate receptor subunit expression by antisense oligonucleotides reveals their role in striatal motor regulation. J Pharmacol Exp Ther. 1996 Jan;276(1):342-52.

After NMDAR1 antisense ODN injection, striatal binding of 3H-glutamate to NMDA sites was not altered, although strychnine-insensitive 3H-glycine binding sites exhibited a small but significant reduction.
N-methyl-D-aspartate (NMDA) glutamate receptors have an established role in the regulation of motor behavior by the basal ganglia.
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9895138 Toru M: Biological research on schizophrenia. . Psychiatry Clin Neurosci. 1998 Dec;52 Suppl:S170-2.

Glutamate receptors, such as the kainate receptor labeled by 3H-kainate, the N-methyl-D-aspartate (NMDA) receptor by 3H MK801, and the strychnine-insensitive glycine sites in the NMDA receptor by 3H-glycine, increased significantly in various cortical areas of schizophrenic brains.
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11692754 Mothet JP: Physiological relevance of endogenous free D-serine in the mammalian brain: are scientists on a royal road for the treatment of glutamatergic-related brain disorders?. Pathol Biol. 2001 Oct;49(8):655-9.

In this review, we focus on recent findings regarding the physiological relevance of D-serine, a new neurotransmitter formed in glial cells, that serves as the endogenous ligand for the accessory strychnine-insensitive glycine site of the N-methyl-D-aspartate (NMDA) subtype of glutamate receptors.
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9673799 Wallis DI, Elliott P, Foster GA, Stringer BM: Synaptic activity, induced rhythmic discharge patterns, and receptor subtypes in enriched primary cultures of embryonic rat motoneurones. Can J Physiol Pharmacol. 1998 Mar;76(3):347-59.

Synaptic activity interrupted by periods of quiescence increased in frequency with culture age and was suppressed by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and strychnine.
Inward currents carried by Cl- were elicited by glycine (10-300 microM) and GABA (1-300 microM), while adenosine (1-10 microM) and cyclopentyladenosine (10 nM-1 microM) evoked a K (+)-dependent hyperpolarization. 5-HT, GABAB, purine A, and metabotropic glutamate receptors modulated synaptic excitation of presumed motoneurones.
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7666201 Lukasiewicz PD, Lawrence JE, Valentino TL: Desensitizing glutamate receptors shape excitatory synaptic inputs to tiger salamander retinal ganglion cells. J Neurosci. 1995 Sep;15(9):6189-99.

Strychnine and picrotoxin blocked inhibitory inputs.
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