Protein Information

Name GLYT1
Synonyms GLYT1; GLYT1; GLYT1A; GLYT1B; GLYT1C; GlyT 1; Glycine transporter 1B; Glycine transporter type 1 A…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
7700536 Luque JM, Nelson N, Richards JG: Cellular expression of glycine transporter 2 messenger RNA exclusively in rat hindbrain and spinal cord. Neuroscience. 1995 Jan;64(2):525-35.

The distribution of glycine transporter 2 messenger RNA-containing cell bodies was very different to that of other glycine transporter messenger RNAs (glycine transporter 1a and glycine transporter 1b), but similar to that of known glycine-immunoreactive neurons and correlated very well with that of strychnine-sensitive glycine receptors in most CNS regions except cerebellum.
31(0,1,1,1) Details
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.
The GLYT1 subtypes of glycine transporters (GLYTs) are responsible for regulation of glycine at excitatory synapses, whereas a combination of GLYT1 and GLYT2 subtypes of glycine transporters are used at inhibitory glycinergic synapses.
5(0,0,0,5) Details
15588724 Raiteri L, Stigliani S, Siri A, Passalacqua M, Melloni E, Raiteri M, Bonanno G: Glycine taken up through GLYT1 and GLYT2 heterotransporters into glutamatergic axon terminals of mouse spinal cord elicits release of glutamate by homotransporter reversal and through anion channels. Biochem Pharmacol. 2005 Jan 1;69(1):159-68.

Glycine effect was insensitive to strychnine or 5,7-dichlorokynurenic acid, but was prevented by the glycine transporter blocker glycyldodecylamide.
4(0,0,0,4) Details
15207356 Whitehead KJ, Pearce SM, Walker G, Sundaram H, Hill D, Bowery NG: Positive N-methyl-D-aspartate receptor modulation by selective glycine transporter-1 inhibition in the rat dorsal spinal cord in vivo. Neuroscience. 2004;126(2):381-90.

In this study we have employed the selective glycine transporter-1 (GlyT-1) and GlyT-2 transporter inhibitors R-(-)-N-methyl-N-[3-[(4-trifluoromethyl) phenoxy]-3-phenyl-propyl] glycine (1:1) lithium salt (Org 24598) and 4-benzyloxy-3,5-dimethoxy-N-[1-(dimethylaminocyclopently) methyl] benzamide (Org 25543), respectively, and microdialysis perfusion to determine the effect of GlyT transporter inhibition on extracellular amino acid concentrations in the lumbar dorsal spinal cord of the halothane-anaesthetised rat.
Co-administration by reverse dialysis of the selective NMDA-R channel blocker MK-801 (0.5 mM) or the selective antagonist of the strychnine-insensitive glycine site, 7-chlorokynurenic acid (1 mM), with Org 24598 (10 microM) did not affect the uptake inhibition-induced increase in glycine efflux, but did significantly attenuate the increase in extracellular citrulline.
4(0,0,0,4) Details
11259500 Raiteri L, Raiteri M, Bonanno G: Glycine is taken up through GLYT1 and GLYT2 transporters into mouse spinal cord axon terminals and causes vesicular and carrier-mediated release of its proposed co-transmitter GABA. J Neurochem. 2001 Mar;76(6):1823-32.

Glycine concentration dependently elicited [(3) H] GABA release which was insensitive to strychnine or 5,7-dichlorokynurenic acid, but was Na (+) dependent and sensitive to the glycine uptake blocker glycyldodecylamide.
3(0,0,0,3) Details
17462677 Igartua I, Solis JM, Bustamante J: Glycine-induced long-term synaptic potentiation is mediated by the glycine transporter GLYT1. Neuropharmacology. 2007 Jun;52(8):1586-95. Epub 2007 Mar 14.

This LTP-GLY is independent of both strychnine-sensitive glycine receptors and nifedipine-sensitive calcium channels.
3(0,0,0,3) Details
9861038 Bergeron R, Meyer TM, Coyle JT, Greene RW: Modulation of N-methyl-D-aspartate receptor function by glycine transport. . Proc Natl Acad Sci U S A. 1998 Dec 22;95(26):15730-4.

Data obtained from whole-cell patch-clamp recordings of hippocampal pyramidal neurons, in vitro, demonstrated that exogenous glycine and glycine transporter type 1 (GLYT1) antagonist selectively enhanced the amplitude of the NMDA component of a glutamatergic excitatory postsynaptic current.
The effect was blocked by 2-amino-5-phosphonovaleric acid and 7-chloro-kynurenic acid but not by strychnine.
3(0,0,0,3) Details
17383967 Vandenberg RJ, Shaddick K, Ju P: Molecular basis for substrate discrimination by glycine transporters. J Biol Chem. 2007 May 11;282(19):14447-53. Epub 2007 Mar 23.

Glycine is an inhibitory neurotransmitter in the spinal cord and brain stem, where it acts on strychnine-sensitive glycine receptors, and is also an excitatory neurotransmitter throughout the brain and spinal cord, where it acts on the N-methyl-d-aspartate family of receptors.
There are two Na (+)/Cl (-)-dependent glycine transporters, GLYT1 and GLYT2, which control extracellular glycine concentrations and these transporters show differences in substrate selectivity and blocker sensitivity.
2(0,0,0,2) Details
11396606 Lopez-Corcuera B, Geerlings A, Aragon C: Glycine neurotransmitter transporters: an update. Mol Membr Biol. 2001 Jan-Mar;18(1):13-20.

This action of glycine is mediated by the strychnine-sensitive glycine receptor, whose activation produces inhibitory post-synaptic potentials.
It is believed that the termination of the different synaptic actions of glycine is produced by rapid re-uptake through two sodium-and-chloride-coupled transporters, GLYT1 and GLYT2, located in the plasma membrane of glial cells or pre-synaptic terminals, respectively.
1(0,0,0,1) Details
20173309 Nishikawa Y, Sasaki A, Kuraishi Y: Blockade of glycine transporter (GlyT) 2, but not GlyT1, ameliorates dynamic and static mechanical allodynia in mice with herpetic or postherpetic pain. J Pharmacol Sci. 2010 Mar 19;112(3):352-60. Epub 2010 Feb 20.

Glycine is an inhibitory neurotransmitter in the spinal dorsal horn and its extracellular concentration is regulated by glial glycine transporter (GlyT) 1 and neuronal GlyT2.
Intrathecal ALX1393 suppressed dynamic allodynia induced by intrathecal strychnine and N-methyl-D-aspartate (NMDA).
1(0,0,0,1) Details
10886333 Belachew S, Malgrange B, Rigo JM, Rogister B, Leprince P, Hans G, Nguyen L, Moonen G: Glycine triggers an intracellular calcium influx in oligodendrocyte progenitor cells which is mediated by the activation of both the ionotropic glycine receptor and Na+-dependent transporters. Eur J Neurosci. 2000 Jun;12(6):1924-30.


Glycine-triggered Ca2+ influx in OP cells actually results from an initial depolarization that is the consequence of the activation of both the ionotropic glycine receptor (GlyR) and Na+-dependent transporters, most probably the glycine transporters 1 (GLYT1) and/or 2 (GLYT2) which are colocalized in these cells.
1(0,0,0,1) Details
7823028 Jursky F, Tamura S, Tamura A, Mandiyan S, Nelson H, Nelson N: Structure, function and brain localization of neurotransmitter transporters. J Exp Biol. 1994 Nov;196:283-95.

A correlation as observed between the pattern we obtained and that observed previously from strychnine binding studies.
A genomic clone of two of the glycine transporters (GLYT1a and GLYT1b) revealed that they derive from differential splicing of a single gene.
1(0,0,0,1) Details
17970719 Issberner JP, Sillar KT: The contribution of the NMDA receptor glycine site to rhythm generation during fictive swimming in Xenopus laevis tadpoles. Eur J Neurosci. 2007 Nov;26(9):2556-64. Epub 2007 Oct 23.

Glycine (100 microm), another endogenous agonist at this site, triggered similar effects to D-serine, but only when applied in the presence of strychnine.
Manipulations of endogenous glycine levels using sarcosine or ALX 5407 (inhibitors of the glycine re-uptake protein, GlyT1b), produced similar effects to glycine site agonists, including increased episode durations, and modulations in cycle period and burst amplitude.
1(0,0,0,1) Details
18602930 Perry KW, Falcone JF, Fell MJ, Ryder JW, Yu H, Love PL, Katner J, Gordon KD, Wade MR, Man T, Nomikos GG, Phebus LA, Cauvin AJ, Johnson KW, Jones CK, Hoffmann BJ, Sandusky GE, Walter MW, Porter WJ, Yang L, Merchant KM, Shannon HE, Svensson KA: Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology. 2008 Oct;55(5):743-54. Epub 2008 Jun 17.

In support of these findings, immuno-staining with pan-GlyT1 and GlyT1a antibodies showed a higher abundance of immunoreactivity in the brain stem/cerebellum as compared to the frontal cortical/hippocampal brain areas in four different species studied, including the mouse, rat, monkey and human.
In addition, the inhibitory effects of ALX5407 on cerebellar levels of cGMP in the mouse could be reversed by the glycine A receptor antagonist strychnine but not the glycine B receptor antagonist L-701324.
1(0,0,0,1) Details