Protein Information

Name G protein
Synonyms G gamma I; Guanine nucleotide binding protein 2; G protein; GNG 2; GNG2; GNGT 2; GNGT2; Guanine nucleotide binding protein gamma 2…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
8714523 Puebla L, Arilla E: Glycine increases the number of somatostatin receptors and somatostatin-mediated inhibition of the adenylate cyclase system in the rat hippocampus. J Neurosci Res. 1996 Feb 1;43(3):346-54.

Since SS receptors are coupled via guanine nucleotide-binding G proteins to the adenylyl cyclase (AC) system, we also examined the inhibitory effects of SS and the guanine nucleotide Gpp (NH) p on AC activity in hippocampal membranes of control, glycine- and strychnine plus glycine-treated rats since the increase in SS receptors was observed only in this brain area.
31(0,1,1,1) Details
8667245 Sorenson EM, Gallagher JP: The membrane hyperpolarization of rat dorsolateral septal nucleus neurons is mediated by a novel nicotinic receptor. J Pharmacol Exp Ther. 1996 Jun;277(3):1733-43.

The pharmacology, calcium dependence and G protein mediation of the membrane hyperpolarization of rat dorsolateral septal nucleus (DLSN) neurons in response to nicotinic agonists was examined to classify the nicotinic receptor mediating the response.
Intracellular recording from DSLN neurons in a brain slice preparation was used to determine whether chlorisondamine, trimethaphan, cytisine or strychnine inhibited the membrane hyperpolarization in response to application of the nicotinic agonist 1,1-dimethyl-4-phenylpiperazinium (DMPP).
2(0,0,0,2) Details
10449792 Ming D, Ninomiya Y, Margolskee RF: Blocking taste receptor activation of gustducin inhibits gustatory responses to bitter compounds. Proc Natl Acad Sci U S A. 1999 Aug 17;96(17):9903-8.

Gustducin, a transducin-like guanine nucleotide-binding regulatory protein (G protein), and transducin are expressed in taste receptor cells where they are thought to mediate taste transduction.
We have monitored this activation with an in vitro assay to identify compounds that inhibited taste receptor activation of transducin by bitter tastants: AMP and chemically related compounds inhibited in vitro responses to several bitter compounds (e.g., denatonium, quinine, strychnine, and atropine).
2(0,0,0,2) 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.
After pre-incubation of slices with pertussis toxin, a G-protein inhibitor, (1S,3R)-ACPD still induced acute and long-term depressions.
2(0,0,0,2) Details
9374187 Tapia JC, Espinoza F, Aguayo LG: Differential intracellular regulation of cortical GABA (A) and spinal glycine receptors in cultured neurons. Brain Res. 1997 Sep 26;769(2):203-10.

Activation of G proteins with internal FAl4- induced an inhibition of the GABA (A) current, but potentiated the amplitude of the strychnine-sensitive Cl- current.
32(0,1,1,2) Details
16107637 Lozovaya N, Yatsenko N, Beketov A, Tsintsadze T, Burnashev N: Glycine receptors in CNS neurons as a target for nonretrograde action of cannabinoids. J Neurosci. 2005 Aug 17;25(33):7499-506.

At many central synapses, endocannabinoids released by postsynaptic cells act retrogradely on presynaptic G-protein-coupled cannabinoid receptors to inhibit neurotransmitter release.
We also demonstrate that, in the presence of a GABA (A) receptor antagonist, GlyRs may contribute to the generation of seizure-like activity induced by short bursts (seven stimuli) of high-frequency stimulation of inputs to hippocampal CA1 region, because this activity was diminished by selective GlyR antagonists (strychnine and ginkgolides B and J).
2(0,0,0,2) Details
17253962 Sainz E, Cavenagh MM, Gutierrez J, Battey JF, Northup JK, Sullivan SL: Functional characterization of human bitter taste receptors. . Biochem J. 2007 May 1;403(3):537-43.

In the present study we address the signalling properties of human and mouse T2Rs using an in vitro reconstitution system in which both the ligands and G-proteins being assayed can be manipulated independently and quantitatively assessed.
We also demonstrate that hT2R14 is a receptor for aristolochic acid and report the first characterization of the ligand specificities of hT2R7, which is a broadly tuned receptor responding to strychnine, quinacrine, chloroquine and papaverine.
2(0,0,0,2) Details
18440992 Hou M, Duan L, Slaughter MM: Synaptic inhibition by glycine acting at a metabotropic receptor in tiger salamander retina. J Physiol. 2008 Jun 15;586(Pt 12):2913-26. Epub 2008 Apr 25.

In retina, we found a strychnine-insensitive glycine response in bipolar and ganglion cells.
It was G-protein mediated and protein kinase A dependent.
2(0,0,0,2) Details
9671782 Ming D, Ruiz-Avila L, Margolskee RF: Characterization and solubilization of bitter-responsive receptors that couple to gustducin. Proc Natl Acad Sci U S A. 1998 Jul 21;95(15):8933-8.

Gustducin, a taste-specific G-protein closely related to the transducins, is a key component in transducing the responses to compounds that humans equate with bitter and sweet.
In this paper, we show that gustducin is expressed in bovine taste tissue and that both gustducin and transducin, in the presence of bovine taste membranes, can be activated specifically by several bitter compounds, including denatonium, quinine, and strychnine.
2(0,0,0,2) Details
11139828 Tranquillini ME, Reggiani A: Glycine-site antagonists and stroke. . Expert Opin Investig Drugs. 1999 Nov;8(11):1837-1848.

Its action is mediated by two main groups of receptors: the ionotropic receptors (which include NMDA, AMPA and kainic acid subtypes) and the metabotropic receptors (mGluR (1-8)) mediating G-protein coupled responses.
This review focuses on the strychnine insensitive glycine binding site located on the NMDA receptor channel, and on the possible use of selective antagonists for the treatment of stroke.
1(0,0,0,1) Details
11740501 Ahmadi S, Lippross S, Neuhuber WL, Zeilhofer HU: PGE (2) selectively blocks inhibitory glycinergic neurotransmission onto rat superficial dorsal horn neurons. Nat Neurosci. 2002 Jan;5(1):34-40.

We identified the inhibitory (strychnine-sensitive) glycine receptor as a specific target of PGE (2).
Inhibition of glycine receptors occurred via a postsynaptic mechanism involving the activation of EP2 receptors, cholera-toxin-sensitive G-proteins and cAMP-dependent protein kinase.
1(0,0,0,1) Details
7878084 Spielman AI, Huque T, Nagai H, Whitney G, Brand JG: Generation of inositol phosphates in bitter taste transduction. Physiol Behav. 1994 Dec;56(6):1149-55.


Addition of both the bitter stimulus, sucrose octaacetate and the G-protein stimulant, GTP gamma S, led to an enhanced production of inositol phosphates compared with either alone.
1(0,0,0,1) Details
10051215 Nabekura J, Xu TL, Rhee JS, Li JS, Akaike N: Alpha2-adrenoceptor-mediated enhancement of glycine response in rat sacral dorsal commissural neurons. Neuroscience. 1999 Mar;89(1):29-41.

In addition, noradrenaline potentiated the strychnine-sensitive postsynaptic currents evoked in a slice preparation of sacral dorsal commissural nucleus.
These results suggest that the activation of alpha2-adrenoceptor by noradrenaline coupled with pertussis toxin-sensitive G-proteins reduces intracellular cyclic AMP formation through the inhibition of adenyl cyclase.
1(0,0,0,1) Details
8596710 Green KA, Harris SJ, Cottrell GA: Dopamine directly activates a ligand-gated channel in snail neurones. Pflugers Arch. 1996 Feb;431(4):639-44.

Here evidence is presented that the fast excitatory response to dopamine is mediated by the direct activation of a ligand-gated channel: unitary currents were observed in outside-out patches of neurones exposed to dopamine, and the response persisted in the presence of intracellular guanosine 5'-o-(2-thiobiphosphate), GDP [beta-S], a condition known to block G-protein-coupled responses to dopamine and other agents.
The response to dopamine was blocked by D-tubocurarine and strychnine (both probably by channel blockade), by apomorphine, chlorpromazine and relatively high doses of (+/-)-sulpiride and spiperone.
1(0,0,0,1) Details
11312281 Hatton GI, Yang QZ: Ionotropic histamine receptors and H2 receptors modulate supraoptic oxytocin neuronal excitability and dye coupling. J Neurosci. 2001 May 1;21(9):2974-82.

IPSPs were blocked by the Cl (-) channel blocker picrotoxin, but not by bicuculline or strychnine, and by histamine H (2), but not by H (1) or H (3) receptor antagonists, suggesting the presence of an ionotropic histamine receptor and the possible nonspecificity of currently used H (2) antagonists.
G-protein mediation of the IPSPs was ruled out using guanosine 5'-O-(2-thiodiphosphate) (GDP-betaS), pertussis toxin, and Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPs), none of which blocked evoked IPSPs.
1(0,0,0,1) Details
8728878 Wikinski SI, Acosta GB: [Role of excitatory amino acids in neuropathology] . Medicina (B Aires). 1995;55(4):355-65.

Along with the site for N-methyl-D-aspartate, which binds glutamate and/or aspartate, there have been identified a site for the binding of glycine (which is different from the strychnine sensitive one), a site for poliamines such as spermine and spermidine, and a site for the binding of Zn2+ (Table 1).
Both are coupled to a G protein and agonists exert their action increasing phospholipase C activity which in turn induces an increment of IP3 and diacyl-glicerol, and a consecutive releasing of Ca2+ from intracellular stores.
1(0,0,0,1) Details
11245589 Yan W, Sunavala G, Rosenzweig S, Dasso M, Brand JG, Spielman AI: Bitter taste transduced by PLC-beta (2)-dependent rise in IP (3) and alpha-gustducin-dependent fall in cyclic nucleotides. Am J Physiol Cell Physiol. 2001 Apr;280(4):C742-51.

Using quench-flow techniques, we show here that the bitter stimuli, denatonium and strychnine, induce rapid (50-100 ms) and transient reductions in cAMP and cGMP and increases in IP (3) in murine taste tissue.
These data suggest a transduction mechanism for bitter taste involving the rapid and transient metabolism of dual second messenger systems, both mediated through a taste cell G protein, likely composed of Galpha (gust)/beta/gamma (13), with both systems being simultaneously activated in the same bitter-sensitive taste receptor cell.
1(0,0,0,1) Details
14551290 Cheng JK, Chou RC, Hwang LL, Chiou LC: Antiallodynic effects of intrathecal orexins in a rat model of postoperative pain. J Pharmacol Exp Ther. 2003 Dec;307(3):1065-71. Epub 2003 Oct 9.

Orexin A and B (hypocretin 1 and 2) are the endogenous ligands of orexin receptors, a G-protein-coupled orphan receptor family containing orexin 1 (OX1) and orexin 2 (OX2) types.
The effects of orexin A and B were abolished by their respective antibodies, but not by naloxone, and were attenuated by suramin and strychnine, the P2X purinergic and glycine receptor antagonists, respectively.
1(0,0,0,1) Details
10561820 Chebib M, Johnston GA: The 'ABC' of GABA receptors: a brief review. Clin Exp Pharmacol Physiol. 1999 Nov;26(11):937-40.

GABAA and GABAC receptors are members of a super-family of transmitter-gated ion channels that include nicotinic acetylcholine, strychnine-sensitive glycine and 5HT3 receptors.
GABAB receptors are seven transmembrane receptors that are coupled to G-proteins and activate second messenger systems and Ca2+ and K+ ion channels.
1(0,0,0,1) Details
7878081 Kurihara K, Katsuragi Y, Matsuoka I, Kashiwayanagi M, Kumazawa T, Shoji T: Receptor mechanisms of bitter substances. Physiol Behav. 1994 Dec;56(6):1125-32.


The presence of Ca ion in the medium prolongs the responses. (c) Bitter substances elicit electrical responses in nongustatory cells such as neuroblastoma cells and olfactory cells, suggesting that bitter substances induce the response by nonreceptor-mediated mechanism. (d) There is also a possibility that receptors for some bitter substances are G-protein coupled.
1(0,0,0,1) Details
8710935 Jakubik J, Bacakova L, Lisa V, el-Fakahany EE, Tucek S: Activation of muscarinic acetylcholine receptors via their allosteric binding sites. Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8705-9.


We have now found that the muscarinic receptor allosteric modulators alcuronium, gallamine, and strychnine (acting in the absence of an agonist) alter the synthesis of cAMP in Chinese hamster ovary (CHO) cells expressing the M2 or the M4 subtype of muscarinic receptors in the same direction as the agonist carbachol.
0(0,0,0,0) Details
8845730 Heilbronn E, Jarlebark L, Lawoko G: Cholinergic and purinergic signalling in outer hair cells of mammalian cochlea. Neurochem Int. 1995 Oct-Nov;27(4-5):301-11.


Strychnine, a glycine receptor blocker suggested to interfere with cholinergic sites of the efferent OHC synapse, was found to bind to OHC (cold strychnine for unspecific binding).
0(0,0,0,0) Details