Page last updated: 2024-10-24

glutamate receptor signaling pathway

Definition

Target type: biologicalprocess

The series of molecular signals initiated by the binding of glutamate to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, PMID:9131252]

Glutamate receptor signaling is a fundamental process in the nervous system, mediating a wide range of neuronal functions, including learning, memory, and synaptic plasticity. This pathway is initiated by the binding of glutamate, the primary excitatory neurotransmitter in the brain, to specific glutamate receptors located on the postsynaptic membrane of neurons. There are two main classes of glutamate receptors: ionotropic receptors (iGluRs) and metabotropic receptors (mGluRs).

iGluRs are ligand-gated ion channels that directly open upon glutamate binding, allowing the influx of ions, primarily sodium and calcium, into the postsynaptic neuron. This influx depolarizes the neuron, increasing its excitability and triggering action potentials. There are three major subtypes of iGluRs: NMDA receptors (NMDARs), AMPA receptors (AMPARs), and kainate receptors (KARs).

NMDARs are unique in requiring both glutamate binding and membrane depolarization to open. This dual requirement makes them critical for synaptic plasticity, particularly long-term potentiation (LTP), a process essential for learning and memory. AMPARs are responsible for the majority of fast excitatory synaptic transmission, while KARs play a more modulatory role.

mGluRs, on the other hand, are G-protein coupled receptors (GPCRs) that initiate intracellular signaling cascades upon glutamate binding. These cascades involve the activation of various second messengers, such as cyclic AMP (cAMP) and inositol triphosphate (IP3), leading to a wide range of downstream effects, including changes in gene expression, neuronal excitability, and synaptic plasticity.

The glutamate receptor signaling pathway is tightly regulated by a complex interplay of factors, including the availability of glutamate, the expression and trafficking of receptors, and the activity of various signaling molecules. Dysregulation of this pathway is implicated in a variety of neurological disorders, including epilepsy, Alzheimer's disease, and schizophrenia. The study of glutamate receptor signaling continues to be a vibrant area of research, with implications for understanding and treating a wide range of neurological conditions.'
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Proteins (15)

ProteinDefinitionTaxonomy
Guanine nucleotide-binding protein G(q) subunit alphaA guanine nucleotide-binding protein G(q) subunit alpha that is encoded in the genome of human. [PRO:DNx, UniProtKB:P50148]Homo sapiens (human)
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase beta-1A 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase beta-1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NQ66]Homo sapiens (human)
NicastrinA nicastrin that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q92542]Homo sapiens (human)
Glutamate receptor ionotropic, kainate 4A glutamate receptor ionotropic, kainate 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16099]Homo sapiens (human)
Glutamate receptor ionotropic, NMDA 2CA glutamate receptor ionotropic, NMDA 2C that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q14957]Homo sapiens (human)
Potassium voltage-gated channel subfamily B member 1A voltage-gated potassium channel KCNB1 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q14721]Homo sapiens (human)
Glutamate receptor ionotropic, NMDA 2BA glutamate receptor ionotropic, NMDA 2B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13224]Homo sapiens (human)
Glutamate receptor ionotropic, kainate 3A glutamate receptor ionotropic, kainate 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13003]Homo sapiens (human)
Glutamate receptor ionotropic, kainate 2A glutamate receptor ionotropic, kainate 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13002]Homo sapiens (human)
Glutamate receptor ionotropic, NMDA 2AA glutamate receptor ionotropic, NMDA 2A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q12879]Homo sapiens (human)
Glutamate receptor 4A glutamate receptor 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P48058]Homo sapiens (human)
Excitatory amino acid transporter 3An excitatory amino acid transporter 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P43005]Homo sapiens (human)
Glutamate receptor 3A glutamate receptor 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P42263]Homo sapiens (human)
Glutamate receptor ionotropic, kainate 1A glutamate receptor ionotropic, kainate 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P39086]Homo sapiens (human)
Somatostatin receptor type 1A somatostatin receptor type 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30872]Homo sapiens (human)

Compounds (169)

CompoundDefinitionClassesRoles
aminolevulinic acid5-aminolevulinic acid : The simplest delta-amino acid in which the hydrogens at the gamma position are replaced by an oxo group. It is metabolised to protoporphyrin IX, a photoactive compound which accumulates in the skin. Used (in the form of the hydrochloride salt)in combination with blue light illumination for the treatment of minimally to moderately thick actinic keratosis of the face or scalp.

Aminolevulinic Acid: A compound produced from succinyl-CoA and GLYCINE as an intermediate in heme synthesis. It is used as a PHOTOCHEMOTHERAPY for actinic KERATOSIS.
4-oxo monocarboxylic acid;
amino acid zwitterion;
delta-amino acid
antineoplastic agent;
dermatologic drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
5-aminovaleric acid5-aminopentanoic acid : A delta-amino acid comprising pentanoic acid with an amino substituent at C-5; a methylene homologue of gamma-aminobutyric acid (GABA) that is a weak GABA agonist.

5-aminovaleric acid: from red fox anal secretion; RN given refers to parent cpd
amino acid zwitterion;
delta-amino acid;
omega-amino fatty acid
human metabolite
alanylalaninealanylalanine: RN given refers to (DL)-isomerdipeptide
sperminepolyazaalkane;
tetramine
antioxidant;
fundamental metabolite;
immunosuppressive agent
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acidalpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid: An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies.non-proteinogenic alpha-amino acid
6,7-dichloroquinoxaline-2,3-dionequinoxaline derivative
tacrinetacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.

Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
acridines;
aromatic amine
EC 3.1.1.7 (acetylcholinesterase) inhibitor
N-(2-aminoethyl)-5-chloro-1-naphthalenesulfonamidenaphthalenes;
sulfonic acid derivative
amantadineamant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first sourceadamantanes;
primary aliphatic amine
analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
aniracetamN-acylpyrrolidine;
pyrrolidin-2-ones
arcaine1,4-diguanidinobutane : A guanidine derivative consisting of butane having guanidino groups at the 1- and 4-positions.

arcaine: RN given refers to parent cpd; structure
guanidines
chlorpromazinechlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.

Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.
organochlorine compound;
phenothiazines;
tertiary amine
anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
clofibric acidclofibric acid : A monocarboxylic acid that is isobutyric acid substituted at position 2 by a p-chlorophenoxy group. It is a metabolite of the drug clofibrate.

Clofibric Acid: An antilipemic agent that is the biologically active metabolite of CLOFIBRATE.
aromatic ether;
monocarboxylic acid;
monochlorobenzenes
anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist
cyclothiazidecyclothiazide : 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted at positions 3, 5 and 6 by a 2-norbornen-5-yl group, chlorine, and a sulfonamide group, respectively. A thiazide diuretic, it has been used in the management of hypertension and oedema.

cyclothiazide: inhibits the desensitization of AMPA-type receptors; structure
benzothiadiazineantihypertensive agent;
diuretic
racemethorphan6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene : An organic heterotetracyclic compound that is 1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene which is substituted by a methoxy group at position 6 and a methyl group at position 11.aromatic ether;
morphinane alkaloid;
morphinane-like compound;
organic heterotetracyclic compound
felbamatefelbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy.

Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.
carbamate esteranticonvulsant;
neuroprotective agent
ifenprodilifenprodil: NMDA receptor antagonistpiperidines
7-amino-4-chloro-3-methoxy-2-benzopyran-1-oneisocoumarins
ketamineketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.

Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.
cyclohexanones;
monochlorobenzenes;
secondary amino compound
analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
kynurenic acidkynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4.

Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool.
monohydroxyquinoline;
quinolinemonocarboxylic acid
G-protein-coupled receptor agonist;
human metabolite;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist;
Saccharomyces cerevisiae metabolite
memantineadamantanes;
primary aliphatic amine
antidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
methoctraminearomatic ether;
tetramine
muscarinic antagonist
orphenadrineorphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.

Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
ether;
tertiary amino compound
antidyskinesia agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
pentamidinepentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.

Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.
aromatic ether;
carboxamidine;
diether
anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
procyclidineprocyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.

Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.
pyrrolidines;
tertiary alcohol
antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist
cysteinecysteine;
cysteine zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid
EC 4.3.1.3 (histidine ammonia-lyase) inhibitor;
flour treatment agent;
human metabolite
aspartic acidaspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent

Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.

L-aspartic acid : The L-enantiomer of aspartic acid.
aspartate family amino acid;
aspartic acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
mouse metabolite;
neurotransmitter
phencyclidinephencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects.

Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.
benzenes;
piperidines
anaesthetic;
neurotoxin;
NMDA receptor antagonist;
psychotropic drug
kainic acidKainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.dicarboxylic acid;
L-proline derivative;
non-proteinogenic L-alpha-amino acid;
pyrrolidinecarboxylic acid
antinematodal drug;
excitatory amino acid agonist
glycylglycinedipeptide;
dipeptide zwitterion
human metabolite
camptothecinNSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first sourcedelta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol
antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
2,3-dihydroxyquinoxaline2,3-dihydroxyquinoxaline: fluorescent oxalic acid deriv.
glutamic acidglutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.

Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
bezafibratearomatic ether;
monocarboxylic acid;
monocarboxylic acid amide;
monochlorobenzenes
antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
eliprodil1-(4-chlorophenyl)-2-[4-(4-fluorobenzyl)piperidin-1-yl]ethanol : A member of the class of piperidines that is piperidine substituted by a 2-(4-chlorophenyl)-2-hydroxyethyl group at position 1 and by a 4-fluorobenzyl group at position 4.monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary alcohol;
tertiary amino compound
fenofibric acidfenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.

fenofibric acid: RN given refers to parent cpd without isomeric designation; structure
aromatic ketone;
chlorobenzophenone;
monocarboxylic acid
drug metabolite;
marine xenobiotic metabolite
25-hydroxycholesterol25-hydroxy steroid;
oxysterol
human metabolite
selfotelselfotel: a N-methyl-D-aspartate (NMDA) antagonist; used to treat stroke-induced impairmentnon-proteinogenic alpha-amino acid
budipinebudipine: RN given refers to parent cpd; structure in Negwer, 5th ed, #6541diarylmethane
rosiglitazoneaminopyridine;
thiazolidinediones
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
6,7-dichloroquinoxaline-2,3-dione
leucyl-alanineLeu-Ala : A dipeptide composed of L-leucine and L-alanine joined by a peptide linkage.dipeptidemetabolite
alanylprolinealanylproline: RN given refers to all (L)-isomerdipeptide;
dipeptide zwitterion
metabolite
tarenflurbiltarenflurbil: R-enantiomer of flurbiprofen but not a COX inhibitor; modulates NF-kB, gamma-secretase, amyloid beta-protein;flurbiprofen
cholanic acid5beta-cholanic acids;
cholanic acid
glycylleucineGly-Leu : A dipeptide composed of glycine and L-leucine joined by a peptide linkage.dipeptide;
dipeptide zwitterion
metabolite
alanyltyrosineAla-Tyr : A dipeptide composed of L-alanine and L-tyrosine joined by a peptide linkage.

alanyltyrosine: tyrosine source; RN given refers to (L)-isomer
dipeptidemetabolite
glycylsarcosineglycylsarcosine : A dipeptide obtained by formal condensation of the carboxy group of glycine with the amino group of sarcosine.dipeptide;
dipeptide zwitterion
sym 2081
glycylaspartic acidglycylaspartic acid: RN given refers to (L)-isomerdipeptidemetabolite
histidinoalaninehistidinoalanine: cross-linking amino acid in calcified tissue collagen; RN given refers to (L)-isomerdipeptide;
dipeptide zwitterion
metabolite
pregnenolone sulfatepregnenolone sulfate: RN given refers to (3 beta)-isomersteroid sulfateEC 2.7.1.33 (pantothenate kinase) inhibitor;
human metabolite
dihydrokainatedicarboxylic acid
jstx-3JSTX-3: structure in first sourceN-acyl-amino acid
24-hydroxycholesterol(24S)-24-hydroxycholesterol : A 24-hydroxycholesterol that has S configuration at position 24. It is the major metabolic breakdown product of cholesterol in the brain.24-hydroxycholesterolbiomarker;
human blood serum metabolite;
mouse metabolite
argiotoxin-636argiotoxin-636: from the venom of Argiope aurantia; blocks neuromuscular transmission in insects; structure in first source.N-acyl-amino acid
1,2-hexanoylphosphatidylcholine1,2-hexanoylphosphatidylcholine: RN given refers to cpd without isomeric designation
2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid: glutamate receptor antagonist; protects against kainic acid neurotoxicity in cultured cerebral cortex neurons
5-fluorowillardiine3-(5-fluorouracil-1-yl)-L-alanine : An alanine derivative that is L-alanine bearing a 5-fluorouracil-1-yl substituent at position 3. A more potent and selective AMPA receptor agonist (at hGluR1 and hGluR2) than AMPA itself (Ki = 14.7, 25.1, and 1820 nM for hGluR1, hGluR2 and hGluR5 respectively).

5-fluorowillardiine: a glutamate agonist; RN given for (S)-isomer
L-alanine derivative;
non-proteinogenic L-alpha-amino acid;
organofluorine compound
AMPA receptor agonist
ly 293558tezampanel: structure given in first source; an AMPA receptor antagonist
alanylglutamic acidalanylglutamic acid: RN given refers to (L)-isomer

L-alanyl-L-glutamic acid : A dipeptide consisting of L-glutamic acid having an L-alanyl attached to its alpha-amino group
dipeptide
ns 1608NS 1608: a BK(Ca) channel openerureas
bdp 121-(quinoxalin-6-ylcarbonyl)piperidine: modulates AMPA receptor desensitization ; an analog of 1-(1,3-benzodioxol-5-ylcarbonyl)piperidineN-acylpiperidine
prolyl-tyrosinePro-Tyr : A dipeptide formed from L-proline and L-tyrosine residues.

prolyl-tyrosine: structure given in first source
dipeptidemetabolite
besonprodilbesonprodil: CI-1041 is also known as PD19680; NMDA receptor antagonist for treatment of Parkinson's disease; structure in first source
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
edotreotideEdotreotide: DOTA - 1,4,7,10-tetraazacyclododecanetetracetic acid; structure given in first source; may be labelled with various radioisotopes
philanthotoxin 343philanthotoxin 343: structure given in first source (see article's footnote); identical to philanthotoxin 433 except that the number of methylene groups between the respective amine moieties is 3,4,3 instead of 4,3,3N-acyl-amino acid
serine o-sulfateL-serine O-sulfate : A non-proteinogenic L-alpha-amino acid that is the O-sulfo derivative of L-serine.

serine O-sulfate: RN given refers to (L)-isomer
L-serine derivative;
non-proteinogenic L-alpha-amino acid;
O-sulfoamino acid
5-bromowillardiine5-bromowillardiine: acts as a kainate-like agonist on chick EAA receptors expressed in Xenopus oocytes; RN given refers to (S)-isomer; RN for cpd without isomeric designation not avail 5/91
dizocilpinesecondary amino compound;
tetracyclic antidepressant
anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
memantine hydrochloridehydrochlorideantidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
esketamineesketamine : The S- (more active) enantiomer of ketamine.ketamineanalgesic;
intravenous anaesthetic;
NMDA receptor antagonist
cns 5161CNS 5161: structure in first source
prolylglutamic acidPro-Glu : A dipeptide formed from L-proline and L-glutamic acid residues.dipeptidemetabolite
cp 101,606traxoprodil mesylate: a selective NMDA antagonist; structure given in first source
cysteinylglycinecysteinylglycine: RN given refers to (L)-isomer; RN for cpd without isomeric designation not in Chemlne 7/13/83

L-cysteinylglycine : A dipeptide consisting of glycine having an L-cysteinyl attached to its alpha-amino group. It is an intermediate metabolite in glutathione metabolism.
dipeptide;
dipeptide zwitterion
Escherichia coli metabolite;
human metabolite;
Saccharomyces cerevisiae metabolite
willardiine3-(uracil-1-yl)-L-alanine : The 3-(uracil-1-yl) derivative of L-alanine.

willardiine: isolated from seeds of Acacia willariana; structure
amino acid zwitterion;
L-alanine derivative;
non-proteinogenic L-alpha-amino acid
hinokininhinokinin : A lignan that is dihydrofuran-2(3H)-one (gamma-butyrolactone) substituted by a 3,4-methylenedioxybenzyl group at positions 3 and 4 (the 3R,4R-diastereoisomer).

hinokinin: suppresses expression of both HBsAg and HBeAg
benzodioxoles;
gamma-lactone;
lignan
trypanocidal drug
3-hydroxyaspartic acid, (threo-l)-isomer(3S)-3-hydroxy-L-aspartic acid : The (3S)-diastereomer of 3-hydroxy-L-aspartic acid.3-hydroxy-L-aspartic acidmetabolite
(S)-ATPA(S)-ATPA : A non-proteinogenic L-alpha-amino acid that is L-alanine in which one of the methyl hydrogens is replaced by a 5-tert-butyl-3-hydroxy-isooxazol-4-yl group.isoxazoles;
non-proteinogenic L-alpha-amino acid
metabolite
t0901317T0901317: an LXRalpha and LXRbeta agonist
aspartyl-aspartic acidAsp-Asp : A dipeptide formed from two L-aspartic acid units.

aspartyl-aspartic acid: do not confuse with cyclo(Asp-Asp)
dipeptideMycoplasma genitalium metabolite
ly382884benzoic acids
4-bromohomoibotenic acid, (rs)-isomer
glycylprolineGly-Pro : A dipeptide consisting of L-proline having a glycyl residue attached to its alpha-amino group.dipeptide;
dipeptide zwitterion
metabolite
6-methyl-2-(phenylethynyl)pyridine2-methyl-6-(phenylethynyl)pyridine : A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.

6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist
acetylenic compound;
methylpyridines
anxiolytic drug;
metabotropic glutamate receptor antagonist
dexoxadrol
7-chloro-thiokynurenate7-chlorothiokynurenic acid: glycine site antagonist of NMDA receptor
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline: structure given in first source; neuroprotectant for cerebral ischemia; AMPA receptor antagonistnaphthalenes;
sulfonic acid derivative
6-cyano-7-nitroquinoxaline-2,3-dione6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.quinoxaline derivative
fg 9041FG 9041: structure given in first sourcequinoxaline derivative
2-amino-3-phenylmethoxybutanedioic acidaspartic acid derivative
(3-chlorophenyl)(6,7-dimethoxy-1-((4-methoxyphenoxy)methyl)-3,4-dihydroisoquinolin-2(1h)-yl)methanone(3-chlorophenyl)(6,7-dimethoxy-1-((4-methoxyphenoxy)methyl)-3,4-dihydroisoquinolin-2(1H)-yl)methanone: a positive modulator of GluN2C/GluN2D subunit-selective NMDA receptor
4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1h-pyrazol-1-yl)-4-oxobutanoic acid4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid: structure in first source
seryl-prolineSer-Pro : A dipeptide formed from L-serine and L-proline residues.dipeptidemetabolite
tcn 201
l 7458703-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine: selective for D(4) receptors; structure in first sourcepiperazines
dl-threo-beta-benzyloxyaspartate
n-(n-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl esterDAPT : A dipeptide consisting of alanylphenylglycine derivatised as a 3,5-difluorophenylacetamide at the amino terminal and a tert-butyl ester at the carboxy terminal. A gamma-secretase inhibitor.carboxylic ester;
difluorobenzene;
dipeptide;
tert-butyl ester
EC 3.4.23.46 (memapsin 2) inhibitor
l803087L-803087 : A fluoroindole that is 1H-indole substituted by phenyl, 4-{[(2S)-5-carbamimidamido-1-methoxy-1-oxopentan-2-yl]amino}-4-oxobutyl, fluoro and fluoro groups at positions 2, 3, 5 and 7, respectively. It is a selective nonpeptidic agonist of the somatostatin subtype-4 (SST4) receptor with Ki of 0.7 nM.

L803087: structure in first source
benzenes;
fluoroindole;
guanidines;
L-arginine derivative;
methyl ester;
phenylindole;
secondary carboxamide
somatostatin receptor agonist
obelinobelin: calcium-sensitive photoprotein obtained from the hydroid Obelia geniculata
seglitideseglitide: more potent than somatostatin for inhibition of insulin, glucagon & growth hormone release; used experimentally in treatment of Alzheimer's disease; somatostatin receptor antagonist
sulindac sulfidesulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.

sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source
aryl sulfide;
monocarboxylic acid;
organofluorine compound
antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug
levorphanolLevorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.morphinane alkaloid
dextromethorphandextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.

Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.
6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
dextrorphanDextrorphan: Dextro form of levorphanol. It acts as a noncompetitive NMDA receptor antagonist, among other effects, and has been proposed as a neuroprotective agent. It is also a metabolite of DEXTROMETHORPHAN.morphinane alkaloid
l 685458L 685458: a gamma-secretase inhibitor; structure in first source

L-685,458 : A peptide and carboxamide that is L-leucyl-L-phenylalaninamide, L-Leu-L-Phe-NH2, which has been acylated on the N-terminus by a Phe-Phe hydroxyethylene dipeptide isotere, 2R-benzyl-5S-tert-butoxycarbonylamino-4R-hydroxy-6-phenylhexanoic acid. Compounds based on the structure of L-685,458 are potent inhibitors of gamma-secretase, which mediates the final catalytic step that generates the amyloid beta-peptide (Abeta), which assembles into the neurotoxic aggregates in the brains of sufferers of Alzheimer's disease.
carbamate ester;
monocarboxylic acid amide;
peptide;
secondary alcohol
EC 3.4.23.46 (memapsin 2) inhibitor;
peptidomimetic
licostinellicostinel: a glycine site NMDA receptor antagonist; structure given in first source
lofepramine hydrochloride
phenylalanylalaninePhe-Ala : A dipeptide formed from L-phenylalanine and L-alanine residues.

phenylalanylalanine: RN given refers to (L)-isomer
dipeptide;
dipeptide zwitterion
metabolite
acetylalanylalanineacetylalanylalanine: RN given refers to (D)-isomer
alpha-aspartylalaninealpha-aspartylalanine: found in pig brain

Asp-Ala : A dipeptide formed from L-alpha-aspartyl and L-valine residues.
dipeptidemetabolite
alanyltyrosineTyr-Ala : A dipeptide formed from L-tyrosine and L-alanine residues.dipeptidemetabolite
ubp 310UBP 310: a GluR5 antagonist; structure in first source
ubp 302
prolylglycineL-prolylglycine : A dipeptide consisting of glycine having an L-prolyl group attached to its alpha-amino nitrogen.

prolylglycine: RN given refers to (L)-isomer
dipeptide;
dipeptide zwitterion
ro 25-6981Ro 25-6981 : A member of the class of piperidines that is 4-benzylpiperidine substituted by a 3-hydroxy-3-(4-hydroxyphenyl)-2-methylpropyl group at position 1 (the 1R,2S-stereoisomer). It is a potent antagonist of the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor.

Ro 25-6981: blocks NMDA receptors containg NR2B subunit; structure in first source
benzenes;
phenols;
piperidines;
secondary alcohol;
tertiary amino compound
anticonvulsant;
antidepressant;
neuroprotective agent;
NMDA receptor antagonist
lanreotide
eaa-090EAA-090: a potent N-methyl-D-aspartate antagonist; structure in first sourcedialkylarylamine;
tertiary amino compound
pd 174494PD 174494: structure in first sourcepiperidines
glutamylalanineGlu-Ala : A dipeptide formed from L-alpha-glutamyl and L-alanine residues.dipeptidemetabolite
phenylalanylphenylalaninePhe-Phe : A dipeptide formed from two L-phenylalanine residues.dipeptide;
L-aminoacyl-L-amino acid zwitterion
human blood serum metabolite;
Mycoplasma genitalium metabolite
phenylalanyl-valineVal-Phe : A dipeptide formed from L-valine and L-phenylalanine residues.dipeptidemetabolite
alanylglycinedipeptide;
dipeptide zwitterion
metabolite
valyltyrosineVal-Tyr : A dipeptide formed from L-valine and L-tyrosine residues.

valyltyrosine: from sardine muscle hydrolyzate
dipeptidemetabolite
phenylalanylprolinePhe-Pro : A dipeptide formed from L-phenylalanine and L-proline residues.dipeptidemetabolite
glycylhistidineGly-His : A dipeptide composed of glycine and L-histidine joined by a peptide linkage.

glycylhistidine: RN given refers to (L)-isomer
dipeptide;
dipeptide zwitterion
metabolite
prolyl-serinePro-Ser : A dipeptide formed from L-proline and L-serine residues.dipeptidemetabolite
fpl 15896ar
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine: an excitatory amino acid antagonist
(4-benzylpiperidin-1-yl)-(6-hydroxy-1h-indol-2-yl)methanone(4-benzylpiperidin-1-yl)-(6-hydroxy-1H-indol-2-yl)methanone: an NR2B-subunit selective antagonist; structure in first source
mk 0752
prolylvalineVal-Pro : A dipeptide formed from L-valine and L-proline residues.dipeptidemetabolite
dysiherbainedysiherbaine : A furopyran that is (3aR,7aR)-hexahydro-2H-furo[3,2-b]pyran substituted by carboxy, (2S)-2-amino-2-carboxyethyl, hydroxy and methylamino groups at positions 2, 2, 6, and 7, respectively (the 2R,3aR,6S,7R,7aR-stereoisomer). A convulsant isolated from the marine sponge Dysidea herbacea that has high affinity for kainate ionotropic glutamate receptors.

dysiherbaine: an exitotoxic amino acid; structure in first source
amino dicarboxylic acid;
furopyran;
hydroxy carboxylic acid;
secondary amino compound
animal metabolite;
excitatory amino acid agonist;
marine metabolite;
neurotoxin
tqx 173
ly 450139peptide
(1rs,1's)-peaqx
gw 9578GW 9578: a peroxisome proliferator-activated receptor alpha agonist; structure in first source
ns 1652NS 1652: an anion conductance inhibitor; structure in first source
l 363301
ym-254890YM-254890: structure in first source
ly 392098LY 392098: structure in first source
ly 404187LY 404187: structure in first source
pasireotidepasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease.homodetic cyclic peptide;
peptide hormone
antineoplastic agent
chf 50741-(3',4'-dichloro-2-fluoro(1,1'-biphenyl)-4-yl)cyclopropanecarboxylic acid: a beta-amyloid(1-42) lowering agent; structure in first source
ns3694NS3694: an apoptosome inhibitorureas
ly 411575dibenzoazepine;
difluorobenzene;
lactam;
secondary alcohol
EC 3.4.23.46 (memapsin 2) inhibitor
4-(2-((1r)-1-(((4-chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acidsulfonamide
begacestat
naluzotannaluzotan: an antidepressant and anti-anxiety agent; structure in first source
e 2012
mrk 560MRK 560: a gamma-secretase inhibitor; MRK-560 is the (cis)-isomer; structure in first source
l-beta-threo-benzyl-aspartateL-beta-threo-benzyl-aspartate: structure in first source
ubp296UBP296: potent and selective kainate receptor antagonist; structure in first sourcealpha-amino acid
FR900359FR900359: G-protein inhibitor from Ardisia crenata sims that shows inhibition of platelet aggregation and decrease of blood pressurecyclodepsipeptide
etoxadroletoxadrol: was heading 1975-94 (see under PIPERIDINES 1975-90); use PIPERIDINES to search ETOXADROL 1975-90; dissociative anesthetic with some cardiovascular effectsketal
methoxydine1-(1-(4-methoxyphenyl)cyclohexyl)piperidine: a glutamate NMDA receptor ligand; structure in first source
l 054522L 054522: somatostatin receptor subtype 2 agonist; structure in first source
somatostatinheterodetic cyclic peptide;
peptide hormone
ucph 1012-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile: structure in first source
1, 3-di-(n-carboxybenzoyl-leucyl-leucyl)amino acetone1, 3-di-(N-carboxybenzoyl-leucyl-leucyl)amino acetone: structure in first source
nitd 609NITD 609: an antimalarial and coccidiostat; structure in first source
pf 3084014nirogacestat : A member of the class of imidazoles that is 1H-imidazole substituted by a 1-[(2,2-dimethylpropyl)amino]-2-methylpropan-2-yl group at position 1 and a {N-[(2S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-L-norvalyl}amino group at position 4. It is a gamma-secretase inhibitor whose hydrobromide salt is indicated for adult patients with progressing desmoid tumours who require systemic treatment.

nirogacestat: an antineoplastic agent
bms 708163BMS 708163: structure in first sourceoxadiazole;
ring assembly
wms 1410
ro 4929097dibenzoazepine;
dicarboxylic acid diamide;
lactam;
organofluorine compound
EC 3.4.23.46 (memapsin 2) inhibitor
jnj 40418677
(r)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1h-pyrazolo(4,3-c)quinoline(R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo(4,3-c)quinoline: gamma secretase inhibitor; structure in first source