eglumetad profile

eglumetad: LY-354740 is the active isomer, LY-366563 is the inactive isomer, and LY 314582 is the racemate; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	213056
CHEMBL ID	8759
CHEBI ID	194387
SCHEMBL ID	481248
MeSH ID	M0273499

Synonym
gtpl1393
[3h]eglumegad
[3h]ly354740
gtpl1396
eglumegad
(1s,2s,5r,6s)-2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid
ly354740
ly 354740
ly-354740
eglumetad anhydrous
CHEMBL8759 ,
D08908
176199-48-7
eglumegad (inn)
2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
(2s,6s)-2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid(ly354740)
(1s,2s,5r,6s)-2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid (ly 354740)
bdbm50056272
eglumetad
(1s,2s,5r,6s)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CHEBI:194387
(+)-(1s,2s,5r,6s)-2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid
bicyclo(3.1.0)hexane-2,6-dicarboxylic acid, 2-amino-, (1s,2s,5r,6s)-
(+)-2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylic acid
unii-onu5a67t2s
eglumetad [usan:inn]
onu5a67t2s ,
bdbm50397661
AKOS015900075
40F ,
eglumetad [inn]
CS-5052
VTAARTQTOOYTES-RGDLXGNYSA-N
SCHEMBL481248
HY-18941
DTXSID40170094
bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1s,2s,5r,6s)- (9ci)
J-011170
NCGC00485401-01
bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-, (1s,2s,5r,6s)-
Q5348096
AMY14831
mfcd04113018
ly354740;eglumetad
A924691
MS-22995
ly 354740 hydrate
EN300-72644
BL162676
AT33389
(1s,2s,5r,6s)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylicacid
HY-18941B
(rel)-eglumegad
CS-0881508

Excerpt	Reference	Relevance
" Herein, we report the in vitro pharmacological profile and pharmacokinetic properties of another potent, selective, and structurally novel mGlu2/3 receptor agonist, (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3."	( Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid Burkey, JL; Calligaro, DO; Catlow, JT; Giera, DD; Herin, MF; Johnson, BG; Kingston, AE; Marek, GJ; McKinzie, DL; Monn, JA; Nisenbaum, ES; Rorick-Kehn, LM; Schoepp, DD; Wright, RA, 2007)	0.34
" The current data describe the pharmacokinetic behavior of LY544344 and LY354740, with a specific focus on the first-pass activation processes and dose linearity in rats and dogs."	( Pharmacokinetics, metabolism, and excretion of the intestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S,2S,5R,6S)-2-[(2'S)-(2-amino)propionyl]aminobicyclo[3.1.0.]hexen-2,6-dicarboxylic acid (LY544344) in rats and dogs: assessment of first-pass Abraham, T; Perkins, EJ, 2007)	0.34

Excerpt	Reference	Relevance
" The oral bioavailability of LY354740 was approximately 10% in rats and 45% in dogs."	( The disposition, metabolism, and pharmacokinetics of a selective metabotropic glutamate receptor agonist in rats and dogs. Chay, SH; Herman, JL; Johnson, JT; Kassahun, K; Mattiuz, EL; Phillips, DL; Swanson, SP; Wheeler, WJ, 2002)	0.31
" Its relatively low bioavailability in different animal species drove the need for an effective prodrug form that would produce a therapeutic response at lower doses for the treatment of anxiety disorders."	( Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist. Bueno, AB; Catlow, J; Clay, MP; Coffey, DS; Collado, I; Dantzig, AH; de Dios, A; Domínguez, C; Herin, MF; Jiang, H; Lindstrom, T; Martín, JA; Martín, LM; Martínez-Grau, MA; Monn, JA; Montero, C; Pedregal, C; Schoepp, DD; Stratford, RE; Tabas, LB; Tizzano, JP; Wright, RA, 2005)	0.33
" Although animal and human studies demonstrate potential therapeutic utility, poor oral bioavailability is a limiting factor in the clinical development of these compounds."	( Improved bioavailability of the mGlu2/3 receptor agonist LY354740 using a prodrug strategy: in vivo pharmacology of LY544344. Hart, JC; Johnson, BG; Knitowski, KM; McKinzie, DL; Perkins, EJ; Rorick-Kehn, LM; Schoepp, DD, 2006)	0.33
" Interestingly, despite the slightly lower potency (approximately 2-5-fold) of LY404039 versus LY354740 in binding, functional, and electrophysiological assays, LY404039 demonstrated higher plasma exposure and better oral bioavailability in pharmacokinetic experiments."	( Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid Burkey, JL; Calligaro, DO; Catlow, JT; Giera, DD; Herin, MF; Johnson, BG; Kingston, AE; Marek, GJ; McKinzie, DL; Monn, JA; Nisenbaum, ES; Rorick-Kehn, LM; Schoepp, DD; Wright, RA, 2007)	0.34
" Pharmacokinetic analysis of mGlu active enantiomers (+)-11 and (-)-12 in rats showed each to be well absorbed following oral administration."	( Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors. Andis, SL; Bures, M; Catlow, J; Giera, D; Henry, SS; Hérin, M; Johnson, BG; Kingston, A; Massey, SM; Monn, JA; Schoepp, DD; Stephenson, GA; Valli, MJ; Wright, RA, 2007)	0.34
"]hexen-2,6-dicarboxylic acid, also known as LY544344, was discovered to improve the oral bioavailability of the parent drug (+)-2-aminobicyclo[3."	( Pharmacokinetics, metabolism, and excretion of the intestinal peptide transporter 1 (SLC15A1)-targeted prodrug (1S,2S,5R,6S)-2-[(2'S)-(2-amino)propionyl]aminobicyclo[3.1.0.]hexen-2,6-dicarboxylic acid (LY544344) in rats and dogs: assessment of first-pass Abraham, T; Perkins, EJ, 2007)	0.34
"The limited oral bioavailability of the potent and selective group II metabotropic glutamate (mGlu) 2/3 receptor agonist, (1S,2S,5R,6S)-2-aminobicyclo[3."	( Transepithelial transport of the group II metabotropic glutamate 2/3 receptor agonist (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate (LY354740) and its prodrug (1S,2S,5R,6S)-2-[(2'S)-(2'-amino)propionyl]aminobicyclo[3.1.0]hexane-2,6-dicarboxy Eriksson, AH; Pak, YA; Perkins, EJ; Sawada, G; Varma, MV; Zimmerman, CL, 2009)	0.35
" Its alanyl prodrug, LY544344, showed high affinity to the intestinal peptide transporter PEPT1, and improved the oral bioavailability of LY354740 in various animal models."	( The intestinal absorption of a prodrug of the mGlu2/3 receptor agonist LY354740 is mediated by PEPT1: in situ rat intestinal perfusion studies. Eriksson, AH; Perkins, EJ; Varma, MV; Zimmerman, CL, 2010)	0.36
" Further characterization of the α-fluoro-substituted analogue (LY459477) in vivo revealed that this molecule possesses good oral bioavailability in rats and effectively suppresses phencyclidine-evoked locomotor activity at doses that do not impair neuromuscular coordination."	( Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists. Bures, MG; Carter, JH; Catlow, JT; Getman, BG; Hao, J; Heinz, BA; Henry, SS; Herin, M; Johnson, BG; Massey, SM; McKinzie, DL; Monn, JA; Reinhard, MR; Stephenson, GA; Swanson, S; Valli, MJ; Wang, X, 2013)	0.39
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" LY354740 and LY379268 were protective against transient global ischemia in gerbils when dosed intraperitoneally."	( Neuroprotective actions of novel and potent ligands of group I and group II metabotropic glutamate receptors. Battaglia, G; Bond, A; Bruno, V; Clark, BP; Harris, JR; Kingston, AE; Lodge, D; Monn, JA; Nicoletti, F; O'Neill, MJ; Schoepp, DD, 1999)	0.3

Class	Description
L-alpha-amino acid	Any alpha-amino acid having L-configuration at the alpha-carbon.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Metabotropic glutamate receptor 8	Homo sapiens (human)	Ki	12.0000	0.0610	3.6885	9.5000	AID107274
Metabotropic glutamate receptor 6	Homo sapiens (human)	Ki	3.0000	0.4000	2.5000	5.8000	AID107093
Glutamate receptor 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0001	1.6179	10.0000	AID92213
Glutamate receptor 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0001	1.7000	10.0000	AID92213
Glutamate receptor 3	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0001	1.7000	10.0000	AID92213
Glutamate receptor 4	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0001	1.7000	10.0000	AID92213
Glutamate receptor ionotropic, kainate 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0070	0.9821	7.0000	AID93553
Metabotropic glutamate receptor 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	458.0000	0.0002	0.5887	8.9900	AID108514
Metabotropic glutamate receptor 2	Rattus norvegicus (Norway rat)	Ki	26,666.8331	0.0031	0.1265	0.4760	AID108996; AID1468323; AID239082
Metabotropic glutamate receptor 3	Rattus norvegicus (Norway rat)	Ki	0.2648	0.0030	0.1340	0.4760	AID109312; AID1468323
Metabotropic glutamate receptor 5	Homo sapiens (human)	Ki	100.0000	0.0005	0.5463	8.2000	AID107059
Glutamate receptor ionotropic, kainate 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0070	1.0132	7.0000	AID93553
Glutamate receptor ionotropic, kainate 3	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0070	1.0132	7.0000	AID93553
Glutamate receptor ionotropic, kainate 4	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0070	1.0132	7.0000	AID93553
Neuronal acetylcholine receptor subunit alpha-7	Rattus norvegicus (Norway rat)	Ki	0.0847	0.0000	0.7307	8.0000	AID239378
Metabotropic glutamate receptor 1	Homo sapiens (human)	Ki	100.0000	0.0003	3.5363	10.0000	AID108489
Metabotropic glutamate receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0063	0.0029	0.4662	4.3000	AID1714559; AID748169
Metabotropic glutamate receptor 2	Homo sapiens (human)	Ki	0.0595	0.0027	0.7158	6.4000	AID108829; AID108830; AID108837; AID1247513; AID1468291; AID239378; AID239426; AID275487
Metabotropic glutamate receptor 7	Homo sapiens (human)	Ki	100.0000	0.9900	0.9900	0.9900	AID107261
Metabotropic glutamate receptor 3	Homo sapiens (human)	IC50 (µMol)	0.0279	0.0028	0.4627	1.5000	AID1714560
Metabotropic glutamate receptor 3	Homo sapiens (human)	Ki	0.0939	0.0013	0.6154	9.0000	AID109163; AID109164; AID1247514; AID1468292; AID239379; AID239427; AID275488
Metabotropic glutamate receptor 4	Homo sapiens (human)	Ki	100.0000	0.1600	1.1567	2.4000	AID109341
Glutamate receptor ionotropic, kainate 5	Rattus norvegicus (Norway rat)	IC50 (µMol)	100.0000	0.0070	1.0132	7.0000	AID93553
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Metabotropic glutamate receptor 8	Homo sapiens (human)	EC50 (µMol)	15.9900	0.0230	0.9778	5.1000	AID221697; AID275491; AID748159
Metabotropic glutamate receptor 6	Homo sapiens (human)	EC50 (µMol)	3.1750	0.0550	2.2786	4.9000	AID221690; AID748163
Metabotropic glutamate receptor 2	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0141	0.0006	1.4262	7.7000	AID108838; AID1468324
Metabotropic glutamate receptor 3	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0363	0.0021	1.8909	9.0000	AID109168; AID1468324
Metabotropic glutamate receptor 4	Rattus norvegicus (Norway rat)	EC50 (µMol)	100.0000	0.0090	2.5440	9.4900	AID246705
Metabotropic glutamate receptor 5	Homo sapiens (human)	EC50 (µMol)	100.0000	0.0019	0.6145	4.1000	AID221684
Metabotropic glutamate receptor 1	Homo sapiens (human)	EC50 (µMol)	100.0000	0.2000	4.4100	9.3000	AID221515
Metabotropic glutamate receptor 2	Homo sapiens (human)	EC50 (µMol)	0.0114	0.0006	1.1784	8.5000	AID108337; AID108674; AID108680; AID1247515; AID1247519; AID1468294; AID246230; AID275489
Metabotropic glutamate receptor 7	Homo sapiens (human)	EC50 (µMol)	100.0000	0.1585	0.6692	1.1800	AID221694
Metabotropic glutamate receptor 3	Homo sapiens (human)	EC50 (µMol)	0.0451	0.0021	0.9322	5.1180	AID109151; AID109153; AID1247522; AID1247526; AID1468298; AID246231; AID275490; AID748167
Metabotropic glutamate receptor 4	Homo sapiens (human)	EC50 (µMol)	100.0000	0.0040	1.7193	9.8000	AID221675
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Metabotropic glutamate receptor 8	Homo sapiens (human)	Activity	11.5000	0.4000	1.2000	2.0000	AID107269
Metabotropic glutamate receptor 6	Homo sapiens (human)	Activity	3.0000	0.4000	1.3333	3.0000	AID107091
Metabotropic glutamate receptor 5	Homo sapiens (human)	Activity	100.0000	4.0000	4.5500	5.1000	AID109491
Metabotropic glutamate receptor 1	Homo sapiens (human)	Activity	100.0000	1.0000	1.0000	1.0000	AID108354
Metabotropic glutamate receptor 2	Homo sapiens (human)	Activity	0.0079	0.0006	0.7686	4.0000	AID108669
Metabotropic glutamate receptor 3	Homo sapiens (human)	Activity	0.0210	0.0027	1.6381	9.0000	AID109149
Metabotropic glutamate receptor 4	Homo sapiens (human)	Activity	100.0000	4.0000	4.0000	4.0000	AID109323
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 8	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 8	Homo sapiens (human)
visual perception	Metabotropic glutamate receptor 8	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 8	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 8	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 6	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 6	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 6	Homo sapiens (human)
locomotory behavior	Metabotropic glutamate receptor 6	Homo sapiens (human)
detection of visible light	Metabotropic glutamate receptor 6	Homo sapiens (human)
detection of light stimulus involved in visual perception	Metabotropic glutamate receptor 6	Homo sapiens (human)
retina development in camera-type eye	Metabotropic glutamate receptor 6	Homo sapiens (human)
positive regulation of calcium ion import across plasma membrane	Metabotropic glutamate receptor 6	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 6	Homo sapiens (human)
desensitization of G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of DNA-templated transcription	Metabotropic glutamate receptor 5	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 5	Homo sapiens (human)
learning or memory	Metabotropic glutamate receptor 5	Homo sapiens (human)
learning	Metabotropic glutamate receptor 5	Homo sapiens (human)
locomotory behavior	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of MAPK cascade	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticity	Metabotropic glutamate receptor 5	Homo sapiens (human)
synapse organization	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Metabotropic glutamate receptor 5	Homo sapiens (human)
cognition	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of postsynaptic membrane potential	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 5	Homo sapiens (human)
cellular response to amyloid-beta	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 5	Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmission	Metabotropic glutamate receptor 5	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 1	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 1	Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 1	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 1	Homo sapiens (human)
locomotory behavior	Metabotropic glutamate receptor 1	Homo sapiens (human)
sensory perception of pain	Metabotropic glutamate receptor 1	Homo sapiens (human)
positive regulation of MAPK cascade	Metabotropic glutamate receptor 1	Homo sapiens (human)
regulation of sensory perception of pain	Metabotropic glutamate receptor 1	Homo sapiens (human)
regulation of postsynaptic membrane potential	Metabotropic glutamate receptor 1	Homo sapiens (human)
cellular response to electrical stimulus	Metabotropic glutamate receptor 1	Homo sapiens (human)
L-glutamate import across plasma membrane	Metabotropic glutamate receptor 1	Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 1	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 1	Homo sapiens (human)
negative regulation of adenylate cyclase activity	Metabotropic glutamate receptor 2	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 2	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 2	Homo sapiens (human)
gene expression	Metabotropic glutamate receptor 2	Homo sapiens (human)
glutamate secretion	Metabotropic glutamate receptor 2	Homo sapiens (human)
regulation of glutamate secretion	Metabotropic glutamate receptor 2	Homo sapiens (human)
regulation of dopamine secretion	Metabotropic glutamate receptor 2	Homo sapiens (human)
behavioral response to nicotine	Metabotropic glutamate receptor 2	Homo sapiens (human)
response to cocaine	Metabotropic glutamate receptor 2	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Metabotropic glutamate receptor 2	Homo sapiens (human)
long-term synaptic depression	Metabotropic glutamate receptor 2	Homo sapiens (human)
intracellular glutamate homeostasis	Metabotropic glutamate receptor 2	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Metabotropic glutamate receptor 2	Homo sapiens (human)
regulation of response to drug	Metabotropic glutamate receptor 2	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 2	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 2	Homo sapiens (human)
behavioral fear response	Metabotropic glutamate receptor 7	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 7	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 7	Homo sapiens (human)
sensory perception of sound	Metabotropic glutamate receptor 7	Homo sapiens (human)
negative regulation of glutamate secretion	Metabotropic glutamate receptor 7	Homo sapiens (human)
axon development	Metabotropic glutamate receptor 7	Homo sapiens (human)
glycosylation	Metabotropic glutamate receptor 7	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 7	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 7	Homo sapiens (human)
negative regulation of adenylate cyclase activity	Metabotropic glutamate receptor 3	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 3	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 3	Homo sapiens (human)
gene expression	Metabotropic glutamate receptor 3	Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmission	Metabotropic glutamate receptor 3	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 3	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 3	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 4	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 4	Homo sapiens (human)
neurotransmitter secretion	Metabotropic glutamate receptor 4	Homo sapiens (human)
positive regulation of MAPK cascade	Metabotropic glutamate receptor 4	Homo sapiens (human)
regulation of neuron apoptotic process	Metabotropic glutamate receptor 4	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 4	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor activity	Metabotropic glutamate receptor 8	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 8	Homo sapiens (human)
group III metabotropic glutamate receptor activity	Metabotropic glutamate receptor 8	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 6	Homo sapiens (human)
protein binding	Metabotropic glutamate receptor 6	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 6	Homo sapiens (human)
protein homodimerization activity	Metabotropic glutamate receptor 6	Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activity	Metabotropic glutamate receptor 6	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 5	Homo sapiens (human)
protein binding	Metabotropic glutamate receptor 5	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 5	Homo sapiens (human)
protein tyrosine kinase activator activity	Metabotropic glutamate receptor 5	Homo sapiens (human)
A2A adenosine receptor binding	Metabotropic glutamate receptor 5	Homo sapiens (human)
identical protein binding	Metabotropic glutamate receptor 5	Homo sapiens (human)
protein tyrosine kinase binding	Metabotropic glutamate receptor 5	Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activity	Metabotropic glutamate receptor 5	Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 5	Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potential	Metabotropic glutamate receptor 5	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 1	Homo sapiens (human)
protein binding	Metabotropic glutamate receptor 1	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 1	Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activity	Metabotropic glutamate receptor 1	Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potential	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 2	Homo sapiens (human)
calcium channel regulator activity	Metabotropic glutamate receptor 2	Homo sapiens (human)
protein binding	Metabotropic glutamate receptor 2	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 2	Homo sapiens (human)
scaffold protein binding	Metabotropic glutamate receptor 2	Homo sapiens (human)
group II metabotropic glutamate receptor activity	Metabotropic glutamate receptor 2	Homo sapiens (human)
group III metabotropic glutamate receptor activity	Metabotropic glutamate receptor 7	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 7	Homo sapiens (human)
adenylate cyclase inhibitor activity	Metabotropic glutamate receptor 7	Homo sapiens (human)
protein dimerization activity	Metabotropic glutamate receptor 7	Homo sapiens (human)
serine binding	Metabotropic glutamate receptor 7	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 3	Homo sapiens (human)
calcium channel regulator activity	Metabotropic glutamate receptor 3	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 3	Homo sapiens (human)
scaffold protein binding	Metabotropic glutamate receptor 3	Homo sapiens (human)
group II metabotropic glutamate receptor activity	Metabotropic glutamate receptor 3	Homo sapiens (human)
G protein-coupled receptor activity	Metabotropic glutamate receptor 4	Homo sapiens (human)
glutamate receptor activity	Metabotropic glutamate receptor 4	Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activity	Metabotropic glutamate receptor 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Metabotropic glutamate receptor 8	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 8	Homo sapiens (human)
Golgi membrane	Metabotropic glutamate receptor 6	Homo sapiens (human)
endoplasmic reticulum membrane	Metabotropic glutamate receptor 6	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 6	Homo sapiens (human)
dendrite	Metabotropic glutamate receptor 6	Homo sapiens (human)
new growing cell tip	Metabotropic glutamate receptor 6	Homo sapiens (human)
synapse	Metabotropic glutamate receptor 6	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 6	Homo sapiens (human)
plasma membrane	Glutamate receptor 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor 2	Rattus norvegicus (Norway rat)
plasma membrane	Metabotropic glutamate receptor 1	Rattus norvegicus (Norway rat)
plasma membrane	Metabotropic glutamate receptor 4	Rattus norvegicus (Norway rat)
dendrite	Metabotropic glutamate receptor 5	Homo sapiens (human)
cytoplasm	Metabotropic glutamate receptor 5	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
dendritic spine	Metabotropic glutamate receptor 5	Homo sapiens (human)
dendritic shaft	Metabotropic glutamate receptor 5	Homo sapiens (human)
astrocyte projection	Metabotropic glutamate receptor 5	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Metabotropic glutamate receptor 5	Homo sapiens (human)
glutamatergic synapse	Metabotropic glutamate receptor 5	Homo sapiens (human)
postsynaptic density membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
nucleus	Metabotropic glutamate receptor 1	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 1	Homo sapiens (human)
dendrite	Metabotropic glutamate receptor 1	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Metabotropic glutamate receptor 1	Homo sapiens (human)
glutamatergic synapse	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled receptor dimeric complex	Metabotropic glutamate receptor 1	Homo sapiens (human)
G protein-coupled receptor homodimeric complex	Metabotropic glutamate receptor 1	Homo sapiens (human)
postsynaptic density membrane	Metabotropic glutamate receptor 1	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 1	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 2	Homo sapiens (human)
axon	Metabotropic glutamate receptor 2	Homo sapiens (human)
dendrite	Metabotropic glutamate receptor 2	Homo sapiens (human)
presynaptic membrane	Metabotropic glutamate receptor 2	Homo sapiens (human)
astrocyte projection	Metabotropic glutamate receptor 2	Homo sapiens (human)
glutamatergic synapse	Metabotropic glutamate receptor 2	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 2	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 7	Homo sapiens (human)
cell cortex	Metabotropic glutamate receptor 7	Homo sapiens (human)
membrane	Metabotropic glutamate receptor 7	Homo sapiens (human)
axon	Metabotropic glutamate receptor 7	Homo sapiens (human)
dendrite	Metabotropic glutamate receptor 7	Homo sapiens (human)
asymmetric synapse	Metabotropic glutamate receptor 7	Homo sapiens (human)
dendritic shaft	Metabotropic glutamate receptor 7	Homo sapiens (human)
postsynaptic membrane	Metabotropic glutamate receptor 7	Homo sapiens (human)
presynaptic active zone	Metabotropic glutamate receptor 7	Homo sapiens (human)
receptor complex	Metabotropic glutamate receptor 7	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 7	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 3	Homo sapiens (human)
postsynaptic density	Metabotropic glutamate receptor 3	Homo sapiens (human)
axon	Metabotropic glutamate receptor 3	Homo sapiens (human)
presynaptic membrane	Metabotropic glutamate receptor 3	Homo sapiens (human)
dendritic spine	Metabotropic glutamate receptor 3	Homo sapiens (human)
postsynaptic membrane	Metabotropic glutamate receptor 3	Homo sapiens (human)
astrocyte projection	Metabotropic glutamate receptor 3	Homo sapiens (human)
glutamatergic synapse	Metabotropic glutamate receptor 3	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 3	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 4	Homo sapiens (human)
cytoplasmic vesicle	Metabotropic glutamate receptor 4	Homo sapiens (human)
presynapse	Metabotropic glutamate receptor 4	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID196702	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 100 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108489	Agonist potency against cloned human metabotropic glutamate receptor 1	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID1468291	Displacement of [3H]-LY459477 from recombinant human mGlu2 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID275487	Displacement of [3H]LY341495 from human recombinant mGluR2 in RGT cells	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID196703	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 1000 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID246231	Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
AID114061	Oral effective dose evaluated in mice by mouse limbic seizure assay	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID248994	Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into chinese hamster ovary cells transfected with human PepT1 (CHO/hPepT1) done for 5-20 min at 37 degree C with compound	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID1714559	Agonist activity at mGlu2 (unknown origin)	2016	Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24	Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
AID196230	Compound was evaluated by measuring the ability to influence stimulated basal [3H]-IP formation in adult rat cerebral cortical slices.	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID1247513	Displacement of [3H]-459477 from human recombinant mGlu2 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID1468325	Agonist activity at mGlu2/3 receptor in Sprague-Dawley rat forebrain assessed as inhibition of spontaneous Ca2+ oscillations in cortical neurons after 300 secs by FLIPR assay relative to vehicle control	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID109149	Inhibition of c-AMP by human Metabotropic glutamate receptor 3 (mGluR3) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID275494	Agonist activity at human mGluR4a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID275495	Agonist activity at human mGluR7a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID239426	Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 2	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
AID92500	Inhibitory concentration against radioligand [3H]AMPA binding to Ionotropic glutamate receptor AMPA in rat forebrain membranes	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID109153	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID1714560	Agonist activity at mGlu3 (unknown origin)	2016	Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24	Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
AID75030	Inhibitory concentration against ACPD-sensitive radioligand [3H]glutamate binding to Group II Metabotropic glutamate receptor in rat forebrain membranes	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID109328	Agonistic activity against Human Metabotropic glutamate receptor 4; not active	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID748159	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID1247527	Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay relative to glutamate	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID1247522	Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID248675	Inhibition of radiolabeled glycylsarcosine (Gly-Sar) uptake into Caco-2 cells done for 15 min at 37 degree C with compound	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID108999	Antagonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid; NT is Not Tested.	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109164	Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID107091	Inhibition of c-AMP by human Metabotropic glutamate receptor 6 (mGluR6) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID1468293	Selectivity ratio of Ki for recombinant human mGlu2 receptor to Ki for recombinant human mGlu3 receptor	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID192828	Tested for % inhibition of PCP induced hyperactivity in rats at 10 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID231225	Potency at metabotropic glutamate receptor 4, measured as the ratio of EC50 to IC50	2002	Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15	Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID748162	Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay relative to LAP4	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID1468292	Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID221694	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR7	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID239378	Inhibition of [3H]LY-341,495 binding to recombinant human mGlu2 receptors	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID113871	Intraperitoneal effective dose evaluated in mice by mouse limbic seizure assay	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID275489	Agonist activity at human mGluR2 assessed as effect on cAMP production in RGT cells	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID748163	Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID108838	Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID1247519	Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID349585	Antipsychotic activity in sc dosed mouse assessed as attenuation of methamphetamine-induced hyperlocomotor activity after 2 hrs	2009	Bioorganic & medicinal chemistry letters, May-01, Volume: 19, Issue:9	3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
AID275499	Antagonist activity against human mGluR7a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID275488	Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID231223	Potency at metabotropic glutamate receptor 1, measured as the ratio of EC50 to IC50	2002	Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15	Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID275497	Antagonist activity against human mGluR5a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID221515	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR1a	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID239082	Inhibition of [3H]LY-341,495 binding to mGlu2 receptors of rat brain	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID196231	Compound was evaluated by measuring the ability to influence stimulated basal [3H]IP formation in adult rat cerebral cortical slices; Not tested	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID108354	Phosphoinositide hydrolysis by human Metabotropic glutamate receptor 1 (mGluR1) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID108829	Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 2 subtypes expressed in RGT cells.	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID107256	Inhibition of c-AMP by human Metabotropic glutamate receptor 7 (mGluR7) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID231224	Potency at metabotropic glutamate receptor 2, measured as the ratio of EC50 to IC50	2002	Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15	Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID1468303	Selectivity ratio of EC50 for recombinant human mGlu2 receptor to EC50 for recombinant human mGlu3 receptor	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID1468295	Agonist activity at human mGlu2 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay relative to glutamate	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID1468294	Agonist activity at human mGlu2 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID108996	Tested for binding affinity against Metabotropic glutamate receptor 2 in CHO cells using [3H]-7 as radioligand	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID748166	Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay relative to glutamate	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID196228	Compound was evaluated by measuring the ability to influence forskolin-stimulated cAMP formation in adult rat cerebral cortical slices	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID748167	Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID93721	Inhibitory concentration against radioligand [3H]-Kainate binding to Ionotropic glutamate receptor kainate in rat forebrain membranes	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID93553	Ability to displace [3H]-KA binding to Ionotropic glutamate receptor kainate from rat forebrain	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID107261	Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID114065	Oral effective dose was evaluated in mice by automated elevated plus-maze assay	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID1468299	Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay relative to glutamate	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID748169	Antagonist activity at human mGlu2 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID108837	Binding affinity at Metabotropic glutamate receptor 2	2002	Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15	Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID239427	Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
AID144908	Inhibitory concentration against radioligand [3H]CGS-19,755 binding to N-methyl-D-aspartate glutamate receptor in rat forebrain membranes	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID1247526	Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID1468323	Displacement of [3H]-LY459477 from mGlu2/3 receptor in Sprague-Dawley rat forebrain primary cortical membranes after 90 mins by liquid scintillation counting	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID75021	The effective concentration for 50% glutamate response was measured on Group II Metabotropic glutamate receptor	1999	Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15	Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity.
AID108337	Compound was evaluated for agonist activity against human mGluR2	1998	Bioorganic & medicinal chemistry letters, Apr-21, Volume: 8, Issue:8	Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.
AID275493	Agonist activity at human mGluR5a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID108674	Agonistic activity against Human Metabotropic glutamate receptor 2	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID221690	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID108830	Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID246705	Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Virtual screening workflow development guided by the "receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.
AID192830	Tested for % inhibition of PCP induced hyperactivity in rats at 30 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID109312	Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID1247515	Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID108669	Inhibition of c-AMP by human Metabotropic glutamate receptor 2 (mGluR2) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID275491	Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID221675	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID1468324	Agonist activity at mGlu2/3 receptor in Sprague-Dawley rat forebrain assessed as inhibition of spontaneous Ca2+ oscillations in cortical neurons after 300 secs by FLIPR assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID109163	Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells.	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID221684	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR5a	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID176194	Effective dose to evaluate PCP induced hyper activity in rats after oral administration	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID251152	Duration of suppression of compound in rat fear-potentiated startle assay at an oral dose of 3.0 mg/kg; Range = 8-24 h	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID108484	Agonistic activity against Human Metabotropic glutamate receptor 1 at 1 uM concentration; no inhibition	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID108680	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 2	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID192824	Tested for % inhibition of PCP induced head-weavings in rats at 300 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID89944	Mean effective dose that significantly blocked fear-potentiated startle(oral administhumanion)	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID109151	Agonistic activity against Human Metabotropic glutamate receptor 3	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID246230	Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu2 receptor	2005	Journal of medicinal chemistry, May-19, Volume: 48, Issue:10	Methyl substitution of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate (LY354740) determines functional activity at metabotropic glutamate receptors: identification of a subtype selective mGlu2 receptor agonist.
AID109168	Agonist potency against cloned Metabotropic glutamate receptor 3	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID221697	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID75015	The effective concentration for 50% glutamate response was measured on Group I Metabotropic glutamate receptor	1999	Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15	Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity.
AID109491	Phosphoinositide hydrolysis by human Metabotropic glutamate receptor 5 (mGluR5) expressed in non neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID176193	Effective dose to evaluate PCP induced head-weaving behavior in rats after oral administration	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID108985	Ratio between EC50 of compound and glutamate measured against Metabotropic glutamate receptor 2	1999	Journal of medicinal chemistry, May-06, Volume: 42, Issue:9	Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID192823	Tested for % inhibition of PCP induced head-weavings in rats at 1000 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID92213	Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand.	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID109323	Inhibition of c-AMP by human Metabotropic glutamate receptor 4 (mGluR4) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID275492	Agonist activity at human mGluR1a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID249393	Onset of suppression of startle of compound in rat fear-potentiated startle assay at an oral dose of 3.0 mg/kg	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID275490	Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID192822	Tested for % inhibition of PCP induced head-weavings in rats at 100 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID1247514	Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID107093	Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID196695	Tested for % inhibition of PCP induced head-weavings in rats at 10000 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID107058	Agonistic activity against Human Metabotropic glutamate receptor 5 at 1 uM concentration; no inhibition	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID748168	Antagonist activity at human mGlu2 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay relative to control	2013	Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11	Synthesis and pharmacological characterization of 4-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates: identification of new potent and selective metabotropic glutamate 2/3 receptor agonists.
AID109315	Antagonist activity against Metabotropic glutamate receptor 3 expressed in CHO cells was evaluated in presence of 30 uM glutamic acid; NT is Not Tested.	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID275496	Antagonist activity against human mGluR1a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID113873	Intraperitoneal effective dose was evaluated in mice by automated elevated plus-maze assay	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic pr
AID239379	Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID109341	Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID196704	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 10000 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID107259	Agonistic activity against Human Metabotropic glutamate receptor 7; not active	1998	Journal of medicinal chemistry, May-07, Volume: 41, Issue:10	Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID107059	Agonist potency against cloned metabotropic glutamate receptor 5	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID1247523	Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay relative to glutamate	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID107274	Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).	2000	Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14	Ligands for glutamate receptors: design and therapeutic prospects.
AID1247516	Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay relative to glutamate	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID1468298	Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay	2018	Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6	Synthesis and Pharmacological Characterization of C4
AID1247520	Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay relative to glutamate	2015	Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18	Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812
AID75022	Ability to displace [3H]LY-341,495 binding to Group II Metabotropic glutamate receptor from rat forebrain	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID275498	Antagonist activity against human mGluR4a assessed as effect on cAMP production in RGT cells upto 100 uM	2007	Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2	Synthesis and metabotropic glutamate receptor activity of S-oxidized variants of (-)-4-amino-2-thiabicyclo-[3.1.0]hexane-4,6-dicarboxylate: identification of potent, selective, and orally bioavailable agonists for mGlu2/3 receptors.
AID196701	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 10 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID244784	Minimally effective dose for suppression of startle in rat fear-potentiated startle assay, p.o.; Range = 0.3-3.0 mg/kg	2005	Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16	Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.
AID143153	Ability to displace [3H]CGP-39653 binding to N-methyl-D-aspartate glutamate receptor from rat forebrain	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID108514	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.	1999	Journal of medicinal chemistry, May-06, Volume: 42, Issue:9	Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID107269	Inhibition of c-AMP by human Metabotropic glutamate receptor 8 (mGluR8) expressed in non-neuronal cells	2002	Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17	(2S,1'S,2'S,3'R)-2-(2'-carboxy-3'-methylcyclopropyl) glycine is a potent and selective metabotropic group 2 receptor agonist with anxiolytic properties.
AID196706	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 30 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID196707	Tested for mGluR agonist activity by measuring the PCP induced hyperactivity in rats at 300 mg/kg	2000	Journal of medicinal chemistry, Dec-14, Volume: 43, Issue:25	Synthesis, SARs, and pharmacological characterization of 2-amino-3 or 6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent, selective, and orally active group II metabotropic glutamate receptor agonists.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346271	Human mGlu2 receptor (Metabotropic glutamate receptors)	1999	Neuropharmacology, Oct, Volume: 38, Issue:10	[3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells.
AID1346272	Human mGlu6 receptor (Metabotropic glutamate receptors)	1999	Journal of medicinal chemistry, Mar-25, Volume: 42, Issue:6	Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists f
AID1346287	Rat mGlu2 receptor (Metabotropic glutamate receptors)	2000	Neuropharmacology, Jul-24, Volume: 39, Issue:10	Characterization of [(3)H]-LY354740 binding to rat mGlu2 and mGlu3 receptors expressed in CHO cells using semliki forest virus vectors.
AID1346287	Rat mGlu2 receptor (Metabotropic glutamate receptors)	1998	British journal of pharmacology, Feb, Volume: 123, Issue:3	Characterization of [3H]-(2S,2'R,3'R)-2-(2',3'-dicarboxy-cyclopropyl)glycine ([3H]-DCG IV) binding to metabotropic mGlu2 receptor-transfected cell membranes.
AID1346282	Human mGlu8 receptor (Metabotropic glutamate receptors)	1999	Brain research. Molecular brain research, Apr-20, Volume: 67, Issue:2	Cloning and functional expression of alternative spliced variants of the human metabotropic glutamate receptor 8.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	36 (19.15)	18.2507
2000's	99 (52.66)	29.6817
2010's	44 (23.40)	24.3611
2020's	9 (4.79)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	5 (2.63%)	5.53%
Reviews	11 (5.79%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	174 (91.58%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.	2.44	2	0	amino acid zwitterion; gamma-amino acid; monocarboxylic acid	human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule
carbamates [no description available]	3.16	1	0	amino-acid anion
choline [no description available]	2.03	1	0	cholines	allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter; nutrient; plant metabolite; Saccharomyces cerevisiae metabolite
chlorine chloride : A halide anion formed when chlorine picks up an electron to form an an anion.	2.7	3	0	halide anion; monoatomic chlorine	cofactor; Escherichia coli metabolite; human metabolite
lactic acid Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.	2	1	0	2-hydroxy monocarboxylic acid	algal metabolite; Daphnia magna metabolite
glycine [no description available]	4.97	12	0	alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid	EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical
taurine [no description available]	2.08	1	0	amino sulfonic acid; zwitterion	antioxidant; Escherichia coli metabolite; glycine receptor agonist; human metabolite; mouse metabolite; nutrient; radical scavenger; Saccharomyces cerevisiae metabolite
urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.	2.06	1	0	isourea; monocarboxylic acid amide; one-carbon compound	Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.	3.52	2	0	non-proteinogenic alpha-amino acid	NMDA receptor antagonist
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid alpha-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.	2.7	3	0	non-proteinogenic alpha-amino acid
alpha-methyl-4-carboxyphenylglycine [no description available]	3.1	1	0
sk&f 82958 [no description available]	2.01	1	0	benzazepine
4-iodo-2,5-dimethoxyphenylisopropylamine 4-iodo-2,5-dimethoxyphenylisopropylamine: RN given refers to unlabeled parent cpd without isomeric designation; a serotonin agonist. 2-(4-iodo-2,5-dimethoxyphenyl)-1-methylethylamine : An organoiodine compound that is amphetamine bearing two methoxy substituents at positions 2 and 5 as well as an iodo substituent at position 4.	3.11	5	0	amphetamines; dimethoxybenzene; organoiodine compound
ibotenic acid Ibotenic Acid: A neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist.	3.1	1	0	non-proteinogenic alpha-amino acid	neurotoxin
(alpha-carboxycyclopropyl)glycine (alpha-carboxycyclopropyl)glycine: structure given in first source; glutamate receptor agonist	2	1	0	alpha-amino acid
4-carboxy-3-hydroxyphenylglycine 4-carboxy-3-hydroxyphenylglycine: weak agonist at metabotropic glutamate receptors; occludes the action of 1-aminocyclopentyl-1,3-dicarboxylate in hippocampus	3.5	2	0	hydroxybenzoic acid
1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine: A dopaminergic neurotoxic compound which produces irreversible clinical, chemical, and pathological alterations that mimic those found in Parkinson disease.. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine : A tetrahydropyridine that is 1,2,3,6-tetrahydropyridine substituted by a methyl group at position 1 and a phenyl group at position 4.	2.31	1	0	methylpyridines; phenylpyridine; tetrahydropyridine	neurotoxin
1-aminoindan-1,5-dicarboxylic acid 1-aminoindan-1,5-dicarboxylic acid: structure given in first source	3.1	1	0
alprazolam Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.	2	1	0	organochlorine compound; triazolobenzodiazepine	anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic
amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source	2.25	1	0	adamantanes; primary aliphatic amine	analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic
2-amino-4-phosphonobutyric acid 2-amino-4-phosphonobutyric acid: glutamate antagonist in locust muscle; structure; do not confuse with L-AP4, which is the propionic acid version	3.11	5	0
baclofen [no description available]	2.13	1	0	amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound	central nervous system depressant; GABA agonist; muscle relaxant
buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.	2.42	2	0	azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines	anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist
chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.	2.41	2	0	benzodiazepine
citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.	2.02	1	0	2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound
clobazam Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.	2.01	1	0	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; GABA modulator
cycloleucine Cycloleucine: An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.. 1-aminocyclopentanecarboxylic acid : A non-proteinogenic alpha-amino acid that is cyclopentane substituted at position 1 by amino and carboxy groups.	2.69	3	0	non-proteinogenic alpha-amino acid	EC 2.5.1.6 (methionine adenosyltransferase) inhibitor
amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.	2.99	4	0	primary amine
diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.	3.11	5	0	1,4-benzodiazepinone; organochlorine compound	anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic
domperidone Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.	2.74	3	0	benzimidazoles; heteroarylpiperidine	antiemetic; dopaminergic antagonist
fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.	2	1	0	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic
flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.	2.41	2	0	ethyl ester; imidazobenzodiazepine; organofluorine compound	antidote to benzodiazepine poisoning; GABA antagonist
gabapentin Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.	2.03	1	0	gamma-amino acid	anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	3.28	6	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
hexobarbital Hexobarbital: A barbiturate that is effective as a hypnotic and sedative.. hexobarbital : A member of the class of barbiturates taht is barbituric acid substituted at N-1 by methyl and at C-5 by methyl and cyclohex-1-enyl groups.	1.99	1	0	barbiturates
ifenprodil ifenprodil: NMDA receptor antagonist	2.03	1	0	piperidines
ketamine 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.. ketamine : 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.	4.14	3	1	cyclohexanones; monochlorobenzenes; secondary amino compound	analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic
memantine [no description available]	2.44	2	0	adamantanes; primary aliphatic amine	antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist
oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.	2.01	1	0	1,4-benzodiazepinone; organochlorine compound	anxiolytic drug; environmental contaminant; xenobiotic
oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).	2.25	1	0	benzenetriol; catecholamine; primary amino compound	drug metabolite; human metabolite; neurotoxin
sulpiride Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine.	2.01	1	0	benzamides; N-alkylpyrrolidine; sulfonamide	antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist
4-methylglutamic acid 4-methylglutamic acid : A glutamic acid derivative that is glutamic acid substituted by a methyl group at position 4.	2	1	0	amino dicarboxylic acid; glutamic acid derivative
xanthurenic acid xanthurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by hydroxy groups at C-4 and C-8.	2.08	1	0	dihydroxyquinoline; quinolinemonocarboxylic acid	animal metabolite; iron chelator; metabotropic glutamate receptor agonist; vesicular glutamate transport inhibitor
zinc chloride zinc chloride: RN given refers to parent cpd. zinc dichloride : A compound of zinc and chloride ions in the ratio 1:2. It exists in four crystalline forms, in each of which the Zn(2+) ions are trigonal planar coordinated to four chloride ions.	2.42	2	0	inorganic chloride; zinc molecular entity	astringent; disinfectant; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; Lewis acid
corticosterone [no description available]	2.41	2	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.	2.43	2	0	1-phenylpropan-2-amine	adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent
aldosterone [no description available]	2.1	1	0	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite
pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.	2.03	1	0	pilocarpine	antiglaucoma drug
pentylenetetrazole Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.	2	1	0	organic heterobicyclic compound; organonitrogen heterocyclic compound
alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2.	6.02	8	1	alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid	EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite
aspartic acid 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.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.	1.99	1	0	aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; mouse metabolite; neurotransmitter
levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease	2.84	3	0	amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid	allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug
valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.	2.13	1	0	L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
cyclopropane cyclopropane : A cycloalkane composed of three carbon atoms to form a ring.	2.02	1	0	cycloalkane; cyclopropanes	inhalation anaesthetic
phencyclidine 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.. phencyclidine : 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.	4.82	10	0	benzenes; piperidines	anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	2.93	4	0	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
xanthenes Xanthenes: Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.	4.43	21	0	xanthene
cyclohexanol Cyclohexanols: Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.. cyclohexanols : An alcohol in which one or more hydroxy groups are attached to a cyclohexane skeleton.	2.06	1	0	cyclohexanols; secondary alcohol	solvent
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	2	1	0	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
cyclopentane Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.	2.46	2	0	cycloalkane; cyclopentanes; volatile organic compound	non-polar solvent
thiazoles [no description available]	2.77	3	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
bicuculline Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.. bicuculline : A benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species.	2.03	1	0	benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines	agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin
kainic acid Kainic 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.	3.27	6	0	dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid	antinematodal drug; excitatory amino acid agonist
methoxyhydroxyphenylglycol Methoxyhydroxyphenylglycol: Synthesized from endogenous epinephrine and norepinephrine in vivo. It is found in brain, blood, CSF, and urine, where its concentrations are used to measure catecholamine turnover.	2.44	2	0	methoxybenzenes; phenols
cyclopentenone 2-cyclopenten-1-one : An enone that is cyclopentanone having a C=C double bond at position 2.	2.02	1	0	alicyclic ketone; enone	Hsp70 inducer
allylglycine Allylglycine: An inhibitor of glutamate decarboxylase and an antagonist of GAMMA-AMINOBUTYRIC ACID. It is used to induce convulsions in experimental animals.	2	1	0
n-methylaspartate N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration.	4.71	9	0	amino dicarboxylic acid; D-alpha-amino acid; D-aspartic acid derivative; secondary amino compound	neurotransmitter agent
d-glutamate [no description available]	2.02	1	0	D-alpha-amino acid; glutamic acid	Escherichia coli metabolite; mouse metabolite
dihydro-beta-erythroidine Dihydro-beta-Erythroidine: Dihydro analog of beta-erythroidine, which is isolated from the seeds and other plant parts of Erythrina sp. Leguminosae. It is an alkaloid with curarimimetic properties.. dihydro-beta-erythroidine : An organic heterotetracyclic compound resulting from the partial hydrogenation of the 1,3-diene moiety of beta-erythroidine to give the corresponding 2-ene.	2.01	1	0	delta-lactone; organic heterotetracyclic compound; tertiary amino compound	nicotinic antagonist
glutamic acid 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 : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.	6.38	30	0	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical
quisqualic acid Quisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.	4.2	5	0	non-proteinogenic alpha-amino acid
paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.	3.41	1	1	aromatic ether; benzodioxoles; organofluorine compound; piperidines	antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor
colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.	2.91	4	0	acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol	adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist
eticlopride eticlopride: blocks dopamine-D2 binding sites; structure given in first source; RN given refers to (S)-isomer	2.01	1	0	salicylamides
venlafaxine hydrochloride Venlafaxine Hydrochloride: A cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT.	2.06	1	0	hydrochloride
glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.	2.31	1	0	D-glucopyranose	epitope; mouse metabolite
cholesteryl succinate cholesteryl succinate: RN given refers to (3beta)-isomer. cholesteryl hemisuccinate : A dicarboxylic acid monoester resulting from the formal condensation of the hydroxy group of cholesterol with one of the carboxy groups of succinic acid. A detergent that is often used to replace cholesterol in protein crystallography, biochemical studies of proteins, and pharmacology.	2.31	1	0	cholestane ester; dicarboxylic acid monoester; hemisuccinate	detergent
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.02	1	0	1,2,3-triazole
plasmenylserine plasmenylserine: RN given refers to (L)-isomer. O-phospho-L-serine : The L-enantiomer of O-phosphoserine.. O-phosphoserine : A serine derivative that is serine substituted at the oxygen atom by a phosphono group.	2.41	2	0	O-phosphoserine	EC 1.4.7.1 [glutamate synthase (ferredoxin)] inhibitor; EC 2.5.1.49 (O-acetylhomoserine aminocarboxypropyltransferase) inhibitor; EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
D-serine [no description available]	3.1	1	0	D-alpha-amino acid; serine zwitterion; serine	Escherichia coli metabolite; human metabolite; NMDA receptor agonist
acamprosate Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3.	2.08	1	0	acetamides; organosulfonic acid	environmental contaminant; neurotransmitter agent; xenobiotic
1-amino-1,3-dicarboxycyclopentane, (trans)-isomer [no description available]	2.4	2	0
d-aspartic acid [no description available]	2.1	1	0	aspartic acid; D-alpha-amino acid	mouse metabolite
nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.	2.42	2	0	3-(1-methylpyrrolidin-2-yl)pyridine	anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic
3,4-dihydroxyphenylglycol 3,4-dihydroxyphenylglycol: noradrenaline metabolite in mouse brain; RN given refers to cpd without isomeric designation. 3,4-dihydroxyphenylethyleneglycol : A tetrol composed of ethyleneglycol having a 3,4-dihydroxyphenyl group at the 1-position.	2.44	2	0	catechols; tetrol	metabolite; mouse metabolite
L-2-aminoadipic acid L-2-aminoadipic acid : The L-enantiomer of 2-aminoadipic acid.	3.1	1	0	2-aminoadipic acid	Escherichia coli metabolite; human metabolite
glycylsarcosine glycylsarcosine : A dipeptide obtained by formal condensation of the carboxy group of glycine with the amino group of sarcosine.	2.05	1	0	dipeptide zwitterion; dipeptide
isovaline isovaline: RN given refers to parent cpd(L)-isomer	2.13	1	0
2-methylglutamic acid 2-methylglutamic acid: RN given refers to parent cpd without isomeric designation	2	1	0
sym 2081 [no description available]	2	1	0
4-methyleneglutamic acid 4-methyleneglutamic acid: RN given refers to (DL-Glu)-isomer	2	1	0	non-proteinogenic alpha-amino acid
diosgenin [no description available]	2.31	1	0	3beta-sterol; hexacyclic triterpenoid; sapogenin; spiroketal	antineoplastic agent; antiviral agent; apoptosis inducer; metabolite
1-amino-1,3-dicarboxycyclopentane 1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer	4.89	11	0
sr 95531 [no description available]	2.03	1	0	methoxybenzenes
3,5-dihydroxyphenylglycine 3,5-dihydroxyphenylglycine: a potent agonst of metabotropic glutamate receptors	2.69	3	0	alpha-amino acid
dodecyl-beta-d-maltoside dodecyl beta-D-maltoside : A glycoside resulting from attachment of a dodecyl group to the reducing-end anomeric centre of a beta-maltose molecule.	2.31	1	0	disaccharide derivative; glycoside	detergent
2-(2,3-dicarboxycyclopropyl)glycine [no description available]	2.91	4	0
azetidine-2,4-dicarboxylic acid azetidine-2,4-dicarboxylic acid: activates neuronal metabotropic receptors; RN given refers to (trans-isomer); RN for cpd without isomeric designation not avail 10/93	2.4	2	0
ly 293558 tezampanel: structure given in first source; an AMPA receptor antagonist	2	1	0
d-apv [no description available]	3.1	1	0
homocysteic acid homocysteic acid: promotes growth in hypophysectomized rats; RN given refers to parent cpd. homocysteic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group has benn oxidised to the corresponding sulfonic acid.. L-homocysteic acid : A homocysteic acid with L-configuration.	2.02	1	0	homocysteic acid	NMDA receptor agonist
2-amino-4-phosphonobutyric acid (2S)-2-amino-4-phosphonobutanoic acid : A non-proteinogenc L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. It is a potent and selective agonist for the group III metabotropic glutamate receptors (mGluR4/6/7/8).	4.02	4	0	non-proteinogenic L-alpha-amino acid; phosphonic acids	metabotropic glutamate receptor agonist
dizocilpine [no description available]	1.99	1	0	secondary amino compound; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
isospaglumic acid isospaglumic acid: mediator in the sensitivity of animals to hyperbaric oxygenation; Naaxia is the tradename; apparently can have both a neuroprotective and a neurotoxic effect. Ac-Asp-Glu : A dipeptide composed of N-acetyl-L-aspartic acid and L-glutamic acid joined by a peptide linkage.	2.45	2	0	dipeptide	human metabolite
1-oxoisoindole 1-oxoisoindole: structure	3.16	1	0
3,5-dihydroxyphenylglycine (S)-3,5-dihydroxyphenylglycine : A glycine derivative that is L-alpha-phenylglycine substituted at positions 3 and 5 on the phenyl ring by hydroxy groups.	4.2	5	0	amino acid zwitterion; non-proteinogenic L-alpha-amino acid; resorcinols
cocaine Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.	2	1	0	benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid	adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic
alpha-methyl-4-carboxyphenylglycine alpha-methyl-4-carboxyphenylglycine: glutamate receptor antagonist. (S)-alpha-methyl-4-carboxyphenylglycine : A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist.	3.1	5	0	non-proteinogenic alpha-amino acid	metabotropic glutamate receptor antagonist
tetragastrin Tetragastrin: L-Tryptophyl-L-methionyl-L-aspartyl-L-phenylalaninamide. The C-terminal tetrapeptide of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin.. tetragastrin : A tetrapeptide composed of L-tryptophan, L-methione, L-aspartic acid and L-phenylalaninamide residues joined in sequence.	3.41	1	1	peptidyl amide; tetrapeptide	anxiogenic; human metabolite
adenosine-5'-(n-ethylcarboxamide) Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.	1.99	1	0	adenosines; monocarboxylic acid amide	adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent
6-methyl-2-(phenylethynyl)pyridine 6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist. 2-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.	4.62	8	0	acetylenic compound; methylpyridines	anxiolytic drug; metabotropic glutamate receptor antagonist
raclopride Raclopride: A substituted benzamide that has antipsychotic properties. It is a dopamine D2 receptor (see RECEPTORS, DOPAMINE D2) antagonist.	2.74	3	0	salicylamides
4-methylglutamic acid, threo-(l)-isomer [no description available]	3.5	2	0
2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline: structure given in first source; neuroprotectant for cerebral ischemia; AMPA receptor antagonist	2.69	3	0	naphthalenes; sulfonic acid derivative
2-chloro-5-hydroxyphenylglycine 2-chloro-5-hydroxyphenylglycine: activates mGlu(5) receptors; structure in first source	2	1	0
6-cyano-7-nitroquinoxaline-2,3-dione 6-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.	2	1	0	quinoxaline derivative
fg 9041 FG 9041: structure given in first source	2.43	2	0	quinoxaline derivative
methylserine phosphate [no description available]	1.99	1	0
sib 1757 SIB 1757: a selective mGluR5 antagonist; structure in first source	3.1	1	0
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	2	1	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	3.12	5	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
l-2-(carboxypropyl)glycine [no description available]	4.6	8	0
2-(2,3-dicarboxycyclopropyl)glycine [no description available]	3.39	7	0
2r,4r-4-aminopyrrolidine-2,4-dicarboxylate [no description available]	4.2	5	0	pyrrolidinedicarboxylic acid
upf 596 UPF 596: structure in first source	3.8	3	0
mdl 100907 Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.	2.31	1	0
sib 1893 SIB 1893: a selective mGluR5 antagonist; structure in first source	3.5	2	0
4-carboxy-3-hydroxyphenylglycine [no description available]	2.7	3	0
barium Barium: An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.	1.99	1	0	alkaline earth metal atom; elemental barium
strontium Strontium: An element of the alkaline earth family of metals. It has the atomic symbol Sr, atomic number 38, and atomic weight 87.62.	2.02	1	0	alkaline earth metal atom
naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.	2	1	0	cyclopropanes; morphinane-like compound; organic heteropentacyclic compound	antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic
pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.	2.03	1	0	gamma-amino acid	anticonvulsant; calcium channel blocker
tetrodotoxin Tetrodotoxin: An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.. tetrodotoxin : A quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.	2.72	3	0	azatetracycloalkane; oxatetracycloalkane; quinazoline alkaloid	animal metabolite; bacterial metabolite; marine metabolite; neurotoxin; voltage-gated sodium channel blocker
dizocilpine maleate Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.	3.13	5	0	maleate salt; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
sdz eaa 494 midafotel : A member of the class of piperazines that is piperazine substituted by a carboxy group at position 2R and a (1E)-1-phosphonoprop-1-en-3-yl group at position 4. It is an antagonist of N-methyl-D-aspartate receptors (NMDARs) and was in clinical development by Novartis for the treatment of cognition disorders and brain injuries (now discontinued).	3.1	1	0	monocarboxylic acid; olefinic compound; phosphonic acids; piperazinecarboxylic acid; tertiary amino compound	anticonvulsant; neuroprotective agent; NMDA receptor antagonist
cgp 39653 CGP 39653: NMDA receptor antagonist; structure given in first source	3.1	1	0
1-amino-1,3-dicarboxycyclopentane, cis-(1s,3s)-isomer [no description available]	2.92	4	0
1-aminocyclopentane-1,3,4-tricarboxylic acid 1-aminocyclopentane-1,3,4-tricarboxylic acid: metabolic glutamate receptor (mGluR) antagonist; structure in first source	2.7	3	0
adenosine-3',5'-cyclic phosphorothioate adenosine-3',5'-cyclic phosphorothioate: RP-cAMP-S is a protein kinase A inhibitor; SP-cAMP-S is a protein kinase A agonist. (Sp)-cAMPS : A nucleoside 3',5'-cyclic phosphorothioate having adenine as the nucleobase (the Sp-stereoisomer).. (Rp)-cAMPS : A nucleoside 3',5'-cyclic phosphorothioate having adenine as the nucleobase (the Rp-stereoisomer).	2.02	1	0	nucleoside 3',5'-cyclic phosphorothioate
staurosporine staurosporinium : Conjugate acid of staurosporine.	2.96	4	0	ammonium ion derivative
ly 341495 [no description available]	4.21	5	0	xanthenes
n-(4-(2-methoxyphenoxy)phenyl)-n-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine: a metabotropic glutamate 2 receptor potentiator; structure in first source	2.99	4	0
ly 404039 LY404039 : An organic heterobicyclic compound that is (1S,5R)-2-thiabicyclo[3.1.0]hexane carrying oxo, oxo, amino, carboxy, and carboxy groups at positions 2, 2, 4S, 4S, and 6S, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 mGluR3 (Ki = 149 nM and 92 nM, respectively) and exhibits antipsychotic and anxiolytic efficacy in animal models.	2.03	1	0	bridged compound; dicarboxylic acid; non-proteinogenic amino acid derivative; organic heterobicyclic compound; sulfone	antipsychotic agent; anxiolytic drug; dopamine agonist; metabotropic glutamate receptor agonist
mgs 0028 MGS 0028: a group II mGluR agonist; structure in first source	2.7	3	0
ro 64-6198 Ro 64-6198: an orphanin FQ/nociceptin receptor agonist; structure in first source	2.03	1	0
biphenyl-indanone a biphenyl-indanone A: an mGluR2 agonist; structure in first source	2.52	2	0	biphenyls
cgp 55845a CGP 55845A: GABA-B receptor antagonist; RN refers to cpd with no isomeric designation; CGP 55845 is the (1S,2S)-isomer	2.41	2	0
ly 389795 LY 389795: a group II metabotropic glutamate receptor agonist; structure in first source	4.01	4	0
phenobarbital sodium 2-(phosphonomethyl)pentanedioic acid: an N-acetylated alpha-linked acidic dipeptidase (NAALADase) antagonist	2.06	1	0
ly 379268 LY 379268: group II metabotropic glutamate receptor agonist; structure in first source. LY 379268 : An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia.	5.32	17	0	amino dicarboxylic acid; bridged compound; organic heterobicyclic compound	antipsychotic agent; anxiolytic drug; metabotropic glutamate receptor agonist; neuroprotective agent
gpi 5693 2-(3-mercaptopropyl)pentanedioic acid: inhibits glutamate carboxypeptidase II; structure in first source	2.06	1	0
oxadiazoles Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.	2.05	1	0
ly 341495 LY 341495: structure in first source	4.43	21	0
veratridine Veratridine: A benzoate-cevane found in VERATRUM and Schoenocaulon. It activates SODIUM CHANNELS to stay open longer than normal.	2.4	2	0
n,n'-dibenzhydrylethane-1,2-diamine dihydrochloride N,N'-dibenzhydrylethane-1,2-diamine dihydrochloride: selective metabotropic glutamate receptor 7 agonist; structure in first source. AMN082 dihydrochloride : A hydrochloride obtained by combining N,N'-bis(diphenylmethyl)ethane-1,2-diamine with two molar equivalent of hydrochloric acid.	2.55	2	0	hydrochloride	geroprotector; metabotropic glutamate receptor agonist; neuroprotective agent
zj43 ZJ43: N-acetylaspartylglutamate (NAAG) peptidase inhibitor; structure in first source	2.06	1	0
diosgenin glucoside diosgenin glucoside: RN given refers to (3beta,25R)-isomer; structure given in first source. diosgenin 3-O-beta-D-glucoside : A sterol 3-beta-D-glucoside having diosgenin as the sterol component.	2.31	1	0	hexacyclic triterpenoid; monosaccharide derivative; spiroketal; sterol 3-beta-D-glucoside	metabolite
scopolamine hydrobromide [no description available]	2.05	1	0
3,4-dicarboxyphenylglycine [no description available]	2.02	1	0
picrotoxin Picrotoxin: A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.. picrotoxin : A mixture consisting of equimolar amounts of picrotoxinin and picrotin found in the climbing plant Anamirta cocculus.	2	1	0
glycolipids [no description available]	2.31	1	0
piperidines Piperidines: A family of hexahydropyridines.	3.13	5	0
omega-agatoxin iva omega-Agatoxin IVA: A neuropeptide toxin from the venom of the funnel web spider, Agelenopsis aperta. It inhibits CALCIUM CHANNELS, P-TYPE by altering the voltage-dependent gating so that very large depolarizations are needed for channel opening. It also inhibits CALCIUM CHANNELS, Q-TYPE.	2.03	1	0
ly 2140023 LY 2140023: prodrug of LY-404039	2.05	1	0
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	2.06	1	0
amyloid beta-peptides amyloid beta-protein (1-40): although acutely neurotoxic in both rat & monkey cerebral cortex, neuronal degeneration in primates resembles more closely to that found in Alzheimer's disease; amino acid sequence has been determined	2.05	1	0
guanosine 5'-o-(3-thiotriphosphate) Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.	3.11	5	0	nucleoside triphosphate analogue
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	2.03	1	0	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic

Condition	Relationship Strength	Studies	Trials
Absence Seizure [description not available]	2.72	3	0
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	2.72	3	0
Dementia Praecox [description not available]	5.02	15	0
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	5.02	15	0
Psychoses [description not available]	2.55	2	0
Psychotic Disorders Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994)	2.55	2	0
Congenital Zika Syndrome [description not available]	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	3.76	10	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1	0
Autosomal Dominant Juvenile Parkinson Disease [description not available]	2.31	1	0
Dyskinesia, Medication-Induced [description not available]	2.69	2	0
Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)	2.69	2	0
Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.	2.31	1	0
Ache [description not available]	4.22	6	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	4.22	6	0
Idiopathic Parkinson Disease [description not available]	2.72	3	0
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	2.72	3	0
Glaucoma, Suspect [description not available]	2.49	2	0
Ocular Hypertension A condition in which the intraocular pressure is elevated above normal and which may lead to glaucoma.	2.49	2	0
Nociceptive Pain Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.	2.17	1	0
Pulsatile Tinnitus [description not available]	3.12	1	0
Tinnitus A nonspecific symptom of hearing disorder characterized by the sensation of buzzing, ringing, clicking, pulsations, and other noises in the ear. Objective tinnitus refers to noises generated from within the ear or adjacent structures that can be heard by other individuals. The term subjective tinnitus is used when the sound is audible only to the affected individual. Tinnitus may occur as a manifestation of COCHLEAR DISEASES; VESTIBULOCOCHLEAR NERVE DISEASES; INTRACRANIAL HYPERTENSION; CRANIOCEREBRAL TRAUMA; and other conditions.	3.12	1	0
Drug Withdrawal Symptoms [description not available]	2.93	4	0
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	7.52	6	2
Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.	2.93	4	0
Hyperactivity, Motor [description not available]	2.52	2	0
Nerve Degeneration Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.	2.71	3	0
Delayed Effects, Prenatal Exposure [description not available]	2.1	1	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.1	1	0
Deaf Mutism [description not available]	2.1	1	0
Deafness A general term for the complete loss of the ability to hear from both ears.	2.1	1	0
Aura [description not available]	2.11	1	0
Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)	2.11	1	0
Ischemia A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.	2.44	2	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	2.13	1	0
Acute Confusional Senile Dementia [description not available]	2.05	1	0
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	2.46	2	0
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	2.05	1	0
Age-Related Memory Disorders [description not available]	2.42	2	0
Memory Disorders Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.	2.42	2	0
Adipocere [description not available]	2.06	1	0
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	2.06	1	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.07	1	0
Anxiety Neuroses [description not available]	5.02	3	1
Anxiety Disorders Persistent and disabling ANXIETY.	5.02	3	1
Chemical Dependence [description not available]	2.01	1	0
Behavior Disorders [description not available]	2.42	2	0
Brain Disorders [description not available]	2.01	1	0
Depression, Endogenous [description not available]	2.01	1	0
Mental Disorders Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function.	2.42	2	0
Brain Diseases Pathologic conditions affecting the BRAIN, which is composed of the intracranial components of the CENTRAL NERVOUS SYSTEM. This includes (but is not limited to) the CEREBRAL CORTEX; intracranial white matter; BASAL GANGLIA; THALAMUS; HYPOTHALAMUS; BRAIN STEM; and CEREBELLUM.	2.01	1	0
Depressive Disorder An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.	2.01	1	0
Substance-Related Disorders Disorders related to substance use or abuse.	2.01	1	0
Panic Attacks [description not available]	4.37	2	2
Panic Disorder A type of anxiety disorder characterized by unexpected panic attacks that last minutes or, rarely, hours. Panic attacks begin with intense apprehension, fear or terror and, often, a feeling of impending doom. Symptoms experienced during a panic attack include dyspnea or sensations of being smothered; dizziness, loss of balance or faintness; choking sensations; palpitations or accelerated heart rate; shakiness; sweating; nausea or other form of abdominal distress; depersonalization or derealization; paresthesias; hot flashes or chills; chest discomfort or pain; fear of dying and fear of not being in control of oneself or going crazy. Agoraphobia may also develop. Similar to other anxiety disorders, it may be inherited as an autosomal dominant trait.	4.37	2	2
Glaucoma An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)	2.03	1	0
Intraocular Pressure The pressure of the fluids in the eye.	2.03	1	0
Adjuvant Arthritis [description not available]	2.03	1	0
Polyarthritis [description not available]	2.03	1	0
Arthritis Acute or chronic inflammation of JOINTS.	2.03	1	0
Cerebral Ischemia [description not available]	2.91	4	0
Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.	2.91	4	0
Anterior Choroidal Artery Infarction [description not available]	1.99	1	0
Cerebral Infarction The formation of an area of NECROSIS in the CEREBRUM caused by an insufficiency of arterial or venous blood flow. Infarcts of the cerebrum are generally classified by hemisphere (i.e., left vs. right), lobe (e.g., frontal lobe infarction), arterial distribution (e.g., INFARCTION, ANTERIOR CEREBRAL ARTERY), and etiology (e.g., embolic infarction).	1.99	1	0
Catatonic Rigidity [description not available]	2.4	2	0
Muscle Rigidity Continuous involuntary sustained muscle contraction which is often a manifestation of BASAL GANGLIA DISEASES. When an affected muscle is passively stretched, the degree of resistance remains constant regardless of the rate at which the muscle is stretched. This feature helps to distinguish rigidity from MUSCLE SPASTICITY. (From Adams et al., Principles of Neurology, 6th ed, p73)	2.4	2	0
Acute Brain Injuries [description not available]	2.4	2	0
Brain Injuries Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.	2.4	2	0
Morphine Abuse [description not available]	2	1	0
Morphine Dependence Strong dependence, both physiological and emotional, upon morphine.	2	1	0
Cerebral Infarction, Middle Cerebral Artery [description not available]	2	1	0
Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.	2	1	0
Anterior Circulation Transient Ischemic Attack [description not available]	2	1	0
Ischemic Attack, Transient Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)	2	1	0
Anochlesia [description not available]	2	1	0
Cocaine Abuse [description not available]	2	1	0
Cocaine-Related Disorders Disorders related or resulting from use of cocaine.	2	1	0

eglumetad

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