Compounds > mavoglurant
Page last updated: 2024-11-12

mavoglurant

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

mavoglurant: antagonist of metabotropic glutamate receptor 5 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9926832
CHEMBL ID3087515
SCHEMBL ID989279
MeSH IDM0585240

Synonyms (42)

Synonym
afq-056
mavoglurant
mavoglurant [usan:inn]
543906-09-8
afq 056
unii-gt0i9sv4f6
afq056
gt0i9sv4f6 ,
1h-indole-1-carboxylic acid, octahydro-4-hydroxy-4-(2-(3-methylphenyl)ethynyl)-, methyl ester, (3ar,4s,7ar)-
bdbm50443085
CHEMBL3087515
mavoglurant [inn]
1h-indole-1-carboxylic acid, octahydro-4-hydroxy-4-((3-methylphenyl)ethynyl)-, methyl ester, (3ar,4s,7ar)-
(-)-(3ar,4s,7ar)-4-hydroxy-4-m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester
methyl (3ar,4s,7ar)-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]octahydro-1h-indole-1-carboxylate
mavoglurant [usan]
mavoglurant [who-dd]
gtpl7586
methyl (3ar,4s,7ar)-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-3,3a,5,6,7,7a-hexahydro-2h-indole-1-carboxylate
2u8 ,
CS-5245
HY-15257
ZFPZEYHRWGMJCV-ZHALLVOQSA-N
SCHEMBL989279
methyl (3ar,4s,7ar)-4-hydroxy-4-(m-tolylethynyl)octahydro-1h-indole-1-carboxylate
DTXSID30202777
4OO9
AKOS027326541
(3ar,4s,7ar)-methyl 4-hydroxy-4-(m-tolylethynyl)octahydro-1h-indole-1-carboxylate
DB13004
(3ar,4s,7ar)-octahydro-4-hydroxy-4-[2-(3-methylphenyl)ethynyl]-1h-indole-1-carboxylic acid methyl ester
methyl (3ar,4s,7ar)-4-hydroxy-4-[(3-methylphenyl)ethynyl]octahydro-1h-indole-1-carboxylate
'methyl (3ar,4s,7ar)-4-hydroxy-4-[(3-methylphenyl)ethynyl]octahydro-1h-indole-1-carboxylate'
BCP20624
EX-A1564
mavoglurant, afq056
Q6589598
1636881-61-2
F85489
F85319
mavoglurant racemate
AS-79009

Research Excerpts

Overview

Mavoglurant (MVG) is an antagonist at the metabotropic glutamate receptor-5. Currently under clinical development at Novartis Pharma AG for the treatment of central nervous system diseases.

ExcerptReferenceRelevance
"Mavoglurant (MVG) is an antagonist at the metabotropic glutamate receptor-5 currently under clinical development at Novartis Pharma AG for the treatment of central nervous system diseases. "( Application of a Bayesian approach to physiological modelling of mavoglurant population pharmacokinetics.
Aarons, L; Dumitras, S; Ogungbenro, K; Wendling, T, 2015)		2.1

Pharmacokinetics

In conclusion, EE PK was unchanged, whereas Cmax and AUClast of LNG were 19% and 32% lower, respectively, when given with mavoglurant. Further investigation regarding the impact on contraceptive efficacy is warranted.

ExcerptReferenceRelevance
" Plasma concentrations of EE and LNG were measured up to 72 hours post administration, and the PK parameters Cmax and AUClast were estimated using noncompartmental methods."( Effect of mavoglurant (AFQ056), a selective mGluR5 antagonist, on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women.
Chakraborty, A; Jakab, A; Legangneux, E; Mensinga, T; Neelakantham, S; Rouzade-Dominguez, ML; Sivasubramanian, R; Ufer, M; Woessner, R, 2015)		0.82
"In conclusion, EE PK was unchanged, whereas Cmax and AUClast of LNG were 19% and 32% lower, respectively, when given with mavoglurant Further investigation regarding the impact on contraceptive efficacy is warranted."( Effect of mavoglurant (AFQ056), a selective mGluR5 antagonist, on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women.
Chakraborty, A; Jakab, A; Legangneux, E; Mensinga, T; Neelakantham, S; Rouzade-Dominguez, ML; Sivasubramanian, R; Ufer, M; Woessner, R, 2015)		1.03
" The aim of this study was to develop and optimise a population whole-body physiologically-based pharmacokinetic (WBPBPK) model for MVG, to predict the impact of drug-drug interaction (DDI) and age on its pharmacokinetics."( Application of a Bayesian approach to physiological modelling of mavoglurant population pharmacokinetics.
Aarons, L; Dumitras, S; Ogungbenro, K; Wendling, T, 2015)		0.65
"Whole-body physiologically based pharmacokinetic (PBPK) models are increasingly used in drug development for their ability to predict drug concentrations in clinically relevant tissues and to extrapolate across species, experimental conditions and sub-populations."( Reduction of a Whole-Body Physiologically Based Pharmacokinetic Model to Stabilise the Bayesian Analysis of Clinical Data.
Aarons, L; Dumitras, S; Ogungbenro, K; Pigeolet, E; Tsamandouras, N; Wendling, T, 2016)		0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
" However, our results suggest that mavoglurant combined with higher doses of L-dopa may be effective in treating patients with Parkinson's disease experiencing L-dopa-related motor fluctuations and dyskinesias."( Mavoglurant (AFQ056) in combination with increased levodopa dosages in Parkinson's disease patients.
Dronamraju, N; Graf, A; Hauser, RA; Kenney, C; Kumar, R; Merschhemke, M; Mostillo, J, 2016)		2.15

Bioavailability

ExcerptReferenceRelevance
" The mean absolute bioavailability from the MR formulation (0."( Model-based evaluation of the impact of formulation and food intake on the complex oral absorption of mavoglurant in healthy subjects.
Aarons, L; Dumitras, S; Ogungbenro, K; Pigeolet, E; Wendling, T; Woessner, R, 2015)		0.63

Dosage Studied

ExcerptRelevanceReference
" Based on final actual doses, there was a dose-response relationship on the modified Abnormal Involuntary Movements Scale, with 200 mg daily demonstrating the most robust effect (difference, -3."( AFQ056 in Parkinson patients with levodopa-induced dyskinesia: 13-week, randomized, dose-finding study.
Destee, A; Gao, H; Graf, A; Hattori, N; Hauser, RA; Kenney, C; Lang, AE; Merschhemke, M; Nagel, J; Poewe, W; Rascol, O; Stacy, M; Stocchi, F; Tolosa, E; Trenkwalder, C, 2013)		0.39
" Mavoglurant (AFQ056) was up-titrated over two weeks from 25 mg twice daily (bid) to 100 mg bid (L-dopa kept stable), followed by three weeks during which the daily L-dopa dosage was increased by up to 300 mg/day."( Mavoglurant (AFQ056) in combination with increased levodopa dosages in Parkinson's disease patients.
Dronamraju, N; Graf, A; Hauser, RA; Kenney, C; Kumar, R; Merschhemke, M; Mostillo, J, 2016)		2.79
" A potential strategy, currently under investigation, is the coadministration of metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators (NAMs) and L-DOPA; a treatment that results in the improvement of dyskinesia symptoms and that permits reductions in l-DOPA dosage frequency."( Mavoglurant as a treatment for Parkinson's disease.
Auladell, C; Beas-Zarate, C; Camins, A; Canudas, AM; de Lemos, ML; Folch, J; Lazarowski, A; Pallàs, M; Pedros, I; Petrov, D, 2014)		1.85
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)IC50 (µMol)0.05160.00000.52627.9700AID1054271
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)Ki0.06600.00050.19643.7600AID1054270
Metabotropic glutamate receptor 5Homo sapiens (human)IC50 (µMol)0.04080.00050.439410.0000AID1054272; AID1240757
Metabotropic glutamate receptor 5Homo sapiens (human)Ki0.00780.00050.54638.2000AID1240756; AID1275086
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
desensitization of G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of DNA-templated transcriptionMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
learning or memoryMetabotropic glutamate receptor 5Homo sapiens (human)
learningMetabotropic glutamate receptor 5Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMetabotropic glutamate receptor 5Homo sapiens (human)
synapse organizationMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of calcium-mediated signalingMetabotropic glutamate receptor 5Homo sapiens (human)
cognitionMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
cellular response to amyloid-betaMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 5Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase activator activityMetabotropic glutamate receptor 5Homo sapiens (human)
A2A adenosine receptor bindingMetabotropic glutamate receptor 5Homo sapiens (human)
identical protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase bindingMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
dendriteMetabotropic glutamate receptor 5Homo sapiens (human)
cytoplasmMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 5Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 5Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 5Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 5Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2014Nature, Jul-31, Volume: 511, Issue:7511
Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain.
AID1275086Displacement of [3H]-M-MPEP from mGluR5 StaR domain (569 to 836 residues) (unknown origin) expressed in HEK293 cell membranes2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.
AID1054271Negative allosteric modulation of mGlu5 receptor in rat primary astrocytes assessed as inhibition of L-quisqualate-induced intracellular calcium mobilization preincubated for 5 mins before L-quisqualate addition by FLIPR assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1054270Displacement of [3H]-M-MPEP from mGlu5 receptor in Sprague-Dawley rat cortex after 1 hr by liquid scintillation counting2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1054267Intrinsic clearance in Sprague-Dawley rat liver microsomes after 45 mins by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1054269Kinetic solubility of the compound in TRIS buffer at pH 7.5 after 15 mins by HPLC analysis2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1240756Displacement of [3H]-M-MPEP from human mGlu5 receptor expressed in HEK293 cells after 90 mins by scintillation spectroscopy analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
AID1054273Thermodynamic solubility of the compound in water at pH 7.4 after 48 hrs by shake-flask method2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1240757Negative allosteric modulation at human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-quisqualic acid-induced inositol phosphate turnover preincubated for 45 mins before L-quisqualic acid challenge measured after 15 mins by IPone as2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
AID1054272Negative allosteric modulation of human mGlu5 receptor expressed in CHO cells assessed as inhibition of L-quisqualate-induced intracellular calcium mobilization preincubated for 5 mins before L-quisqualate addition by FLIPR assay2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
AID1054268Intrinsic clearance in human liver microsomes after 45 mins by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (36)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's33 (91.67)24.3611
2020's3 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.02

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.02 (24.57)
Research Supply Index3.87 (2.92)
Research Growth Index4.54 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (30.56%)5.53%
Reviews4 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (58.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		2.1110dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		8.51117-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
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		9.3974amino 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
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.2110isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		2.57201,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		8.51117beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
ethinyl estradiol-norgestrel combination
Ethinyl Estradiol-Norgestrel Combination: ETHINYL ESTRADIOL and NORGESTREL given in fixed proportions.		3.511
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.		2.57201,2,3-triazole
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.5111aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
zm 241385
ZM 241385: a high affinity radioligand selective for the A2a adenosine receptor		2.1310diamino-1,3,5-triazine
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.		2.7930acetylenic compound;
methylpyridines		anxiolytic drug;
metabotropic glutamate receptor antagonist
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine: an excitatory amino acid antagonist		2.1310
azd2066
[no description available]		2.2110
6-fluoro-2-(4-(pyridin-2-yl)but-3-yn-1-yl)imidazo(1,2-a)pyridine
6-fluoro-2-(4-(pyridin-2-yl)but-3-yn-1-yl)imidazo(1,2-a)pyridine: an mGluR5 antagonist; structure in first source		2.5820
grn-529
GRN-529: an mGluR5 antagonist; structure in first source		2.0810
3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile
3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile: a metabotropic glutamate receptor 5 antagonist; structure in first source		2.5220
fenobam
fenobam: in USAN fenobam refers to monohydrate		2.2110ureas
ConditionIndicatedRelationship StrengthStudiesTrials
Abnormal Movements
[description not available]		03.2310
Idiopathic Parkinson Disease
[description not available]		010.186
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)		112.186
Esophageal Reflux
[description not available]		08.5311
Gastroesophageal Reflux
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.		110.5311
Fra(X) Syndrome
[description not available]		010.27126
Fragile X Syndrome
A condition characterized genotypically by mutation of the distal end of the long arm of the X chromosome (at gene loci FRAXA or FRAXE) and phenotypically by cognitive impairment, hyperactivity, SEIZURES, language delay, and enlargement of the ears, head, and testes. INTELLECTUAL DISABILITY occurs in nearly all males and roughly 50% of females with the full mutation of FRAXA. (From Menkes, Textbook of Child Neurology, 5th ed, p226)		112.27126
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.1710
Behavior Disorders
[description not available]		03.5611
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.		03.5611
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		04.3911
Dyskinesia, Medication-Induced
[description not available]		09.3375
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)		09.3375
Action Tremor
[description not available]		03.5111
Tremor
Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE.		03.5111
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.9340
Chorea Disorders
[description not available]		04.4111
Akinetic-Rigid Variant of Huntington Disease
[description not available]		04.4111
Chorea
Involuntary, forcible, rapid, jerky movements that may be subtle or become confluent, markedly altering normal patterns of movement. Hypotonia and pendular reflexes are often associated. Conditions which feature recurrent or persistent episodes of chorea as a primary manifestation of disease are referred to as CHOREATIC DISORDERS. Chorea is also a frequent manifestation of BASAL GANGLIA DISEASES.		16.4111
Huntington Disease
A familial disorder inherited as an autosomal dominant trait and characterized by the onset of progressive CHOREA and DEMENTIA in the fourth or fifth decade of life. Common initial manifestations include paranoia; poor impulse control; DEPRESSION; HALLUCINATIONS; and DELUSIONS. Eventually intellectual impairment; loss of fine motor control; ATHETOSIS; and diffuse chorea involving axial and limb musculature develops, leading to a vegetative state within 10-15 years of disease onset. The juvenile variant has a more fulminant course including SEIZURES; ATAXIA; dementia; and chorea. (From Adams et al., Principles of Neurology, 6th ed, pp1060-4)		16.4111
Anankastic Personality
[description not available]		04.4511
Obsessive-Compulsive Disorder
An anxiety disorder characterized by recurrent, persistent obsessions or compulsions. Obsessions are the intrusive ideas, thoughts, or images that are experienced as senseless or repugnant. Compulsions are repetitive and seemingly purposeful behavior which the individual generally recognizes as senseless and from which the individual does not derive pleasure although it may provide a release from tension.		16.4511
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0810