Page last updated: 2024-12-04

1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester

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

1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester is a chemical compound, often referred to by its shorter name, **MPEP**. It is a potent and selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5).

Here's why MPEP is important for research:

* **Understanding mGluR5 function:** MPEP is a valuable tool for studying the role of mGluR5 in the brain. By blocking the receptor, researchers can investigate how mGluR5 activation affects various processes, such as learning, memory, neuronal plasticity, and neurotransmission.
* **Investigating therapeutic potential:** mGluR5 is implicated in a variety of neurological and psychiatric disorders, including anxiety, depression, Parkinson's disease, Alzheimer's disease, and epilepsy. MPEP and related compounds are being investigated as potential therapeutic agents for these conditions.
* **Preclinical studies:** MPEP has been extensively used in preclinical studies to evaluate the therapeutic potential of mGluR5 antagonists for various neurological and psychiatric disorders. These studies have yielded promising results, suggesting that mGluR5 antagonism could offer novel treatment strategies.
* **Understanding brain circuitry:** mGluR5 plays a critical role in brain circuitry. Research with MPEP helps to decipher the complex interactions between mGluR5 and other receptors and signaling pathways, providing insights into the underlying mechanisms of brain function.

**However, it is crucial to note that MPEP is a research tool and not a commercially available drug.** It has not been approved for human use, and its safety and efficacy in humans are still under investigation.

Overall, 1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester (MPEP) is a valuable tool for research into the role of mGluR5 in various physiological and pathological processes. Its importance lies in its ability to dissect the complex role of this receptor in the brain and its potential as a therapeutic target for various neurological and psychiatric disorders.

Cross-References

ID SourceID
PubMed CID2229
CHEMBL ID128365
CHEBI ID92418
SCHEMBL ID13184690

Synonyms (30)

Synonym
BRD-K23922020-075-01-1
prop-2-ynyl 1-methyl-5,6-dihydro-2h-pyridine-3-carboxylate
gtpl295
NCGC00015006-01 ,
lopac-a-140
LOPAC0_000136
NCGC00162072-02
NCGC00162072-01
NCGC00015006-04
arecaidine propargyl ester
CHEMBL128365
L000114
prop-2-ynyl 1-methyl-3,6-dihydro-2h-pyridine-5-carboxylate
CCG-204231
NCGC00015006-03
NCGC00015006-02
3-pyridinecarboxylic acid, 1,2,5,6-tetrahydro-1-methyl-, 2-propynyl ester
35516-99-5
2-propynyl 1-methyl-1,2,5,6-tetrahydro-3-pyridinecarboxylate #
SPHRJZBOFYIKMC-UHFFFAOYSA-N
1-methyl-1,2,5,6-tetrahydropyridine-3-carboxylic acid, 2-propynyl ester
SCHEMBL13184690
DTXSID30274358
CHEBI:92418
bdbm50475680
Q27074500
3-pyridinecarboxylic acid, 1,2,5,6-tetrahydro-1-methyl-, 2-butynyl ester,4-methylbenzenesulfonate
SDCCGSBI-0050124.P002
NCGC00015006-07
arecaidine-propargyl-ester
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
dihydropyridine
[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 Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
NFKB1 protein, partialHomo sapiens (human)Potency22.38720.02827.055915.8489AID895; AID928
ThrombopoietinHomo sapiens (human)Potency1.25890.02517.304831.6228AID917; AID918
regulator of G-protein signaling 4Homo sapiens (human)Potency0.53230.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency15.10141.069113.955137.9330AID720538
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.00001.000010.475628.1838AID1457
Ataxin-2Homo sapiens (human)Potency31.62280.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.75690.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.53220.00000.690210.0000AID261554; AID261556
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.91420.00000.79519.1201AID261555; AID261556
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.93330.00000.72926.9183AID261567
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki1.04070.00000.59729.1201AID261553; AID261555
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki4.84500.00051.42495.2000AID1090601; AID1090602
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.85110.00000.54057.7600AID261555
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID343197Intrinsic activity at muscarinic M3 receptor in guinea pig ileum assessed as effect on tissue tension changes relative to control2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID1090597Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090601Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID261556Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID261557Agonist potency at muscarinic M1 receptor in rabbit vas deferens2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID343193Agonist activity at muscarinic M1/M4 receptor in New Zealanda white rabbit vas deferens assessed as effect on isometric tissue contraction2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID1090589Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID261559Agonist potency at muscarinic M2 receptor in guinea pig atrium2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID79824Inotropic responses, induced by the compound in electrically paced (Hz) guinea pig left atria2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
AID261553Binding affinity to cloned human muscarinic M1 receptor expressed in CHO cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID1090598Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID261555Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID343198Agonist activity at muscarinic M3 receptor in guinea pig ileum assessed as effect on tissue tension changes2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID343200Intrinsic activity at muscarinic M1/M4 receptor in guinea pig lung assessed as effect on tissue contraction relative to control2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID1090591Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID343195Intrinsic activity at muscarinic M2 receptor in guinea pig atrium assessed as effect on inotropic activity relative to control2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID77368Inotropic response relative to APE (APE = 100) in electrically paced (Hz) guinea pig left atria2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
AID1090593Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID261563Agonist potency at muscarinic M4 receptor in guinea pig lung strips2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID261561Agonist potency at muscarinic M3 receptor in guinea pig ileum2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID261554Binding affinity to cloned human muscarinic M2 receptor expressed in CHO cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID1090590Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID261567Binding affinity to cloned human muscarinic M5 receptor expressed in CHO cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
AID343196Agonist activity at muscarinic M2 receptor in guinea pig atrium assessed as effect on inotropic activity2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID343201Agonist activity at muscarinic M1/M4 receptor in guinea pig lung assessed as effect on tissue contraction2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID1090594Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090595Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090592Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1090602Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID343192Intrinsic activity at muscarinic M1/M4 receptor in New Zealanda white rabbit vas deferens assessed as effect on isometric tissue contraction relative to control2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.
AID1090596Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))1997Molecular pharmacology, Jul, Volume: 52, Issue:1
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1997Molecular pharmacology, Jul, Volume: 52, Issue:1
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1997Molecular pharmacology, Jul, Volume: 52, Issue:1
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1997Molecular pharmacology, Jul, Volume: 52, Issue:1
Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (6.25)18.2507
2000's5 (31.25)29.6817
2010's5 (31.25)24.3611
2020's5 (31.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.34

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.34 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index5.17 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.34)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]