Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H19NO4 |
| Molecular Weight | 325.3585 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCOC(=O)NC(=O)C1C2=CC=CC=C2OC3=CC=CC=C13
InChI
InChIKey=RQBUXEUMZZQUFY-UHFFFAOYSA-N
InChI=1S/C19H19NO4/c1-2-3-12-23-19(22)20-18(21)17-13-8-4-6-10-15(13)24-16-11-7-5-9-14(16)17/h4-11,17H,2-3,12H2,1H3,(H,20,21,22)
| Molecular Formula | C19H19NO4 |
| Molecular Weight | 325.3585 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11606768Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/16645124
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11606768
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/16645124
Ro 67-4853 exhibited activity at all group I of metabotropic glutamate receptors including mGluR1 and mGluR5. It enhances the effects of (S)-DHPG in CA3 neurons. Site-directed mutagenesis revealed that valine at position 757 in transmembrane V of mGluR1 is crucial for the activity of multiple classes of allosteric mGluR1 potentiators. The discovery of selective mGluR1 enhancers opens the possibility for therapeutically relevant positive modulation of family 3 G proteincoupled receptors.
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11606768
Curator's Comment: # F. Hoffmann-La Roche Ltd.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3772 |
7.16 null [pEC50] | ||
Target ID: CHEMBL2564 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11606768 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Function of mGlu1 receptors in the modulation of nociceptive processing in the thalamus. | 2014-04 |
|
| Extracellular calcium modulates actions of orthosteric and allosteric ligands on metabotropic glutamate receptor 1α. | 2014-01-17 |
|
| Potentiation of sensory responses in ventrobasal thalamus in vivo via selective modulation of mGlu1 receptors with a positive allosteric modulator. | 2012-03 |
|
| Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. | 2001-11-06 |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11606768
Concentration-response curves for the effect of Ro 67-4853 was generated in CA3 neurons by using 5 uM S-DHPG. The maximum potentiation of the S-DHPG effect by Ro 67-4853 was 637 % of control. Ro 67-4853 was potent in enhancing the effect of S-DHPG with EC50 values of 95 nM.
| Substance Class |
Chemical
Created
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admin
on
Edited
Wed Apr 02 09:19:54 GMT 2025
by
admin
on
Wed Apr 02 09:19:54 GMT 2025
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| Record UNII |
QM27L9Q3RZ
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| Record Status |
Validated (UNII)
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9949202
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Ro67-4853
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302841-89-0
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DTXSID70433240
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QM27L9Q3RZ
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET->MODULATOR |
POSITIVE ALLOSTERIC MODULATOR
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