Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C11H16N2O5.ClH |
Molecular Weight | 292.716 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 5 / 5 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.[H][C@@]12CC[C@@](NC(=O)[C@H](C)N)(C(O)=O)[C@]1([H])[C@H]2C(O)=O
InChI
InChIKey=TWZDLCLCMKMJPE-OAOSNHGPSA-N
InChI=1S/C11H16N2O5.ClH/c1-4(12)8(14)13-11(10(17)18)3-2-5-6(7(5)11)9(15)16;/h4-7H,2-3,12H2,1H3,(H,13,14)(H,15,16)(H,17,18);1H/t4-,5-,6-,7-,11-;/m0./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/12789623https://www.ncbi.nlm.nih.gov/pubmed/16223873 | https://www.ncbi.nlm.nih.gov/pubmed/15821951Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800008428
https://en.wikipedia.org/wiki/Eglumegad
https://www.ncbi.nlm.nih.gov/pubmed/17712352
https://www.ncbi.nlm.nih.gov/pubmed/17204749
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12789623https://www.ncbi.nlm.nih.gov/pubmed/16223873 | https://www.ncbi.nlm.nih.gov/pubmed/15821951
Curator's Comment: description was created based on several sources, including:
http://adisinsight.springer.com/drugs/800008428
https://en.wikipedia.org/wiki/Eglumegad
https://www.ncbi.nlm.nih.gov/pubmed/17712352
https://www.ncbi.nlm.nih.gov/pubmed/17204749
Talaglumetad (also known as LY-544344) is a bicyclohexane derivative patented by Eli Lilly and Company as modulators of metabotropic glutamate receptor. Talaglumetad acts as a prodrug of Eglumegad, a selective agonist of metabotropic glutamate receptors (mGluR2/3) and metabolized to release active compound by both human jejunal homogenates and rat liver homogenates. In experiments on mice, Talaglumetad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL5137 |
99.0 nM [Ki] | ||
Target ID: CHEMBL2888 |
94.0 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Doses
Dose | Population | Adverse events |
---|---|---|
200 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: panic disorder Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: |
Disc. AE: headache, Nausea... AEs leading to discontinuation/dose reduction: headache (1 pt) Sources: Nausea (1 pt) allergic reaction (2 patients) Dizziness (1 pt) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dizziness | 1 pt Disc. AE |
200 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: panic disorder Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: |
Nausea | 1 pt Disc. AE |
200 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: panic disorder Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: |
headache | 1 pt Disc. AE |
200 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: panic disorder Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: |
allergic reaction | 2 patients Disc. AE |
200 mg 1 times / day multiple, oral (unknown) Studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: |
unhealthy n = 18 Health Status: unhealthy Condition: panic disorder Sex: M+F Food Status: UNKNOWN Population Size: 18 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
LY354740, a group II metabotropic glutamate receptor agonist with potential antiparkinsonian properties in rats. | 1998 Oct |
|
The role of metabotropic glutamate receptor (mGluR) ligands in parkinsonian muscle rigidity. | 2000 |
|
The role of striatal metabotropic glutamate receptors in Parkinson's disease. | 2002 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16192835
Curator's Comment: 8 or 16 mg twice per day (LY544344). LY544344 is a LY354740 prodrug that increases LY354740 bioavailability.
https://www.ncbi.nlm.nih.gov/pubmed/17712352
100 or 200 mg (LY354740)
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19755662
LY354740 failed to inhibit Dopamine D(2) receptor binding in both native striatal tissue homogenates and cloned receptors at concentrations up to 10 uM.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C28197
Created by
admin on Fri Dec 15 17:20:50 GMT 2023 , Edited by admin on Fri Dec 15 17:20:50 GMT 2023
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DTXSID40963180
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300000044511
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PP-78
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CHEMBL1189257
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C81620
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441765-97-5
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9857255
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X30300EU7I
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ACTIVE MOIETY
SUBSTANCE RECORD