Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H18O2 |
| Molecular Weight | 278.345 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12COC(=O)[C@]1(CC3=CC=C4C=CC=CC4=C3)CC(=C)C2
InChI
InChIKey=CVIRWLJKDBYYOG-MJGOQNOKSA-N
InChI=1S/C19H18O2/c1-13-8-17-12-21-18(20)19(17,10-13)11-14-6-7-15-4-2-3-5-16(15)9-14/h2-7,9,17H,1,8,10-12H2/t17-,19+/m1/s1
| Molecular Formula | C19H18O2 |
| Molecular Weight | 278.345 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
BAY-36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 uM). BAY-36-7620 is thus the first described mGlu1 receptor inverse agonist. It impairs classical conditioning and associated synaptic plasticity in hippocampal neurons. BAY-36-7620 exhibits neuroprotective and anticonvulsive effects in vivo following systemic administration.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. | 2001 May |
|
| Neuroprotective and behavioral effects of the selective metabotropic glutamate mGlu(1) receptor antagonist BAY 36-7620. | 2001 Oct 5 |
|
| Glutamate metabotropic receptors as targets for drug therapy in epilepsy. | 2003 Aug 22 |
|
| [3H]R214127: a novel high-affinity radioligand for the mGlu1 receptor reveals a common binding site shared by multiple allosteric antagonists. | 2003 May |
Patents
Sample Use Guides
Mice: BAY-36-7620 was given i.p. once a day, at a single dose level of 10 mg/kg. Treatment of mice bearing MDA-MB-231 xenografts with BAY-36-7620, by intraperitoneal injection, resulted in a significant reduction in tumor volume of up to 80%.
Route of Administration:
Intraperitoneal
To test for an antagonistic effect of BAY-36-7620 on mGlu1 or mGlu5 receptors, HEK 293 cells were stimulated with a Glu concentration around its EC50 value (1 uM for mGlu1a & 5 uM for mGlu5a), in the presence of BAY-36-7620, applied at a concentration of 0.1 or 10 uM. A strong inhibition of the Glu effect (61 ± 3 % inhibition) was observed with 0.1 uM BAY-36-7620 and a total inhibition was observed with 10 uM BAY-36-7620 on mGlu1 receptors whereas no effect was seen on mGlu5 receptors. The antagonist effect of BAY-36-7620 on mGlu1a receptors was concentration-dependent with an IC50 of 0.16 ± 0.01 uM.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:44:18 GMT 2023
by
admin
on
Sat Dec 16 09:44:18 GMT 2023
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| Record UNII |
0P934RSF8B
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| Record Status |
Validated (UNII)
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| Record Version |
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0P934RSF8B
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admin on Sat Dec 16 09:44:18 GMT 2023 , Edited by admin on Sat Dec 16 09:44:18 GMT 2023
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