E-resources
Peer reviewed
Open access
-
Dickson, Louise; Teall, Martin; Chevalier, Elodie; Cheung, Toni; Liwicki, Gemma M.; Mack, Stephen; Stephenson, Anne; White, Kathryn; Fosbeary, Richard; Harrison, David C.; Brice, Nicola L.; Doyle, Kevin; Ciccocioppo, Roberto; Wu, Chaobo; Almond, Sarah; Patel, Toshal R.; Mitchell, Philip; Barnes, Matt; Ayscough, Andrew P.; Dawson, Lee A.; Carlton, Mark; Bürli, Roland W.
ACS medicinal chemistry letters, 04/2023, Volume: 14, Issue: 4Journal Article
The low affinity metabotropic glutamate receptor mGluR7 has been implicated in numerous CNS disorders; however, a paucity of potent and selective activators has hampered full delineation of the functional role and therapeutic potential of this receptor. In this work, we present the identification, optimization, and characterization of highly potent, novel mGluR7 agonists. Of particular interest is the chromane CVN636, a potent (EC50 7 nM) allosteric agonist which demonstrates exquisite selectivity for mGluR7 compared to not only other mGluRs, but also a broad range of targets. CVN636 demonstrated CNS penetrance and efficacy in an in vivo rodent model of alcohol use disorder. CVN636 thus has potential to progress as a drug candidate in CNS disorders involving mGluR7 and glutamatergic dysfunction.
Author
Shelf entry
Permalink
- URL:
Impact factor
Access to the JCR database is permitted only to users from Slovenia. Your current IP address is not on the list of IP addresses with access permission, and authentication with the relevant AAI accout is required.
Year | Impact factor | Edition | Category | Classification | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Select the library membership card:
If the library membership card is not in the list,
add a new one.
DRS, in which the journal is indexed
Database name | Field | Year |
---|
Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
---|
Source: Personal bibliographies
and: SICRIS
The material is available in full text. If you wish to order the material anyway, click the Continue button.