| Name | LY2794193 |
| Description | LY2794193, a potent and selective mGlu3 (metabotropic glutamate 3) receptor agonist, Ki=0.927 nM, EC50=0.47 nM, reduces akathisia seizures and depressive-like behaviors and increases GAT1, GLAST and GLT-1 protein levels in rats. |
| In vitro | When its agonist responses were examined in cells co-expressing a promiscuous G protein (Gαq), LY2794193 exhibited agonist activity against both hmGlu3 (EC50 value of 11.6 nM) and hmGlu2 (EC50 value of 277 nM).[1] |
| In vivo | Methods: Two doses of LY2794193 (0.1, 0.3, and 1 mg/kg, sc) and LY2794193 (1, 3, and 10 mg/kg, sc) were administered to rats; the first study employed dose levels, while the second evaluated higher doses; in each study, plasma and cerebrospinal fluid (CSF) levels were determined 1 h after LY2794193 administration.
Results: Plasma and CSF levels of LY2794193 were observed at all dose levels, and a linear increase in each compartment with increasing dose was observed. The fraction of LY2794193 partitioning into the CSF was both low and highly consistent across dose levels, with a CSF to plasma ratio of 1% calculated over a 100-fold concentration range. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 1 mg/mL (2.99 mM), when pH is adjusted to 14 with NaOH.
DMSO : 180 mg/mL (538.41 mM), Sonication is recommended.
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| Keywords | mGluR3 | mGluR2 | LY-2794193 | LY2794193 |
| Inhibitors Related | S-Sulfo-L-cysteine sodium salt | IDRA-21 | Urethane | Decanoic Acid | DCB | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Memantine hydrochloride | O-Phospho-L-serine |
United States
