Bioactivity | LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research[2]. |
In Vivo | LY487379 hydrochloride (intraperitoneal injection; 30 mg/kg; injected 30 min before the test) requires significantly fewer trials to criterion during the ED phase of the ASST in attentional set-shifting task in male Sprague-Dawley rats. But there has no significant drug effect during any other discrimination stage[1].LY487379 hydrochloride (intraperitoneal injection; 10-30 mg/kg) induces an increase in microdialysate norepinephrine levels; the dose-effect resembled a bell-shape relationship increased. And it dose-dependently increases extracellular serotonin levels in the medial prefrontal cortex in male Sprague-Dawley rats[1]. |
Name | LY487379 hydrochloride |
CAS | 353229-59-1 |
Formula | C21H20ClF3N2O4S |
Molar Mass | 488.91 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Agnieszka Nikiforuk, et al. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J Pharmacol Exp Ther. 2010 Dec;335(3):665-73. [2]. Hervé Schaffhauser, et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol. 2003 Oct;64(4):798-810. |