353229-59-1

353229-59-1 structure

Name: LY-487379 hydrochloride
Chemical Name: 2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(pyridin-3-ylmethyl)ethanesulfonamide,hydrochloride
CAS Number: 353229-59-1
Molecular Formula: C₂₁H₂₀ClF₃N₂O₄S
Molecular Weight: 488.90800
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2017-09-20 02:05:00
Modify Date: 2024-01-14 18:04:08
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].

Name	2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(pyridin-3-ylmethyl)ethanesulfonamide,hydrochloride

Description	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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
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].
References	[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.

Molecular Formula	C₂₁H₂₀ClF₃N₂O₄S
Molecular Weight	488.90800
Exact Mass	488.07800
PSA	77.11000
LogP	6.66400

RIDADR	NONH for all modes of transport

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