3-aMino-5-chloro-N-cyclopropyl-4-Methyl-6-(2-(4-Methylpiperazin-1-yl)-2-oxoethoxy)thieno[2,3-b]pyridine-2-carboxaMide

Description

LY2119620 is a positive allosteric modulator of the M₂ and M₄ muscarinic acetylcholine receptors (mAChRs). It binds to allosteric sites on M₂ and M₄ receptors with K_B values ranging from 1.8 to 3.4 μM. LY2119620 potentiates the activity of the AChR agonist acetylcholine (ACh; ) and the mAChR agonists iperoxo and oxotremorine M at human recombinant M₂ and M₄ receptors expressed in CHO cell membranes. LY2119620 also exhibits allosteric agonism at M₂ and M₄ receptors (23.2 and 16.8%, respectively, of the maximal ACh response).

Uses

LY 2119620 acts as a novel positive allosteric modulator in the treatment of schizophrenia acting as an anti-psychotic agent.

storage

Store at -20°C

References

[1]. croy ch, schober da, xiao h, et al. characterization of the novel positive allosteric modulator, ly2119620, at the muscarinic m(2) and m(4) receptors. mol pharmacol, 2014, 86(1): 106-115. kruse ac, ring am, manglik a, et al. activation and allosteric modulation of a muscarinic acetylcholine receptor. nature, 2013, 504(7478): 101-106.schober da, croy ch, xiao h, et al. development of a radioligand, [(3)h]ly2119620, to probe the human m(2) and m(4) muscarinic receptor allosteric binding sites. mol pharmacol, 2014, 86(1): 116-123.