886047-22-9 Usage
Description
3-aMino-5-chloro-N-cyclopropyl-4-Methyl-6-(2-(4-Methylpiperazin-1-yl)-2-oxoethoxy)thieno[2,3-b]pyridine-2-carboxaMide, also known as LY 2119620, 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 KB values ranging from 1.8 to 3.4 μM and 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
Used in Pharmaceutical Industry:
3-aMino-5-chloro-N-cyclopropyl-4-Methyl-6-(2-(4-Methylpiperazin-1-yl)-2-oxoethoxy)thieno[2,3-b]pyridine-2-carboxaMide is used as an anti-psychotic agent for the treatment of schizophrenia. It acts as a novel positive allosteric modulator, enhancing the activity of acetylcholine and other mAChR agonists at M2 and M4 receptors, which can help improve cognitive function and reduce positive and negative symptoms associated with schizophrenia.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 886047-22-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,8,6,0,4 and 7 respectively; the second part has 2 digits, 2 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 886047-22:
(8*8)+(7*8)+(6*6)+(5*0)+(4*4)+(3*7)+(2*2)+(1*2)=199
199 % 10 = 9
So 886047-22-9 is a valid CAS Registry Number.
886047-22-9Relevant articles and documents
THIENOPYRIDINES AS ALLOSTERIC POTENTIATORS OF THE M4 MUSCARINIC RECEPTOR
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Page/Page column 21-22, (2008/06/13)
The present invention relates to selective allosteric potentiators of the Formula (I): or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors.
