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品質水準
アッセイ
≥98% (HPLC)
形状
solid
保管条件
desiccated
色
off-white to tan
溶解性
DMSO: >20 mg/mL
オーガナイザー
Eli Lilly
保管温度
−20°C
SMILES記法
COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl
InChI
1S/C13H14ClN3O2S/c1-5-7-9(15)10(11(18)16-6-3-4-6)20-13(7)17-12(19-2)8(5)14/h6H,3-4,15H2,1-2H3,(H,16,18)
InChI Key
CTEGQKDJTBWFHW-UHFFFAOYSA-N
生物化学的／生理学的作用
LY2033298は、ヒトM4ムスカリン性アセチルコリン受容体サブタイプに高度に選択的に作用する頑健でアロステリックな増強剤です。LY2033298は、ACh-M4結合を強めますが、M1/3/5受容体には影響しません。LY2033298は、M ACh受容体にも結合でき、受容体活性を調べるために使用されるリガンドに応じて、正または負のアロステリックな作用を調節します。
特徴および利点
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
シグナルワード
Danger
危険有害性情報
危険有害性の分類
Resp. Sens. 1
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Vindhya Nawaratne et al.
Molecular pharmacology, 74(4), 1119-1131 (2008-07-17)
The M4 muscarinic acetylcholine (ACh) receptor (mAChR) is a potential therapeutic target but characterized by a lack of subtype-selective ligands. We recently generated "designer receptors exclusively activated by a designer drug" (DREADDs), which contained mutations of two conserved orthosteric-site residues
W Y Chan et al.
Proceedings of the National Academy of Sciences of the United States of America, 105(31), 10978-10983 (2008-08-06)
Current antipsychotics provide symptomatic relief for patients suffering from schizophrenia and related psychoses; however, their effectiveness is variable and many patients discontinue treatment due to side effects. Although the etiology of schizophrenia is still unclear, a leading hypothesis implicates an
Jana K Shirey et al.
Nature chemical biology, 4(1), 42-50 (2007-12-07)
Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of multiple central nervous system disorders. We have used cheminformatics and medicinal chemistry to develop new, highly selective M4 allosteric potentiators. VU10010, the lead compound, potentiates the M4 response to
Michael Bubser et al.
ACS chemical neuroscience, 5(10), 920-942 (2014-08-20)
Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR) represent a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders. We recently reported that the selective M4 PAM VU0152100 produced an antipsychotic
Jing Wu et al.
European journal of pharmacology, 882, 173274-173274 (2020-06-14)
Opioids strongly inhibit GABAergic neurons in the rostromedial tegmental nucleus (RMTg) that expresses μ-opioid receptors to induce rewarding and psychomotor effects. M3 and M4 muscarinic receptors are co-localized with μ-opioid receptors at these GABAergic neurons. This study explored whether RMTg
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