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基本描述
| 英文名称 | donecopride |
|---|---|
| 别名 | compound 1;MR31147 |
| 英文别名 | compound 1;MR31147 |
名称和标识符
| IUPAC Name | 1-(4-amino-5-chloro-2-methoxyphenyl)-3-[1-(cyclohexylmethyl)piperidin-4-yl]propan-1-one |
|---|---|
| INCHI | InChI=1S/C22H33ClN2O2/c1-27-22-14-20(24)19(23)13-18(22)21(26)8-7-16-9-11-25(12-10-16)15-17-5-3-2-4-6-17/h13-14,16-17H,2-12,15,24H2,1H3 |
| InChi Key | FTRZTHFGTILUPE-UHFFFAOYSA-N |
| Canonical SMILES | COc1cc(N)c(cc1C(=O)CCC1CCN(CC1)CC1CCCCC1)Cl |
| PubChem CID | 86582973 |
数据库链接
| PubChem CID | 86582973 |
|---|---|
| ChEMBL Ligand | CHEMBL3417009 |
| BindingDB Ligand | 50079362 |
| GPCRdb Ligand | donecopride |
关联配体
| Ligand ID | 10584 |
|---|---|
| 名称 | donecopride |
| 别名 | compound 1 [PMID: 25793650] |
| 类别 | Synthetic organic |
| 学名 | 1-(4-amino-5-chloro-2-methoxyphenyl)-3-[1-(cyclohexylmethyl)piperidin-4-yl]propan-1-one |
| 生物活性评价 |
In vitro, donecopride promotes secretion of the neurotrophic protein sAPPα, and it produces a procognitive effect in vivo Donecopride produces around half of the maximum agonist-induced cAMP response at the human 5-HT4e receptor that is produced by 5-HT |
| 评价 |
Donecopride is a small molecule that exhibits potent dual actions as an acetylcholinesterase (AChE) inhibitor and as a partial 5-HT4 receptor agonist |
产品问答
产品问答
参考文献
| 1. Lecoutey C, Hedou D, Freret T, Giannoni P, Gaven F, Since M, Bouet V, Ballandonne C, Corvaisier S, Malzert Fréon A et al.. (2014) Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatment.. Proc Natl Acad Sci USA, 111 (36): (E3825-30). [PMID:25157130] |
| 2. Rochais C, Lecoutey C, Gaven F, Giannoni P, Hamidouche K, Hedou D, Dubost E, Genest D, Yahiaoui S, Freret T et al.. (2015) Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride.. J Med Chem, 58 (7): (3172-87). [PMID:25793650] |
| 3. Rochais C, Lecoutey C, Hamidouche K, Giannoni P, Gaven F, Cem E, Mignani S, Baranger K, Freret T, Bockaert J et al.. (2020) Donecopride, a Swiss army knife with potential against Alzheimer's disease.. Br J Pharmacol, 177 (9): (1988-2005). [PMID:31881553] |
| 4. Eglen RM, Bonhaus DW, Johnson LG, Leung E, Clark RD. (1995) Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.. Br J Pharmacol, 115 (8): (1387-92). [PMID:8564196] |
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