Chemistry:ABT-239
From HandWiki
Short description: Chemical compound
 | |
| Identifiers | |
|---|---|
| |
| CAS Number |
|
| PubChem CID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C22H22N2O |
| Molar mass | 330.431 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
ABT-239 is an H3-receptor inverse agonist developed by Abbott. It has stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia.[1][2][3][4] ABT-239 is more active at the human H3 receptor than comparable agents such as thioperamide, ciproxifan, and cipralisant. It was ultimately dropped from human trials after showing the dangerous cardiac side effect of QT prolongation,[5] but is still widely used in animal research into H3 antagonists / inverse agonists.
References
- ↑ "Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties". J. Pharmacol. Exp. Ther. 313 (1): 165–75. 2005. doi:10.1124/jpet.104.078303. PMID 15608078.
- ↑ "Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist". J. Pharmacol. Exp. Ther. 313 (1): 176–90. 2005. doi:10.1124/jpet.104.078402. PMID 15608077.
- ↑ "4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention". J. Med. Chem. 48 (1): 38–55. 2005. doi:10.1021/jm040118g. PMID 15634000.
- ↑ "Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists". J. Pharmacol. Exp. Ther. 325 (3): 902–9. June 2008. doi:10.1124/jpet.107.135343. PMID 18305012.
- ↑ Hancock, AA (2006). "The challenge of drug discovery of a GPCR target: analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists.". Biochemical Pharmacology 71 (8): 1103–13. doi:10.1016/j.bcp.2005.10.033. PMID 16513092.
External links
- 4-(2-(2-(2-methyl-1-pyrrolidinyl)ethyl)-1-benzofuran-5-yl)benzonitrile at the US National Library of Medicine Medical Subject Headings (MeSH)
 |  |
