Chemistry:PF-4455242
From HandWiki
Short description: Chemical compound
 | |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| ATC code |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| Chemical and physical data | |
| Formula | C21H28N2O2S |
| Molar mass | 372.53 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor.[1][2] Discovered by Pfizer in 2009, it was pursued in a phase I clinical trial for the treatment of bipolar disorder,[3] and was also investigated as a treatment for depression and substance abuse.[4] However, development was stopped in September 2010 due to toxicology findings in animals that had been exposed to the drug for three months.[3]
See also
- κ-Opioid receptor § Antagonists
- List of investigational antidepressants
References
- ↑ "Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242)". Journal of Medicinal Chemistry 54 (16): 5868–5877. August 2011. doi:10.1021/jm2006035. PMID 21744827.
- ↑ "Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation". Molecular Pharmacology 80 (5): 920–929. November 2011. doi:10.1124/mol.111.074195. PMID 21832171.
- ↑ 3.0 3.1 "Neuropeptide Receptors: Novel Therapeutic Targets for Depression and Anxiety Disorders". Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. 2012. pp. 314–317. ISBN 978-1-84973-365-6. https://books.google.com/books?id=J4Mq3Lm1R7kC&pg=PA314.
- ↑ "Oral Opioids". Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. 2013. p. 50. ISBN 978-1-84973-645-9. https://books.google.com/books?id=zUINAgAAQBAJ&pg=PA50.
External links
 |  |
