PF-4455242: Difference between revisions
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'''PF-4455242''' is a selective, short-acting (non-"inactivating") [[receptor antagonist|antagonist]] of the [[kappa-opioid receptor|κ-opioid receptor]].<ref name="pmid21744827">{{cite journal |vauthors=Verhoest PR, Basak AS, Parikh V, etal | title = 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 = J. Med. Chem. | volume = 54 | issue = 16 | pages = 5868–77 |date=August 2011 | pmid = 21744827 | doi = 10.1021/jm2006035 | url = }}</ref><ref name="pmid21832171">{{cite journal |vauthors=Melief EJ, Miyatake M, Carroll FI, etal | title = Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation | journal = Mol. Pharmacol. | volume = 80 | issue = 5 | pages = 920–9 |date=November 2011 | pmid = 21832171 | pmc = 3198912 | doi = 10.1124/mol.111.074195 | url = }}</ref> Discovered by [[Pfizer]] in 2009, it was pursued in a [[Phases of clinical research#Phase I|phase I]] [[clinical trial]] for the treatment of [[bipolar disorder]],<ref name="RankovicHargreaves2012">{{cite book | author1 = Zoran Rankovic | author2 = Richard Hargreaves | author3 = Matilda Bingham | title = Drug Discovery for Psychiatric Disorders | url = |
'''PF-4455242''' is a selective, short-acting (non-"inactivating") [[receptor antagonist|antagonist]] of the [[kappa-opioid receptor|κ-opioid receptor]].<ref name="pmid21744827">{{cite journal |vauthors=Verhoest PR, Basak AS, Parikh V, etal | title = 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 = J. Med. Chem. | volume = 54 | issue = 16 | pages = 5868–77 |date=August 2011 | pmid = 21744827 | doi = 10.1021/jm2006035 | url = }}</ref><ref name="pmid21832171">{{cite journal |vauthors=Melief EJ, Miyatake M, Carroll FI, etal | title = Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation | journal = Mol. Pharmacol. | volume = 80 | issue = 5 | pages = 920–9 |date=November 2011 | pmid = 21832171 | pmc = 3198912 | doi = 10.1124/mol.111.074195 | url = }}</ref> Discovered by [[Pfizer]] in 2009, it was pursued in a [[Phases of clinical research#Phase I|phase I]] [[clinical trial]] for the treatment of [[bipolar disorder]],<ref name="RankovicHargreaves2012">{{cite book | author1 = Zoran Rankovic | author2 = Richard Hargreaves | author3 = Matilda Bingham | title = Drug Discovery for Psychiatric Disorders | url = https://books.google.com/books?id=J4Mq3Lm1R7kC&pg=PA314 | year = 2012 | publisher = Royal Society of Chemistry | isbn = 978-1-84973-365-6 | pages = 314–317}}</ref> and was also investigated as a treatment for [[depression (mood)|depression]] and [[substance abuse]].<ref name="AllertonFox2013">{{cite book | author1 = Charlotte Allerton | author2 = David Fox | title = Pain Therapeutics: Current and Future Treatment Paradigms | url = https://books.google.com/books?id=zUINAgAAQBAJ&pg=PA50 | year = 2013 | publisher = Royal Society of Chemistry | isbn = 978-1-84973-645-9 | page = 50}}</ref> However, development was stopped in September 2010 due to [[toxicology]] findings in animals that had been exposed to the drug for three months.<ref name="RankovicHargreaves2012" /> |
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==See also== |
==See also== |
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Revision as of 06:12, 23 October 2016
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| Routes of administration | Oral |
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| Formula | C21H28N2O2S |
| Molar mass | 372.524 g/mol g·mol−1 |
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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
References
- ^ Verhoest PR, Basak AS, Parikh V, et al. (August 2011). "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)". J. Med. Chem. 54 (16): 5868–77. doi:10.1021/jm2006035. PMID 21744827.
- ^ Melief EJ, Miyatake M, Carroll FI, et al. (November 2011). "Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation". Mol. Pharmacol. 80 (5): 920–9. doi:10.1124/mol.111.074195. PMC 3198912. PMID 21832171.
- ^ a b Zoran Rankovic; Richard Hargreaves; Matilda Bingham (2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 314–317. ISBN 978-1-84973-365-6.
- ^ Charlotte Allerton; David Fox (2013). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. p. 50. ISBN 978-1-84973-645-9.
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