Chemistry:AMG-517
From HandWiki
Short description: Chemical compound
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| Formula | C20H13F3N4O2S |
| Molar mass | 430.41 g·mol−1 |
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AMG-517 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel.[1][2] It was developed as a potential treatment for chronic pain, but while it was an effective analgesic in animal studies it was dropped from human clinical trials at Phase I due to producing hyperthermia as a side effect, as well as poor water solubility. It is still used in scientific research into the function of the TRPV1 channel and its role in pain and inflammation, and has been used as a template for the design of several newer analogues which have improved properties.[3][4][5][6][7]
See also
References
- ↑ "Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate". Journal of Medicinal Chemistry 50 (15): 3515–27. July 2007. doi:10.1021/jm070190p. PMID 17585750.
- ↑ "Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties". Journal of Medicinal Chemistry 50 (15): 3528–39. July 2007. doi:10.1021/jm070191h. PMID 17585751.
- ↑ "Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility". Bioorganic & Medicinal Chemistry Letters 17 (23): 6539–45. December 2007. doi:10.1016/j.bmcl.2007.09.080. PMID 17937985.
- ↑ "Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans". Pain 136 (1–2): 202–10. May 2008. doi:10.1016/j.pain.2008.01.024. PMID 18337008.
- ↑ "Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1". Trends in Pharmacological Sciences 29 (11): 550–7. November 2008. doi:10.1016/j.tips.2008.08.003. PMID 18805596.
- ↑ "Transient Receptor Potential Vanilloid 1 Antagonists Prevent Anesthesia-induced Hypothermia and Decrease Postincisional Opioid Dose Requirements in Rodents". Anesthesiology 127 (5): 813–823. November 2017. doi:10.1097/ALN.0000000000001812. PMID 28806222.
- ↑ "Thermal Hyperalgesia and Mechanical Allodynia Elicited by Histamine and Non-histaminergic Itch Mediators: Respective Involvement of TRPV1 and TRPA1". Neuroscience 449: 35–45. November 2020. doi:10.1016/j.neuroscience.2020.09.048. PMID 33010342.
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