Tanaproget
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| Systematic (IUPAC) name | |
|---|---|
| 5-(4,4-dimethyl-2-thioxo-1,4-dihydro-2H-3,1-benzoxazin-6-yl)-1-methyl-1H-pyrrole-2-carbonitrile | |
| Clinical data | |
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| Identifiers | |
| 304853-42-7 | |
| None | |
| PubChem | CID 4369524 |
| DrugBank | DB04787 |
| ChemSpider | 3572060 |
| Chemical data | |
| Formula | C16H15N3OS |
| 297.375 g/mol | |
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SMILES
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Tanaproget (NSP-989) is a novel, non-steroidal progestin.[1] It is a high affinity, high efficacy, and very selective agonist of the progesterone receptor (PR).[1] Due to its much more selective binding profile relative to most conventional, steroidal progestins, tanaproget may prove to produce fewer side effects in comparison.[1] It is currently in the process of being developed for clinical use as a contraceptive by Ligand Pharmaceuticals.[2][3]
An analog of tanaproget, 4-fluoropropyltanaproget (18F), has been developed as a radiotracer for imaging of the PR in positron emission tomography.[4]
References
- ↑ 1.0 1.1 1.2 Zhang Z, Olland AM, Zhu Y et al. (August 2005). "Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget". J. Biol. Chem. 280 (31): 28468–75. doi:10.1074/jbc.M504144200. PMID 15937332.
- ↑ Bapst JL, Ermer JC, Ferron GM, Foss D, Orczyk GP (November 2006). "Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women". Contraception 74 (5): 414–8. doi:10.1016/j.contraception.2006.06.004. PMID 17046384.
- ↑ Bayés M, Rabasseda X, Prous JR (September 2005). "Gateways to clinical trials". Methods Find Exp Clin Pharmacol 27 (7): 505–22. PMID 16258596.
- ↑ Lee JH, Zhou HB, Dence CS, Carlson KE, Welch MJ, Katzenellenbogen JA (June 2010). "Development of [F-18]fluorine-substituted Tanaproget as a progesterone receptor imaging agent for positron emission tomography". Bioconjug. Chem. 21 (6): 1096–104. doi:10.1021/bc1001054. PMID 20496889.
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