Chemistry:Zelatriazin
From HandWiki
Short description: Chemical compound
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| Other names | NBI-1065846; TAK-041 |
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| Formula | C18H15F3N4O3 |
| Molar mass | 392.338 g·mol−1 |
Zelatriazin (NBI-1065846 or TAK-041) is a small-molecule agonist of GPR139. It was developed for schizophrenia and anhedonia in depression but trials were unsuccessful and its development was discontinued in 2023.[1][2][3][4][5][6][7]
References
- ↑ Kamel, Amin; Bowlin, Steve; Hosea, Natalie; Arkilo, Dimitrios; Laurenza, Antonio (February 2021). "In Vitro Metabolism of Slowly Cleared G Protein–Coupled Receptor 139 Agonist TAK-041 Using Rat, Dog, Monkey, and Human Hepatocyte Models (HepatoPac): Correlation with In Vivo Metabolism". Drug Metabolism and Disposition 49 (2): 121–132. doi:10.1124/dmd.120.000246. PMID 33273044.
- ↑ Schiffer, Hans; Atienza, Josephine; Reichard, Holly; Mulligan, Victoria; Cilia, Jackie; Monenschein, Holger; Collia, Deanna; Ray, Jim et al. (18 May 2020). "S180. The Selective Gpr139 Agonist Tak-041 Reverses Anhedonia and Social Interaction Deficits in Rodent Models Related to Negative Symptoms in Schizophrenia". Schizophrenia Bulletin 46 (Supplement_1): S106–S107. doi:10.1093/schbul/sbaa031.246.
- ↑ Yin, Wei; Han, David; Khudyakov, Polyna; Behrje, Rhett; Posener, Joel; Laurenza, Antonio; Arkilo, Dimitrios (August 2022). "A phase 1 study to evaluate the safety, tolerability and pharmacokinetics of TAK-041 in healthy participants and patients with stable schizophrenia". British Journal of Clinical Pharmacology 88 (8): 3872–3882. doi:10.1111/bcp.15305. PMID 35277995.
- ↑ Rabiner, Eugenii A.; Uz, Tolga; Mansur, Ayla; Brown, Terry; Chen, Grace; Wu, Jingtao; Atienza, Joy; Schwarz, Adam J. et al. (June 2022). "Endogenous dopamine release in the human brain as a pharmacodynamic biomarker: evaluation of the new GPR139 agonist TAK-041 with [11CPHNO PET"]. Neuropsychopharmacology 47 (7): 1405–1412. doi:10.1038/s41386-021-01204-1. PMID 34675381.
- ↑ Reichard, Holly A.; Schiffer, Hans H.; Monenschein, Holger; Atienza, Josephine M.; Corbett, Gerard; Skaggs, Alton W.; Collia, Deanna R.; Ray, William J. et al. (12 August 2021). "Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia". Journal of Medicinal Chemistry 64 (15): 11527–11542. doi:10.1021/acs.jmedchem.1c00820. PMID 34260228.
- ↑ Münster, Alexandra; Sommer, Susanne; Kúkeľová, Diana; Sigrist, Hannes; Koros, Eliza; Deiana, Serena; Klinder, Klaus; Baader-Pagler, Tamara et al. (August 2022). "Effects of GPR139 agonism on effort expenditure for food reward in rodent models: Evidence for pro-motivational actions". Neuropharmacology 213: 109078. doi:10.1016/j.neuropharm.2022.109078. PMID 35561791.
- ↑ Taylor, Nick Paul (10 November 2023). "Neurocrine hit with one-two punch as Takeda and Xenon pacts deliver midphase flops". Fierce Biotech. https://www.fiercebiotech.com/biotech/neurocrine-hit-1-2-punch-takeda-and-xenon-pacts-deliver-midphase-flops.
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