CVN45502

CVN45502
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name N-[(1S,2S)-2-Methyl-2-[[5-(trifluoromethyl)pyrazin-2-yl]amino]cyclopentyl]-3-(triazol-2-yl)pyridine-2-carboxamide;
PubChem CID	118308152;
Chemical and physical data
Formula	C19H19F3N8O
Molar mass	432.411 g·mol−1

CVN45502 is a selective hypocretin (orexin) receptor 1 antagonist. It significantly reduces food intake and body weight in a mouse model of obesity.^[1] Although HCRTR1 variants are significantly correlated with body weight in humans, it is not known if the drug has psychiatric side effects or could be combined with GLP-1 agonists.^[2]

References[edit]

^ Schneeberger, Marc; Brice, Nicola L.; Pellegrino, Kyle; Parolari, Luca; Shaked, Jordan T.; Page, Keith J.; Marchildon, François; Barrows, Douglas W.; Carroll, Thomas S.; Topilko, Thomas; Mulligan, Victoria M.; Newman, Robert; Doyle, Kevin; Bürli, Roland; Barker, Daniel F.; Glen, Angela; Ortuño, María José; Nectow, Alexander R.; Renier, Nicolas; Cohen, Paul; Carlton, Mark; Heintz, Nathaniel; Friedman, Jeffrey M. (November 2022). "Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction". Nature Metabolism. 4 (11): 1495–1513. doi:10.1038/s42255-022-00677-8. ISSN 2522-5812. PMC 9684079.
^ Tsang, Anthony; Blouet, Clemence (April 2023). "A pipeline for identification and validation of brain targets for weight loss". Nature Reviews Endocrinology. 19 (4): 190–191. doi:10.1038/s41574-023-00803-w. ISSN 1759-5037.

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[1] Schneeberger, Marc; Brice, Nicola L.; Pellegrino, Kyle; Parolari, Luca; Shaked, Jordan T.; Page, Keith J.; Marchildon, François; Barrows, Douglas W.; Carroll, Thomas S.; Topilko, Thomas; Mulligan, Victoria M.; Newman, Robert; Doyle, Kevin; Bürli, Roland; Barker, Daniel F.; Glen, Angela; Ortuño, María José; Nectow, Alexander R.; Renier, Nicolas; Cohen, Paul; Carlton, Mark; Heintz, Nathaniel; Friedman, Jeffrey M. (November 2022). "Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction". Nature Metabolism. 4 (11): 1495–1513. doi:10.1038/s42255-022-00677-8. ISSN 2522-5812. PMC 9684079.

[2] Tsang, Anthony; Blouet, Clemence (April 2023). "A pipeline for identification and validation of brain targets for weight loss". Nature Reviews Endocrinology. 19 (4): 190–191. doi:10.1038/s41574-023-00803-w. ISSN 1759-5037.

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