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1.	Solmi, M, et al. (author) 2022 In: Journal of affective disorders. - : Elsevier BV. - 1573-2517 .- 0165-0327. ; 299, s. 367-376 Journal article (peer-reviewed)
2.	Veronese, N, et al. (author) Physical activity and exercise for the prevention and management of mild cognitive impairment and dementia: a collaborative international guideline 2023 In: European geriatric medicine. - 1878-7649 .- 1878-7657. ; 14:5, s. 925-952 Journal article (peer-reviewed)
3.	Deplano, Alessandro, et al. (author) Novel propanamides as fatty acid amide hydrolase inhibitors 2017 In: European Journal of Medicinal Chemistry. - : Elsevier. - 0223-5234 .- 1768-3254. ; 136, s. 523-542 Journal article (peer-reviewed)abstract Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroary1)-2-(4(2-(trifluoromethyl)pyridin-4-y0amino)phenyl)propanamides, as FAAH inhibitors. Enzymatic assays showed potencies toward FAAH ranging from nanomolar to micromolar range, and the most compounds lack activity toward the two isoforms of cyclooxygenase. Extensive structure-activity studies and the definition of the binding mode for the lead compound of the series are also presented. Kinetic assays in rat and mouse FAAH on selected compounds of the series demonstrated that slight modifications of the chemical structure could influence the binding mode and give rise to competitive (TPA1) or noncompetitive (TPA14) inhibition modes.

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Type of publication: journal article (3)

Type of content: peer-reviewed (3)

Author/Editor: Solmi, M (2); Fusar-Poli, P (2); Brambilla, P (1); Kishimoto, T. (1); Yu, X. (1); Kim, M. (1); show more...; De Leo, D (1); Koyanagi, A (1); Sadeghi, M (1); Seedat, S (1); Shin, JI (1); Yang, L. (1); Lee, J. (1); Kwon, JS (1); Radua, J (1); Smith, L (1); Hamilton, J (1); Reginster, JY (1); Marx, W (1); Meyer-Lindenberg, A (1); Balazs, J (1); Bauer, M (1); Tiihonen, J (1); Pinto, D (1); Tsamakis, K (1); Soysal, P (1); Solanes, A (1); Vieta, E (1); Fullana, MA (1); Nordentoft, M (1); Fowler, Christopher ... (1); Quinn, T (1); Sowa, P (1); Estradé, A. (1); Ward, P. (1); Rubio, J. (1); Pfennig, A. (1); Brand, S (1); Verdolini, N (1); Hidalgo-Mazzei, D (1); Lopez-Jaramillo, C (1); Yatham, LN (1); Mavridis, D (1); Ng, B (1); Domschke, K (1); Firth, J (1); Carvalho, AF (1); Rosenbaum, S (1); Schuch, FB (1); Vancampfort, D (1); show less...

University: Karolinska Institutet (2); Umeå University (1); Stockholm University (1)

Language: English (3)

Research subject (UKÄ/SCB): Medical and Health Sciences (2)

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