Selective Fatty Acid Amide Hydrolase Inhibitors as Potential Novel Antiepileptic Agents.

Amidohydrolases Anticonvulsants / pharmacology Endocannabinoids Enzyme Inhibitors / pharmacology Humans Seizures
Endocannabinoid system enzyme inhibitors epilepsy fatty acid amide hydrolase seizures selective inhibitors temporal lobe epilepsy

Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
05 05 2021
Historique:
pubmed: 24 4 2021
medline: 22 6 2021
entrez: 23 4 2021
Statut: ppublish

Résumé

Temporal lobe epilepsy is the most common form of epilepsy, and current antiepileptic drugs are ineffective in many patients. The endocannabinoid system has been associated with an on-demand protective response to seizures. Blocking endocannabinoid catabolism would elicit antiepileptic effects, devoid of psychotropic effects. We herein report the discovery of selective anandamide catabolic enzyme fatty acid amide hydrolase (FAAH) inhibitors with promising antiepileptic efficacy, starting from a further investigation of our prototypical inhibitor

Identifiants

DOI: 10.1021/acschemneuro.1c00192 PMID: 33890763
pubmed: 33890763
doi: 10.1021/acschemneuro.1c00192
doi:

Substances chimiques

Anticonvulsants 0
Endocannabinoids 0
Enzyme Inhibitors 0
Amidohydrolases EC 3.5.-
fatty-acid amide hydrolase EC 3.5.1.-

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1716-1736

Auteurs

Alessandro Grillo (A)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.

Filomena Fezza (F)

Department of Experimental Medicine Tor Vergata, University of Rome, Via Montpellier 1, 00121 Rome, Italy.

Giulia Chemi (G)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0002-3868-6752

Roberto Colangeli (R)

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, MSD2080 Msida, Malta.
Department of Experimental and Clinical Medicine, Section of Neuroscience and Cell Biology, Università Politecnica delle Marche, 60126 Ancona, Italy.

Simone Brogi (S)

Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
ORCID: 0000-0001-9375-6242

Domenico Fazio (D)

European Center for Brain Research/IRCCS Santa Lucia Foundation, Via del Fosso di Fiorano 64, 00143 Rome, Italy.

Stefano Federico (S)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0002-7478-6128

Alessandro Papa (A)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.

Nicola Relitti (N)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0001-9783-8966

Roberto Di Maio (R)

Pittsburgh Institute for Neurodegenerative Diseases and Department of Neurology, University of Pittsburgh, Pittsburgh, 15261 Pennsylvania, United States.

Gianluca Giorgi (G)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0002-8817-7745

Stefania Lamponi (S)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.

Massimo Valoti (M)

Department of Life Sciences, University of Siena, Via Aldo Moro, 2, 53100 Siena, Italy.

Beatrice Gorelli (B)

Department of Life Sciences, University of Siena, Via Aldo Moro, 2, 53100 Siena, Italy.

Simona Saponara (S)

Department of Life Sciences, University of Siena, Via Aldo Moro, 2, 53100 Siena, Italy.

Mascia Benedusi (M)

Department of Biomedical and Specialist Surgical Sciences, Section of Medical Biochemistry, Molecular Biology and Genetics, University of Ferrara, 44121 Ferrara, Italy.

Alessandra Pecorelli (A)

Plants for Human Health Institute, Animal Science Department, NC Research Campus, NC State University, 600 Laureate Way, Kannapolis, 28081 North Carolina, United States.

Patrizia Minetti (P)

Sigma Tau, Via Pontina Km 30,400, 00040 Pomezia, Italy.

Giuseppe Valacchi (G)

Department of Biomedical and Specialist Surgical Sciences, Section of Medical Biochemistry, Molecular Biology and Genetics, University of Ferrara, 44121 Ferrara, Italy.
Plants for Human Health Institute, Animal Science Department, NC Research Campus, NC State University, 600 Laureate Way, Kannapolis, 28081 North Carolina, United States.
Department of Food and Nutrition, Kyung Hee University, 02447 Seoul, South Korea.

Stefania Butini (S)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0002-8471-0880

Giuseppe Campiani (G)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0001-5295-9529

Sandra Gemma (S)

Department of Excellence of Biotechnology, Chemistry and Pharmacy, 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
ORCID: 0000-0002-8313-2417

Mauro Maccarrone (M)

European Center for Brain Research/IRCCS Santa Lucia Foundation, Via del Fosso di Fiorano 64, 00143 Rome, Italy.
Department of Biotechnological and Applied Clinical Sciences, University of L'Aquila, Via Vetoio snc, 67100 L'Aquila, Italy.

Giuseppe Di Giovanni (G)

Laboratory of Neurophysiology, Department of Physiology and Biochemistry, Faculty of Medicine and Surgery, University of Malta, MSD2080 Msida, Malta.
Neuroscience Division, School of Biosciences, Cardiff University, CF10 3AT Cardiff, United Kingdom.
ORCID: 0000-0003-2006-563X

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Classifications MeSH

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Amidohydrolases › Selective Fatty Acid Amide Hydrolase...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Anticonvulsivants › Selective Fatty Acid Amide Hydrolase...
questionsmedicales.fr › Lipides › Acides gras › Endocannabinoïdes › Selective Fatty Acid Amide Hydrolase...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Selective Fatty Acid Amide Hydrolase...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Selective Fatty Acid Amide Hydrolase...
questionsmedicales.fr › États, signes et symptômes pathologiques › Signes et symptômes › Manifestations neurologiques › Crises épileptiques › Selective Fatty Acid Amide Hydrolase...