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Endocannabinoid Degradation Enzyme Inhibitors as Potential Antipsychotics: A Medicinal Chemistry Perspective

2023Journal article Open access
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dc.contributor.authorMangiatordi, Giuseppe Felice
dc.contributor.authorCavalluzzi, Maria Maddalena
dc.contributor.authorDelre, Pietro
dc.contributor.authorLamanna, Giuseppe
dc.contributor.authorLumuscio, Maria Cristina
dc.contributor.authorSaviano, Michele
dc.contributor.authorMajoral, Jean-Pierre
dc.contributor.authorMignani, Serge
dc.contributor.authorDuranti, Andrea
dc.contributor.authorLentini, Giovanni
dc.date.accessioned2024-03-20T11:38:42Z
dc.date.available2024-03-20T11:38:42Z
dc.date.issued2023
dc.description.abstractThe endocannabinoid system (ECS) plays a very important role in numerous physiological and pharmacological processes, such as those related to the central nervous system (CNS), including learning, memory, emotional processing, as well pain control, inflammatory and immune response, and as a biomarker in certain psychiatric disorders. Unfortunately, the half-life of the natural ligands responsible for these effects is very short. This perspective describes the potential role of the inhibitors of the enzymes fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), which are mainly responsible for the degradation of endogenous ligands in psychic disorders and related pathologies. The examination was carried out considering both the impact that the classical exogenous ligands such as ∆ 9 -tetrahydrocannabinol (THC) and (−)-trans-cannabidiol (CBD) have on the ECS and through an analysis focused on the possibility of predicting the potential toxicity of the inhibitors before they are subjected to clinical studies. In particular, cardiotoxicity (hERG liability), probably the worst early adverse reaction studied during clinical studies focused on acute toxicity, was predicted, and some of the most used and robust metrics available were considered to select which of the analyzed compounds could be repositioned as possible oral antipsychotics.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationMangiatordi, G.F.; Cavalluzzi, M.M.; Delre, P.; Lamanna, G.; Lomuscio, M.C.; Saviano, M.; Majoral, J.-P.; Mignani, S.; Duranti, A.; Lentini, G. Endocannabinoid Degradation Enzyme Inhibitors as Potential Antipsychotics: A Medicinal Chemistry Perspective. Biomedicines 2023, 11, 469. https://doi.org/ 10.3390/biomedicines11020469pt_PT
dc.identifier.doi10.3390/biomedicines11020469pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.13/5607
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationMadeira Chemistry Research Centre
dc.relationMadeira Chemistry Research Centre
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectEndocannabinoid systempt_PT
dc.subjectFAAH inhibitorspt_PT
dc.subjectMGL inhibitorspt_PT
dc.subjectRepositioningpt_PT
dc.subjectDrug-likenesspt_PT
dc.subjecthERGpt_PT
dc.subjectLigand efficiency metricspt_PT
dc.subject.pt_PT
dc.subjectFaculdade de Ciências Exatas e da Engenhariapt_PT
dc.subjectCentro de Química da Madeirapt_PT
dc.titleEndocannabinoid Degradation Enzyme Inhibitors as Potential Antipsychotics: A Medicinal Chemistry Perspectivept_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00674%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F00674%2F2020/PT
oaire.citation.issue2pt_PT
oaire.citation.startPage469pt_PT
oaire.citation.titleBiomedicinespt_PT
oaire.citation.volume11pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNameMangiatordi
person.familyNameCavalluzzi
person.familyNameSaviano
person.familyNameMignani
person.familyNameDuranti
person.familyNameLentini
person.givenNameGiuseppe Felice
person.givenNameMaria Maddalena
person.givenNameMichele
person.givenNameSerge
person.givenNameAndrea
person.givenNameGiovanni
person.identifier1025037
person.identifier1013419
person.identifier42568
person.identifier.ciencia-id8018-B5D2-6983
person.identifier.orcid0000-0003-4042-2841
person.identifier.orcid0000-0002-3402-8170
person.identifier.orcid0000-0001-5086-2459
person.identifier.orcid0000-0002-1383-5256
person.identifier.orcid0000-0002-7531-4472
person.identifier.orcid0000-0001-7079-5994
person.identifier.ridG-3234-2013
person.identifier.scopus-author-id36552716300
person.identifier.scopus-author-id7102546786
person.identifier.scopus-author-id7003374430
person.identifier.scopus-author-id7004070916
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
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