Recently, the potential use of phytocannabinoids (pCBs) to treat different pathological conditions has attracted great attention in the scientific community. Among the different pCBs, cannabidiol (CBD) has showed interesting biological properties, making it a promising molecule with a high security profile that has been approved for treatment as an add-on therapy in patients afflicted by severe pharmaco-resistant epilepsy, including Dravet syndrome (DS), Lennox-Gastaut syndrome (LGS) and tuberous sclerosis complex (TSC). CBD is pharmacologically considered a "dirty drug", since it has the capacity to bind different targets and to activate several cellular pathways. GABAergic impairment is one of the key processes during the epileptogenesis period able to induce a generalized hyperexcitability of the central nervous system (CNS), leading to epileptic seizures. Here, by using the microtransplantation of human brain membranes approach in Xenopus oocytes and electrophysiological recordings, we confirm the ability of CBD to modulate GABAergic neurotransmission in human cerebral tissues obtained from patients afflicted by different forms of pharmaco-resistant epilepsies, such as DS, TSC, focal cortical dysplasia (FCD) type IIb and temporal lobe epilepsy (TLE). Furthermore, using cDNAs encoding for human GABA(A) receptor subunits, we found that alpha 1 beta 2 receptors are still affected by CBD, while classical benzodiazepine lost its efficacy as expected.

GABAergic neurotransmission in human tissues is modulated by cannabidiol / Ruffolo, Gabriele; Gaeta, Alessandro; Cannata, Beatrice; Pinzaglia, Camilla; Aronica, Eleonora; Morano, Alessandra; Cifelli, Pierangelo; Palma, Eleonora. - In: LIFE. - ISSN 2075-1729. - 12:12(2022). [10.3390/life12122042]

GABAergic neurotransmission in human tissues is modulated by cannabidiol

Gabriele Ruffolo;Alessandro Gaeta;Beatrice Cannata;Alessandra Morano;Eleonora Palma
2022

Abstract

Recently, the potential use of phytocannabinoids (pCBs) to treat different pathological conditions has attracted great attention in the scientific community. Among the different pCBs, cannabidiol (CBD) has showed interesting biological properties, making it a promising molecule with a high security profile that has been approved for treatment as an add-on therapy in patients afflicted by severe pharmaco-resistant epilepsy, including Dravet syndrome (DS), Lennox-Gastaut syndrome (LGS) and tuberous sclerosis complex (TSC). CBD is pharmacologically considered a "dirty drug", since it has the capacity to bind different targets and to activate several cellular pathways. GABAergic impairment is one of the key processes during the epileptogenesis period able to induce a generalized hyperexcitability of the central nervous system (CNS), leading to epileptic seizures. Here, by using the microtransplantation of human brain membranes approach in Xenopus oocytes and electrophysiological recordings, we confirm the ability of CBD to modulate GABAergic neurotransmission in human cerebral tissues obtained from patients afflicted by different forms of pharmaco-resistant epilepsies, such as DS, TSC, focal cortical dysplasia (FCD) type IIb and temporal lobe epilepsy (TLE). Furthermore, using cDNAs encoding for human GABA(A) receptor subunits, we found that alpha 1 beta 2 receptors are still affected by CBD, while classical benzodiazepine lost its efficacy as expected.
2022
GABAA receptor; epilepsy; neurophysiology
01 Pubblicazione su rivista::01a Articolo in rivista
GABAergic neurotransmission in human tissues is modulated by cannabidiol / Ruffolo, Gabriele; Gaeta, Alessandro; Cannata, Beatrice; Pinzaglia, Camilla; Aronica, Eleonora; Morano, Alessandra; Cifelli, Pierangelo; Palma, Eleonora. - In: LIFE. - ISSN 2075-1729. - 12:12(2022). [10.3390/life12122042]
File allegati a questo prodotto
File Dimensione Formato  
Ruffolo_GABAergic_2022.pdf

accesso aperto

Note: articolo originale
Tipologia: Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza: Creative commons
Dimensione 350.34 kB
Formato Adobe PDF
350.34 kB Adobe PDF

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1666755
Citazioni
  • ???jsp.display-item.citation.pmc??? 3
  • Scopus 8
  • ???jsp.display-item.citation.isi??? 8
social impact