GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol

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...
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Gespeichert in:

Autor*in:	Gabriele Ruffolo [verfasserIn] Alessandro Gaeta [verfasserIn] Beatrice Cannata [verfasserIn] Camilla Pinzaglia [verfasserIn] Eleonora Aronica [verfasserIn] Alessandra Morano [verfasserIn] Pierangelo Cifelli [verfasserIn] Eleonora Palma [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	GABA neurophysiology epilepsy

Übergeordnetes Werk:	In: Life - MDPI AG, 2012, 12(2022), 12, p 2042
Übergeordnetes Werk:	volume:12 ; year:2022 ; number:12, p 2042

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/life12122042

Katalog-ID:	DOAJ083045104

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author	Gabriele Ruffolo
spellingShingle	Gabriele Ruffolo misc GABA<sub<A</sub< receptor misc neurophysiology misc epilepsy misc Science misc Q GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol
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topic_title	GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol GABA<sub<A</sub< receptor neurophysiology epilepsy
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title	GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol
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title_sort	gabaergic neurotransmission in human tissues is modulated by cannabidiol
title_auth	GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol
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 <i<Xenopus</i< 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<sub<A</sub< receptor subunits, we found that α1β2 receptors are still affected by CBD, while classical benzodiazepine lost its efficacy as expected.
abstractGer	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 <i<Xenopus</i< 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<sub<A</sub< receptor subunits, we found that α1β2 receptors are still affected by CBD, while classical benzodiazepine lost its efficacy as expected.
abstract_unstemmed	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 <i<Xenopus</i< 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<sub<A</sub< receptor subunits, we found that α1β2 receptors are still affected by CBD, while classical benzodiazepine lost its efficacy as expected.
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title_short	GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol
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GABAergic Neurotransmission in Human Tissues Is Modulated by Cannabidiol

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