The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment
Epilepsy is characterized by repeated spontaneous bursts of neuronal hyperactivity and high synchronization in the central nervous system. It seriously affects the quality of life of epileptic patients, and nearly 30% of individuals are refractory to treatment of antiseizure drugs. Therefore, there...
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| Format: | Article |
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MDPI AG
2021-08-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/22/16/8961 |
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| author | Xiaoyu Ji Yang Zeng Jie Wu |
| author_facet | Xiaoyu Ji Yang Zeng Jie Wu |
| author_sort | Xiaoyu Ji |
| collection | DOAJ |
| description | Epilepsy is characterized by repeated spontaneous bursts of neuronal hyperactivity and high synchronization in the central nervous system. It seriously affects the quality of life of epileptic patients, and nearly 30% of individuals are refractory to treatment of antiseizure drugs. Therefore, there is an urgent need to develop new drugs to manage and control refractory epilepsy. Cannabinoid ligands, including selective cannabinoid receptor subtype (CB<sub>1</sub> or CB<sub>2</sub> receptor) ligands and non-selective cannabinoid (synthetic and endogenous) ligands, may serve as novel candidates for this need. Cannabinoid appears to regulate seizure activity in the brain through the activation of CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors (CB<sub>1</sub>R and CB<sub>2</sub>R). An abundant series of cannabinoid analogues have been tested in various animal models, including the rat pilocarpine model of acquired epilepsy, a pentylenetetrazol model of myoclonic seizures in mice, and a penicillin-induced model of epileptiform activity in the rats. The accumulating lines of evidence show that cannabinoid ligands exhibit significant benefits to control seizure activity in different epileptic models. In this review, we summarize the relationship between brain CB<sub>2</sub> receptors and seizures and emphasize the potential mechanisms of their therapeutic effects involving the influences of neurons, astrocytes, and microglia cells. The unique features of CB<sub>2</sub>Rs, such as lower expression levels under physiological conditions and high inducibility under epileptic conditions, make it an important target for future research on drug-resistant epilepsy. |
| first_indexed | 2024-03-10T08:43:44Z |
| format | Article |
| id | doaj.art-3d8183ca1f1544668ca53fd81df6dc5c |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T08:43:44Z |
| publishDate | 2021-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-3d8183ca1f1544668ca53fd81df6dc5c2023-11-22T08:03:16ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-08-012216896110.3390/ijms22168961The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy TreatmentXiaoyu Ji0Yang Zeng1Jie Wu2Brain Function and Disease Laboratory, Shantou University Medical College, Xin-Ling Road #22, Shantou 515041, ChinaMedical Education Assessment and Research Center, Shantou University Medical College, Xin-Ling Road #22, Shantou 515041, ChinaBrain Function and Disease Laboratory, Shantou University Medical College, Xin-Ling Road #22, Shantou 515041, ChinaEpilepsy is characterized by repeated spontaneous bursts of neuronal hyperactivity and high synchronization in the central nervous system. It seriously affects the quality of life of epileptic patients, and nearly 30% of individuals are refractory to treatment of antiseizure drugs. Therefore, there is an urgent need to develop new drugs to manage and control refractory epilepsy. Cannabinoid ligands, including selective cannabinoid receptor subtype (CB<sub>1</sub> or CB<sub>2</sub> receptor) ligands and non-selective cannabinoid (synthetic and endogenous) ligands, may serve as novel candidates for this need. Cannabinoid appears to regulate seizure activity in the brain through the activation of CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors (CB<sub>1</sub>R and CB<sub>2</sub>R). An abundant series of cannabinoid analogues have been tested in various animal models, including the rat pilocarpine model of acquired epilepsy, a pentylenetetrazol model of myoclonic seizures in mice, and a penicillin-induced model of epileptiform activity in the rats. The accumulating lines of evidence show that cannabinoid ligands exhibit significant benefits to control seizure activity in different epileptic models. In this review, we summarize the relationship between brain CB<sub>2</sub> receptors and seizures and emphasize the potential mechanisms of their therapeutic effects involving the influences of neurons, astrocytes, and microglia cells. The unique features of CB<sub>2</sub>Rs, such as lower expression levels under physiological conditions and high inducibility under epileptic conditions, make it an important target for future research on drug-resistant epilepsy.https://www.mdpi.com/1422-0067/22/16/8961cannabinoid receptor 2epilepsycAMPM-currentanti-inflammatory |
| spellingShingle | Xiaoyu Ji Yang Zeng Jie Wu The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment International Journal of Molecular Sciences cannabinoid receptor 2 epilepsy cAMP M-current anti-inflammatory |
| title | The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment |
| title_full | The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment |
| title_fullStr | The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment |
| title_full_unstemmed | The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment |
| title_short | The CB<sub>2</sub> Receptor as a Novel Therapeutic Target for Epilepsy Treatment |
| title_sort | cb sub 2 sub receptor as a novel therapeutic target for epilepsy treatment |
| topic | cannabinoid receptor 2 epilepsy cAMP M-current anti-inflammatory |
| url | https://www.mdpi.com/1422-0067/22/16/8961 |
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