Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels
γ-Ethyl-γ-phenyl-butyrolactone (EFBL) is a structural combination of the anticonvulsant γ-hydroxy-γ-ethyl-γ-phenylbutyramide (HEPB) and the hypnotic γ-butyrolactone (GBL), which inherits both properties. To clarify its mechanism of action, the effects of EFBL, GBL and HEPB on dopamine (DA) and norad...
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2017-06-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2017-0014 |
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| author | Rasgado Lourdes A. Vega Villanueva Iván Díaz Fernando Vega |
| author_facet | Rasgado Lourdes A. Vega Villanueva Iván Díaz Fernando Vega |
| author_sort | Rasgado Lourdes A. Vega |
| collection | DOAJ |
| description | γ-Ethyl-γ-phenyl-butyrolactone (EFBL) is a structural combination of the anticonvulsant γ-hydroxy-γ-ethyl-γ-phenylbutyramide (HEPB) and the hypnotic γ-butyrolactone (GBL), which inherits both properties. To clarify its mechanism of action, the effects of EFBL, GBL and HEPB on dopamine (DA) and noradrenaline (NA) brain levels were investigated. Influences of chlorpromazine, phenelzine and aminooxyacetic acid were also studied. EFBL increased DA in a dose-dependent manner, remaining enhanced by 80 % over a period of 24 h and augmented NA by 54 % one hour after treatment. HEPB increased DA and NA approximately 2-fold after the first hour. GBL raised DA and NA after three and 24 h, resp. EFBL reversed chlorpromazine effects but potentiated those of phenelzine on DA. Amino-oxyacetic modified neither DA nor NA brain levels, not even in the presence of EFBL. The anticonvulsant and hypnotic properties of EFBL are attributed to its effect on presynaptic dopaminergic receptors and its lasting effect on ethyl and phenyl radicals that hinder its degradation. The results support the role of DA and NA in regulating seizure activity in the brain and indicate that EFBL offers a potential treatment for refractory epilepsy without complementary drugs and Parkinson’s disease, without the drawbacks of oral therapies. |
| format | Article |
| id | doaj-art-cd9353bb29b147ffa5f1bfcb5d0f3f14 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2017-06-01 |
| publisher | Sciendo |
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| series | Acta Pharmaceutica |
| spelling | doaj-art-cd9353bb29b147ffa5f1bfcb5d0f3f142025-02-02T09:44:22ZengSciendoActa Pharmaceutica1846-95582017-06-0167221522610.1515/acph-2017-0014acph-2017-0014Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levelsRasgado Lourdes A. Vega0Villanueva Iván1Díaz Fernando Vega2Laboratorio de Neuroquímica Departamento de Bioquímica Escuela Nacional de Ciencias Biológica Instituto Politécnico Nacional Carpio y Plan de Ayala S/N Colonia Casco de Santo Tomás C.P. 11340, México, D.F., MéxicoDepartamento de Fisiología Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Carpio y Plan de Ayala S/N Colonia Casco de Santo Tomás C.P. 11340, México, D.F., MéxicoLaboratorio de Neuroquímica Departamento de Bioquímica Escuela Nacional de Ciencias Biológica Instituto Politécnico Nacional Carpio y Plan de Ayala S/N Colonia Casco de Santo Tomás C.P. 11340, México, D.F., Méxicoγ-Ethyl-γ-phenyl-butyrolactone (EFBL) is a structural combination of the anticonvulsant γ-hydroxy-γ-ethyl-γ-phenylbutyramide (HEPB) and the hypnotic γ-butyrolactone (GBL), which inherits both properties. To clarify its mechanism of action, the effects of EFBL, GBL and HEPB on dopamine (DA) and noradrenaline (NA) brain levels were investigated. Influences of chlorpromazine, phenelzine and aminooxyacetic acid were also studied. EFBL increased DA in a dose-dependent manner, remaining enhanced by 80 % over a period of 24 h and augmented NA by 54 % one hour after treatment. HEPB increased DA and NA approximately 2-fold after the first hour. GBL raised DA and NA after three and 24 h, resp. EFBL reversed chlorpromazine effects but potentiated those of phenelzine on DA. Amino-oxyacetic modified neither DA nor NA brain levels, not even in the presence of EFBL. The anticonvulsant and hypnotic properties of EFBL are attributed to its effect on presynaptic dopaminergic receptors and its lasting effect on ethyl and phenyl radicals that hinder its degradation. The results support the role of DA and NA in regulating seizure activity in the brain and indicate that EFBL offers a potential treatment for refractory epilepsy without complementary drugs and Parkinson’s disease, without the drawbacks of oral therapies.https://doi.org/10.1515/acph-2017-0014γ-ethyl-γ-phenyl-butyrolactone (efbl)anticonvulsanthypnoticmouse braincatecholamine |
| spellingShingle | Rasgado Lourdes A. Vega Villanueva Iván Díaz Fernando Vega Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels Acta Pharmaceutica γ-ethyl-γ-phenyl-butyrolactone (efbl) anticonvulsant hypnotic mouse brain catecholamine |
| title | Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels |
| title_full | Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels |
| title_fullStr | Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels |
| title_full_unstemmed | Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels |
| title_short | Effect of γ-ethyl-γ-phenyl-butyrolactone (EFBL), anticonvulsant and hypnotic drug, on mouse brain catecholamine levels |
| title_sort | effect of γ ethyl γ phenyl butyrolactone efbl anticonvulsant and hypnotic drug on mouse brain catecholamine levels |
| topic | γ-ethyl-γ-phenyl-butyrolactone (efbl) anticonvulsant hypnotic mouse brain catecholamine |
| url | https://doi.org/10.1515/acph-2017-0014 |
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