Enhanced brain penetration of hexamethonium in complexes with derivatives of fullerene C60
| Autor: | A. Yu. Bespalov, D. N. Nikolaev, E. E. Yakovleva, L. B. Piotrovskiy, E. V. Litasova, Olga A. Dravolina, M. A. Dumpis |
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| Rok vydání: | 2015 |
| Předmět: |
Male
Nicotine Fullerene Biophysics 02 engineering and technology Hexamethonium Compounds Nicotinic Antagonists Pharmacology digestive system Biochemistry 03 medical and health sciences chemistry.chemical_compound Mice 0302 clinical medicine Seizures High doses medicine Animals Rats Wistar Receptor Aminocaproates Dose-Response Relationship Drug musculoskeletal neural and ocular physiology Brain General Chemistry General Medicine Penetration (firestop) 021001 nanoscience & nanotechnology Locomotor stimulation chemistry Drug delivery Hexamethonium Anticonvulsants Fullerenes 0210 nano-technology 030217 neurology & neurosurgery Locomotion medicine.drug |
| Zdroj: | Doklady. Biochemistry and biophysics. 468(1) |
| ISSN: | 1608-3091 |
| Popis: | The present report describes development of hexamethonium complexes based on fullerene C60. Hexamethonium has a limited penetration into CNS and therefore can antagonize central effects of nicotine only when given at high doses. In the present studies conducted in laboratory rodents, intraperitoneal administration of hexamethonium-fullerene complexes blocked effects of nicotine (convulsions and locomotor stimulation). When compared to equimolar doses of hexamethonium, complexes of hexamethonium with derivatives of fullerene C60 were 40 times more potent indicating an enhanced ability to interact with central nicotine receptors. Thus, fullerene C60 derivatives should be explored further as potential carrier systems for polar drug delivery into CNS. |
| Databáze: | OpenAIRE |
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