Cytisine - From the Past to the Future
| Autor: | Agata Bielecka-Dąbrowa, Paulina Gąsiorek, Aleksandra Paduszyńska, Marek Dąbrowa, Maciej Banach, Jacek Rysz |
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| Rok vydání: | 2018 |
| Předmět: |
Agonist
medicine.drug_class Pharmacology Receptors Nicotinic 01 natural sciences Partial agonist Nicotine 03 medical and health sciences Cytisine chemistry.chemical_compound Alkaloids Drug Discovery medicine Animals Humans Nicotinic Agonists Receptor 030304 developmental biology 0303 health sciences business.industry Azocines Antidepressive Agents 0104 chemical sciences 010404 medicinal & biomolecular chemistry Nicotinic agonist Neuroprotective Agents chemistry Diabetes Mellitus Type 2 Antidepressant business Ion channel linked receptors Quinolizines medicine.drug |
| Zdroj: | Current pharmaceutical design. 24(37) |
| ISSN: | 1873-4286 |
| Popis: | Introduction Neuronal nicotinic acetylcholine receptors are ligand-gated ion channel receptors, distributed throughout central nervous system, as well as in peripheral ganglia and some non-neuronal cells. Cytisine, a qulinolizidine alkaloid, could be considered a high affinity ligand of those receptors. It is a partial agonist of β2*-containing receptors and a full agonist of α7 and β4*-containing receptors. Current indication At present, pharmacodynamic properties of cytisine are leveraged only in a few European countries where it is available as medicinal product (Desmoxan and Tabex) indicated in the pharmacotherapy of nicotine addiction. Cytisine mimics the influence of nicotine on α4β2* receptors, but with higher affinity and lower activity. It lowers rewarding and reinforcing effects of nicotine in smoking persons and reduces withdrawal symptoms and craving in quitting ones. Potential indications The results of non-clinical studies suggest that cytisine could affect ethanol consumption, has an antidepressant and neuroprotective effect and could be useful in reducing body mass and preventing weight gain. Although there is a lack of research on cytisine in the treatment of areca nuts usage, the preliminary data suggest its usefulness. The combination of cytisine and Trolox C was selected as a possible effective treatment for type 2 diabetes. Though these drugs alone are not effective, their theoretical usefulness was confirmed in animal models. Summary Treatment with cytisine is an effective, cost-efficient, affordable and well tolerated nicotine addiction therapy. Potential new indications for cytisine include the treatment of alcoholism, areca nuts usage, Parkinson's disease, an autonomic-system failure. Further studies are necessary. |
| Databáze: | OpenAIRE |
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