Picamilon
From Wikipedia, the free encyclopedia
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| Systematic (IUPAC) name | |
| 4-(pyridine-3-carbonylamino)butanoic acid | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Unscheduled |
| Routes | Oral |
| Pharmacokinetic data | |
| Bioavailability | 50%–88% |
| Half-life | 30 minutes |
| Excretion | Renal |
| Identifiers | |
| CAS number | 34562-97-5  |
| ATC code | N02CX |
| PubChem | CID 60608 |
| ChemSpider | 54634 |
| Synonyms | nicotinoyl-GABA |
| Chemical data | |
| Formula | C10H12N2O3 |
| Mol. mass | 208.214 g/mol |
| SMILES | eMolecules & PubChem |
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Picamilon (also known as nicotinoyl-GABA, Pycamilon, Pikamilon, etc) is a dietary supplement formed by combining niacin with GABA. It was developed in the Soviet Union in 1969 by the All-Union Vitamins Scientific Research Institute[1][2] and further studied in both Russia[3] and Japan as a prodrug of GABA.[4]
Picamilon is sold in the United States as a dietary supplement, while in Russia it is sold over the counter. The rights to the drug belong to pharmaceutical company NPK ECHO ("НПК ЭХО"), Moscow, Russia.
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[edit] Mechanism of action and potential therapeutic applications
Picamilon is able to cross the blood-brain barrier[5] and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[6] The second released component, niacin acts as a strong vasodilator,[7] which might be useful for the treatment of migraine headaches.[8][9]
[edit] Medical use in Russia
In Russia, Picamilon is used for treatment of these illness.[10]
- Violations of cerebral blood flow (ischemic acute, subacute and rehabilitation period of ischemic stroke, chronic insufficiency of cerebral blood flow);
- Vasoneurosis;
- Asthenia;
- Depression;
- Senile psychosis;
- Alcohol (period of abstinence), acute alcohol intoxication;
- Migraine
- Craniocerebral trauma
- Neuroinfections;
- Primary open-angle glaucoma (for stabilization of visual function).
[edit] References
- ^ Kopelevich VM, Gunar VI (April 1999). "Some approaches to the directed search for new drugs based on nicotinic acid". Pharmaceutical Chemistry Journal 33 (4): 177–187. doi:10.1007/BF02509934. http://www.springerlink.com/content/r8430r0l4x596027/.
- ^ Kopelevich VM, Shmuylovichem LM, Trubnikov VI.[citation needed]
- ^ Mirzoian RS, Gan'shina TS (1989). "[The new cerebrovascular preparation pikamilon]" (in Russian). Farmakologiia i toksikologiia 52 (1): 23–6. PMID 2707413.
- ^ Matsuyama K, Yamashita C, Noda A, Goto S, Noda H, Ichimaru Y, Gomita Y (October 1984). "Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA". Chem. Pharm. Bull. 32 (10): 4089–95. PMID 6529802. http://www.journalarchive.jst.go.jp/english/jnlabstract_en.php?cdjournal=cpb1958&cdvol=32&noissue=10&startpage=4089.
- ^ Dorofeev BF, Kholodov LE (1991). "[Pikamilon pharmacokinetics in animals]" (in Russian). Farmakologiia i toksikologiia 54 (2): 66–9. PMID 1884802.
- ^ Shephard RA (June 1987). "Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action". Life Sci. 40 (25): 2429–36. doi:10.1016/0024-3205(87)90758-2. PMID 2884549.
- ^ Gille A, Bodor ET, Ahmed K, Offermanns S (2008). "Nicotinic acid: pharmacological effects and mechanisms of action". Annu. Rev. Pharmacol. Toxicol. 48: 79–106. doi:10.1146/annurev.pharmtox.48.113006.094746. PMID 17705685.
- ^ Pukhal'skaia TG, Maĭsov NI, Mirzoian RS (1989). "[The effect of antimigraine preparations on serotonin transport in the brain synaptosomes of rats]" (in Russian). Farmakol Toksikol 52 (6): 39–43. PMID 2625145.
- ^ Prousky J, Seely D (2005). "The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature". Nutr J 4: 3. doi:10.1186/1475-2891-4-3. PMC 548511. PMID 15673472. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=548511.
- ^ "Пикамилон". Энциклопедия лекарств. Регистр лекарственных средств России. http://www.rlsnet.ru/tn_index_id_5545.htm.
[edit] External links
- MeSH nicotinoyl-GABA
- A.L. Karayev. "Picamilon introduction". http://www.picamilon.net/picamilon/picamilon-intro.htm. Retrieved 2008-05-28.
- R.P. Kruglikova (July 1997). "How And Why Picamilon Works". Life Extension Magazine. http://www.lef.org/magazine/mag97/july-lbn297.html. Retrieved 2008-05-28.
- Erowid Picamilon experience reports
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