Picamilon
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Picamilon
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| Systematic (IUPAC) name | |
| 4-(pyridine-3-carbonylamino)butanoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | N |
| PubChem | |
| Chemical data | |
| Formula | C10H12N2O3 |
| Mol. mass | 208.214 g/mol |
| SMILES | & |
| Synonyms | nicotinoyl-GABA |
| Pharmacokinetic data | |
| Bioavailability | 50%–88% |
| Metabolism | ? |
| Half life | 30 minutes |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Unscheduled |
| Routes | Oral |
Picamilon (also known as nicotinoyl-GABA) is a compound formed by reacting niacin with GABA. It was developed in Japan as a prodrug of GABA[1] and further studied in Russia.[2]
[edit] Mechanism of action and potential therapeutic applications
Picamilon is able to cross the blood-brain barrier[3] and then is hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[4] The second released component, niacin acts as a strong vasodilator,[5] which might be useful for the treatment of migraine headaches.[6][7]
[edit] References
- ^ 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.
- ^ Mirzoian RS, Gan'shina TS (1989). "[The new cerebrovascular preparation pikamilon]" (in Russian). Farmakologiia i toksikologiia 52 (1): 23–6. PMID 2707413.
- ^ 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. 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:. 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:. PMID 15673472.
[edit] External links
- MeSH nicotinoyl-GABA
- A.L. Karayev. Picamilon introduction. Retrieved on 2008-05-28.
- R.P. Kruglikova (July 1997). How And Why Picamilon Works. Life Extension Magazine. Retrieved on 2008-05-28.
