Picamilon

Picamilon

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 Y
ATC code	N02CX
PubChem	CID 60608
ChemSpider	54634 Y
Synonyms	nicotinoyl-GABA
Chemical data
Formula	C10H12N2O3
Mol. mass	208.214 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C10H12N2O3/c13-9(14)4-2-6-12-10(15)8-3-1-5-11-7-8/h1,3,5,7H,2,4,6H2,(H,12,15)(H,13,14) Y Key:NAJVRARAUNYNDX-UHFFFAOYSA-N Y
Y(what is this?)  (verify)

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.

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]

Medical use in Russia

In Russia, Picamilon is used for treatment of these illness.^[10]

1. Violations of cerebral blood flow (ischemic acute, subacute and rehabilitation period of ischemic stroke, chronic insufficiency of cerebral blood flow);
2. Vasoneurosis;
3. Asthenia;
4. Depression;
5. Senile psychosis;
6. Alcohol (period of abstinence), acute alcohol intoxication;
7. Migraine
8. Craniocerebral trauma
9. Neuroinfections;
10. Primary open-angle glaucoma (for stabilization of visual function).

References

1. ^ 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/. 
2. ^ Kopelevich VM, Shmuylovichem LM, Trubnikov VI. ^{[citation needed]}
3. ^ Mirzoian RS, Gan'shina TS (1989). "[The new cerebrovascular preparation pikamilon]" (in Russian). Farmakologiia i toksikologiia 52 (1): 23–6. PMID 2707413. 
4. ^ 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. 
5. ^ Dorofeev BF, Kholodov LE (1991). "[Pikamilon pharmacokinetics in animals]" (in Russian). Farmakologiia i toksikologiia 54 (2): 66–9. PMID 1884802. 
6. ^ 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. 
7. ^ 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. 
8. ^ 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. 
9. ^ 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. 
10. ^ "Пикамилон". Энциклопедия лекарств. Регистр лекарственных средств России. http://www.rlsnet.ru/tn_index_id_5545.htm. 

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