| 词条 | Picamilon |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464206196 | IUPAC_name = 4-(Pyridine-3-carbonylamino)butanoic acid | image = Picamilon2d.png | image2 = Picamilon3d.png | tradename = НПК ЭХО | pregnancy_AU = | pregnancy_US = | legal_US = Not FDA approved; unscheduled | legal_status = RU: OTC | routes_of_administration = Oral | bioavailability = 50%–88% | metabolism = | elimination_half-life = 30 minutes | excretion = Renal | CAS_number_Ref = {{cascite|correct|CAS}} | CAS_number = 34562-97-5 | ATC_prefix = N | ATC_suffix = 02CX | ATC_supplemental = | PubChem = 60608 | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 0S5N9SEK4N | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 54634 | C=10 | H=12 | N=2 | O=3 | smiles = O=C(NCCCC(=O)O)c1cccnc1 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = NAJVRARAUNYNDX-UHFFFAOYSA-N | synonyms = nicotinoyl-GABA }}Picamilon (also known as N-nicotinoyl-GABA, pycamilon, and pikamilon) is a drug formed by a synthetic combination of niacin and γ-aminobutyric acid (GABA). It was developed in the Soviet Union in 1969[1] and further studied in both Russia[2] and Japan as a prodrug of GABA.[3] In Russia, picamilon is sold as a prescription drug. The rights to the drug belong to the Russian pharmaceutical company NPK ECHO ("НПК ЭХО"). It is not approved for sale in the United States and has been deemed an adulterating agent in dietary supplements,[4] with five American companies required to remove their picamilon products from the market in November, 2015.[5] Mechanism of action and potential therapeutic applicationsOne study in animals showed that picamilon permeated the blood–brain barrier[6] and then is hydrolyzed into GABA and niacin.[7] The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response.[8] The second released component, niacin, is a vasodilator.[9][10] Detection in biological fluidsPlasma picamilon concentrations are generally in the 500–3000 μg/L range during the first few hours after single oral doses of 50–200 mg with a half-life of 1–2 hours.[11] The drug undergoes hydrolysis to GABA and nicotinic acid. Urinary excretion of parent drug and the two metabolites accounts for up to 79% of a single dose.[11] RegulationIn the United States, the Food and Drug Administration ruled in 2015 that picamilon does not fit any of the dietary ingredient categories in the Dietary Supplement Health and Education Act of 1994,[5][12] namely that it is not a vitamin; a dietary mineral; an herb or other botanical; an amino acid; a dietary substance for use by humans to supplement the diet by increasing the total dietary intake; or a concentrate, metabolite, constituent, extract, or combination of any ingredient described above. It is not clear if this has led to the removal of picamilon as a pure substance or from various supplements manufactured in the US.[4][5][13] References1. ^{{cite journal | vauthors = Kopelevich VM, Gunar VI | title = Some approaches to the directed search for new drugs based on nicotinic acid | journal = Pharmaceutical Chemistry Journal | volume = 33 | issue = 4 | pages = 177–187 |date=April 1999 | pmid = | doi = 10.1007/BF02509934 | url = http://www.springerlink.com/content/r8430r0l4x596027/ }} 2. ^{{cite journal | vauthors = Mirzoian RS, Gan'shina TS | title = [The new cerebrovascular preparation pikamilon] | language = Russian | journal = Farmakologiia I Toksikologiia | volume = 52 | issue = 1 | pages = 23–6 | year = 1989 | pmid = 2707413 | doi = }} 3. ^{{cite journal | vauthors = Matsuyama K, Yamashita C, Noda A, Goto S, Noda H, Ichimaru Y, Gomita Y | title = Evaluation of isonicotinoyl-gamma-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA | journal = Chemical & Pharmaceutical Bulletin | volume = 32 | issue = 10 | pages = 4089–95 | date = October 1984 | pmid = 6529802 | doi = 10.1248/cpb.32.4089 | url = http://www.journalarchive.jst.go.jp/english/jnlabstract_en.php?cdjournal=cpb1958&cdvol=32&noissue=10&startpage=4089 }} 4. ^1 {{cite journal | vauthors = Avula B, Chittiboyina AG, Sagi S, Wang YH, Wang M, Khan IA, Cohen PA | title = Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States | journal = Drug Testing and Analysis | volume = 8 | issue = 3-4 | pages = 334–43 | date = March 2016 | pmid = 26426301 | doi = 10.1002/dta.1853 }} 5. ^1 2 {{cite web | url = http://www.nutraingredients-usa.com/Regulation/FDA-sends-five-warning-letters-over-supplements-containing-picamilon/?c=7InNqGv0AjdjxWpyk%2BfGQw%3D%3D&p2= | title = FDA sends five warning letters over supplements containing picamilon | date = 2 December 2015 | publisher = NutraIngredients-USA.com, William Reed Business Media|access-date=3 December 2015}} 6. ^{{cite journal | vauthors = Dorofeev BF, Kholodov LE | title = [Pikamilon pharmacokinetics in animals] | language = Russian | journal = Farmakologiia I Toksikologiia | volume = 54 | issue = 2 | pages = 66–9 | year = 1991 | pmid = 1884802 | doi = }} 7. ^{{cite web|url=http://picamilon.org/|title=Technical Description of Picamilon}} 8. ^{{cite journal | vauthors = Shephard RA | title = Behavioral effects of GABA agonists in relation to anxiety and benzodiazepine action | journal = Life Sciences | volume = 40 | issue = 25 | pages = 2429–36 | date = June 1987 | pmid = 2884549 | doi = 10.1016/0024-3205(87)90758-2 }} 9. ^{{cite journal | vauthors = Gille A, Bodor ET, Ahmed K, Offermanns S | title = Nicotinic acid: pharmacological effects and mechanisms of action | journal = Annual Review of Pharmacology and Toxicology | volume = 48 | issue = | pages = 79–106 | year = 2008 | pmid = 17705685 | doi = 10.1146/annurev.pharmtox.48.113006.094746 }} 10. ^{{cite journal | vauthors = Prousky J, Seely D | title = The treatment of migraines and tension-type headaches with intravenous and oral niacin (nicotinic acid): systematic review of the literature | journal = Nutrition Journal | volume = 4 | issue = | pages = 3 | date = January 2005 | pmid = 15673472 | pmc = 548511 | doi = 10.1186/1475-2891-4-3 }} 11. ^1 {{cite journal | vauthors = Cui W, Chen X, Zhan Y, Zhang Z, Zhang Y, Zhong D | title = Determination of picamilon concentration in human plasma by liquid chromatography-tandem mass spectrometry | journal = Journal of Chromatography B | volume = 878 | issue = 15-16 | pages = 1181–4 | date = May 2010 | pmid = 20359966 | doi = 10.1016/j.jchromb.2010.03.013 }} 12. ^{{cite web | last1 = Welch | first1 = Cara| name-list-format = vanc | title = Declaration of Dr. Cara Welch|url=https://blog.priceplow.com/wp-content/uploads/Picamilon-FDA_Ruling-20150928.pdf|publisher=Department of Health and Human Services|access-date=21 October 2015}} 13. ^{{cite web | last1 = Roberto | first1 = Mike | name-list-format = vanc | title = Picamilon Under FDA Attack | url = https://blog.priceplow.com/supplement-news/picamilon-fda|website=PricePlow | access-date = 21 October 2015 | date = 13 October 2015 }} External links
9 : Anxiolytics|Nicotinamides|GABA analogues|GABAA receptor agonists|GABAA-rho receptor agonists|GABAB receptor agonists|Russian drugs|Prodrugs|Drugs in the Soviet Union |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。