Picamilon Struktur

Picamilon

Bezeichnung:Picamilon

CAS-Nr34562-97-5

Englisch Name:Picamilon

CBNumberCB4106397

SummenformelC10H12N2O3

Molgewicht208.21

MOL-Datei34562-97-5.mol

Picamilon physikalisch-chemischer Eigenschaften

Schmelzpunkt	211.0 to 215.0 °C
Siedepunkt	522.4±30.0 °C(Predicted)
Dichte	1.245
storage temp.	Inert atmosphere,Room Temperature
Löslichkeit	DMSO (Slightly, Heated), Methanol (Slightly)
Aggregatzustand	Solid
pka	4.60±0.10(Predicted)
Farbe	White to Off-White
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)
InChIKey	NAJVRARAUNYNDX-UHFFFAOYSA-N
SMILES	C(O)(=O)CCCNC(C1=CC=CN=C1)=O
CAS Datenbank	34562-97-5(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
HazardClass	IRRITANT
HS Code	2933599590

Picamilon Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Picamilon: an analogue of the neurotransmitter γ-aminobutyric acid (GABA)
Picamilon is a derivative of γ-aminobutyric acid (GABA) and nicotinic acid developed in 1970 by the All-Union Vitamin Research Institute to increase central nervous system (CNS) levels of γ-aminobutyric acid (GABA). Drugs that can mimic or increase GABA activity in the brain have the potential to provide anti-anxiety and anti-convulsive effects. GABA itself, when consumed orally, does not cross the blood-brain barrier. Much research has, therefore, been devoted to developing orally active agents that have GABA-like effects. Both gabapentin (a GABA analogue) and picamilon were designed to be orally administered drugs that cross the blood-brain barrier and provide inhibitory CNS effects. Picamilon, prescribed in dosages from 50 mg to 200 mg, can cross the blood-brain barrier in animal models and, once in the CNS, is hydrolyzed into GABA and nicotinic acid. The released GABA could potentially have inhibitory properties, including anti-anxiety and anti-convulsant effects. Nicotinic acid would also be released, potentially leading to dilation of CNS blood vessels. The FDA has never approved picamilon for use in the USA, but picamilon is used in Russia to treat various neurological conditions[1].
Verwenden
Nicotinoyl-γ-aminobutyric Acid is a pro-drug of γ-Aminobutyric Acid (A602920). Studies show that Nicotinoyl-γ-aminobutyric Acid is involved in the regulation of the processes in the brain of streptozotocin-induced diabetic rats.
Verwenden
anti-cancer agent
Pharmakokinetik
Because Picamilon can dramatically increase blood flow and circulation within the brain, picamilon is used as a nootropic. Also used for the treatment of depression, anxiety, and migraine, picamilon works by crossing the blood-brain barrier, after which it is hydrolyzed into GABA and nicotinic acid. In addition, picamilon has extremely low toxicity and no allergenic or carcinogenic properties. An animal study has shown that picamilon is rapidly absorbed (Tmax = 0.23 h) and penetrates well through the blood-brain barrier in mice. At oral administration, the drug bioavailability in mice was 21.9% and in rats between 53% and 78.9%[2].
Einzelnachweise
[1] Bharathi Avula. “Identification and quantification of vinpocetine and picamilon in dietary supplements sold in the United States.” Drug Testing and Analysis 8 3–4 (2015): 334–343.
[2] Wenqi Cui . “Determination of picamilon concentration in human plasma by liquid chromatography–tandem mass spectrometry.” Journal of Chromatography B 878 15 (2010): Pages 1181-1184.

Picamilon Upstream-Materialien And Downstream Produkte

Picamilon Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

34562-97-5, Picamilon Verwandte Suche:

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