Description Clinical Use
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Picamilon

Description Clinical Use
Product Name
Picamilon
CAS No.
34562-97-5
Chemical Name
Picamilon
Synonyms
PIKAMILON;PICAMILON;Pikamiline;Pikamilone;PikamiloneHCl;Picamilon >PICAMILON BASE;NICOTINOYL-GABA;N-Nicotinoyl-GABA;PICAMILON PIKAMILON
CBNumber
CB4106397
Molecular Formula
C10H12N2O3
Formula Weight
208.21
MOL File
34562-97-5.mol
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Picamilon Property

Melting point:
211.0 to 215.0 °C
Boiling point:
522.4±30.0 °C(Predicted)
Density 
1.245
storage temp. 
Inert atmosphere,Room Temperature
solubility 
DMSO (Slightly, Heated), Methanol (Slightly)
form 
Solid
pka
4.60±0.10(Predicted)
color 
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 DataBase Reference
34562-97-5(CAS DataBase Reference)
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Safety

Hazard Codes 
Xi
HazardClass 
IRRITANT
HS Code 
2933599590
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TCI Chemical
Product number
N0998
Product name
Picamilon
Purity
>98.0%(HPLC)(T)
Packaging
5g
Price
$137
Updated
2024/03/01
Cayman Chemical
Product number
29397
Product name
Picamilon
Packaging
100mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
29397
Product name
Picamilon
Packaging
250mg
Price
$73
Updated
2024/03/01
Cayman Chemical
Product number
29397
Product name
Picamilon
Packaging
500mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
29397
Product name
Picamilon
Packaging
1g
Price
$243
Updated
2024/03/01
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Picamilon Chemical Properties,Usage,Production

Description

Pikamilone is a drug having a central (vegetotropic and vascular) and peripheral (vasodilating) mechanisms of action.

Clinical Use

Pikamilone treatment of benign prostatic hyperplasia
Pikamilone is an original drug of Russian produce having a central (vegetotropic and vascular) and peripheral (vasodilating) mechanisms of action. The drug was tried as monotherapy in elderly patients with benign prostatic hyperplasia who had symptoms of the lower urinary tracts to estimate its effect on local and general mechanisms of nervous and vascular regulation of detruzor function in infravesical obstruction.
https://pubmed.ncbi.nlm.nih.gov/11150159/

Description

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].

Uses

anti-cancer agent

Uses

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.

Pharmacokinetics

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].

References

[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 Preparation Products And Raw materials

Raw materials

Preparation Products

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Picamilon Suppliers

TCI Europe
Tel
320-37350700
Fax
+32 (0)37350701
Email
sales@tcieurope.eu
Country
Europe
ProdList
23671
Advantage
75
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View Lastest Price from Picamilon manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Pikamilone 34562-97-5
Price
US $1.00/KG
Min. Order
1KG
Purity
≥99%
Supply Ability
1000kg/month
Release date
2021-06-21
Hebei Yanxi Chemical Co., Ltd.
Product
Pikamilon 34562-97-5
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20tons
Release date
2023-10-10
Wuhan Senwayer Century Chemical Co.,Ltd
Product
Pikamilone 34562-97-5
Price
US $160.00/kg
Min. Order
1kg
Purity
99% min
Supply Ability
20 tons
Release date
2022-10-17

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