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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
Molecular Weight:
208.21
MDL Number:
MFCD08272808
MOL File:
34562-97-5.mol
MSDS File:
SDS
Last updated:2024-11-20 11:41:24

Picamilon Properties

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)
FDA UNII 0S5N9SEK4N

SAFETY

Risk and Safety Statements

Hazard Codes  Xi
HazardClass  IRRITANT
HS Code  2933599590

Picamilon price More Price(18)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TCI Chemical N0998 Picamilon >98.0%(HPLC)(T) 34562-97-5 5g $137 2024-03-01 Buy
Cayman Chemical 29397 Picamilon 34562-97-5 100mg $32 2024-03-01 Buy
Cayman Chemical 29397 Picamilon 34562-97-5 250mg $73 2024-03-01 Buy
Cayman Chemical 29397 Picamilon 34562-97-5 500mg $139 2024-03-01 Buy
Cayman Chemical 29397 Picamilon 34562-97-5 1g $243 2024-03-01 Buy
Product number Packaging Price Buy
N0998 5g $137 Buy
29397 100mg $32 Buy
29397 250mg $73 Buy
29397 500mg $139 Buy
29397 1g $243 Buy

Picamilon Chemical Properties,Uses,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

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.

Uses

anti-cancer agent

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.

121667-28-5
34562-97-5
Synthesis of Picamilon from Butanoic acid, 4-[(3-pyridinylcarbonyl)amino]-, phenylmethyl ester
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View Lastest Price from Picamilon manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Pikamilone pictures 2024-12-13 Pikamilone
34562-97-5
US $1.00 / KG 1KG ≥99% 1000kg/month WUHAN FORTUNA CHEMICAL CO., LTD
Pikamilone pictures 2024-11-19 Pikamilone
34562-97-5
US $50.00 / mL 98.25% 10g TargetMol Chemicals Inc.
Pikamilon pictures 2024-10-25 Pikamilon
34562-97-5
US $0.00 / kg 1kg 0.99 20tons Hebei Yanxi Chemical Co., Ltd.
  • Pikamilone pictures
  • Pikamilone
    34562-97-5
  • US $1.00 / KG
  • ≥99%
  • WUHAN FORTUNA CHEMICAL CO., LTD
  • Pikamilone pictures
  • Pikamilone
    34562-97-5
  • US $50.00 / mL
  • 98.25%
  • TargetMol Chemicals Inc.
  • Pikamilon pictures
  • Pikamilon
    34562-97-5
  • US $0.00 / kg
  • 0.99
  • Hebei Yanxi Chemical Co., Ltd.

Picamilon Spectrum

4-((Pyridine-3-carbonyl)-amino)-butyric acid Pikamiline PikamiloneHCl 3-[(3-Carboxypropyl)carbamoyl]pyridine PIKAMILON 4-Nicotinoylamino-butylric acid PIKAMILONE HYDROCHLORIDE NICOTINOYL-GABA N-(3-CARBOXYPROPYL) NICOTINAMIDE 4-[(PYRIDIN-3-YLCARBONYL)AMINO]BUTANOIC ACID 4-(NICOTINAMIDO)BUTANOIC ACID 4-(3-PYRIDYLCARBOXAMIDO)BUTYRIC ACID 4-[(3-PYRIDINYLCARBONYL)AMINO]BUTANOIC ACID 4-Nicotinoylamino-butyric acid Pikamilone Pikamilone sodium sale 4-Nicotinoylamino-butanoic acid PikaMilone, 4-NicotinoylaMino-butyric acid Butanoic acid,4-[(3-pyridinylcarbonyl)aMino]- PICAMILON BASE 4-(pyridine-3-carbonylamino)butanoic acid 4-[[oxo(3-pyridinyl)methyl]amino]butanoic acid Nicotinoyl-γ-aminobutyric Acid Picamilon > N-Nicotinoyl-gamma-aminobutyric Acid N-Nicotinoyl-GABA 4-(Nicotinamido)butyric Acid PICAMILON PIKAMILON PICAMILON 34562-97-5 Other APIs API Chemistry Heterocycles 34562-97-5