- Picamilon
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- $0.00 / 1kg
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2025-08-15
- CAS:34562-97-5
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 1000
- Pikamilone
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- $29.00 / 1mL
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2025-07-15
- CAS:34562-97-5
- Min. Order:
- Purity: 98.25%
- Supply Ability: 10g
- Pikamilon
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- $0.00 / 1kg
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2025-06-20
- CAS:34562-97-5
- Min. Order: 1kg
- Purity: 0.99
- Supply Ability: 20tons
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| | Picamilon Chemical 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) |
| Hazard Codes | Xi | | HazardClass | IRRITANT | | HS Code | 2933599590 |
| | Picamilon Usage And Synthesis |
| 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].
| | Synthesis | General procedure for the synthesis of 3-((3-carboxypropyl)carbamoyl)pyridine from compound (CAS: 121667-28-5): 10% palladium charcoal (10 mmol) and dry methanol (10 v/v) were added to a 50 mL flask, followed by the addition of compound-2 (10 mmol) under stirring. The atmosphere in the flask was replaced with nitrogen and then hydrogen. The reaction mixture was stirred vigorously in hydrogen atmosphere for 2.0 hours at room temperature. After completion of the reaction, the reaction mixture was filtered through diatomaceous earth and washed with methanol. The organic layer was evaporated and the residue was dissolved in ethyl acetate and washed with water. The organic layer was dried with sodium sulfate, filtered and the solvent was evaporated to give compound-3 (yield: 90%). | | in vivo | Picamilon (PM) (20 or 50 mg/kg; i.p.) significantly decreases the frequency and duration of seizure spike-wave discharges (SWDs) in Picrotoxin (HY-101391)-induced convulsive activity in rats[2].
Picamilon (250 mg/kg; p.o.) inhibits NLRP3 inflammasome activation in pancreatic cells during Alloxan (HY-W017227) -induced diabetes mellitus rats model[3].
| Animal Model: | Picrotoxin (HY-101391)-induced epilepsy model in rats [2] | | Dosage: | 20 or 50 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Significantly decreased the frequency and duration of seizure spike-wave discharges (SWDs) in doses of 50 mg/kg.
Decreased the intensity of SWDs in smaller doses (20 mg/kg).
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| Animal Model: | Alloxan (HY-W017227)-induced diabetes mellitus model in rats [3] | | Dosage: | 250 mg/ kg | | Administration: | Oral gavage (p.o.)
| | Result: | Suppressed NLRP3 activity, as indicated by a significant decrease in the area of immunopositive pancreatocytes to (21,30 ± 5,44) and (39,31 ± 5,24) %, respectively, relative to the value in the group of animals that were not treated (75,19±7,69%).
Promoted correction of functional disorders of the pancreas during alloxan-induced diabetes mellitus by inhibiting activation of NLRP3 inflammasome in pancreatocytes.
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| | 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.
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| | Picamilon Preparation Products And Raw materials |
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