34562-97-5

Hazard Information

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].

Synthesis

121667-28-5

34562-97-5

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).

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.

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.

Questions And Answer

• 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/;

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