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Journal of Pharmaceutical Sciences Oct 1983Preparation of some simple lactone analogues of picrotoxin and their biological evaluation is reported. Certain analogues possessed activity, but at potencies...
Preparation of some simple lactone analogues of picrotoxin and their biological evaluation is reported. Certain analogues possessed activity, but at potencies insufficient to warrant further work.
Topics: Alkylation; Animals; Central Nervous System Stimulants; Female; Lactones; Picrotoxin; Rats; Rats, Inbred Strains
PubMed: 6139469
DOI: 10.1002/jps.2600721005 -
Journal de Pharmacie de Belgique 1963
Topics: Picrotoxin
PubMed: 13998117
DOI: No ID Found -
Lancet (London, England) Sep 1946
Topics: Barbital; Barbiturates; Drug Overdose; Picrotoxin
PubMed: 20997264
DOI: 10.1016/s0140-6736(46)90893-8 -
Proceedings of the National Academy of... Apr 2006
Topics: Animals; GABA Antagonists; GABA-A Receptor Antagonists; Molecular Structure; Picrotoxin
PubMed: 16606858
DOI: 10.1073/pnas.0601121103 -
Biochemical Pharmacology May 1993The induction by the central stimulant picrotoxin of hepatic drug-metabolizing enzymes was studied in rats. The hepatic content of P450 and the activity of benzphetamine... (Comparative Study)
Comparative Study
The induction by the central stimulant picrotoxin of hepatic drug-metabolizing enzymes was studied in rats. The hepatic content of P450 and the activity of benzphetamine N-demethylation increased gradually after administration of picrotoxin dissolved in drinking water (2 mg/mL), to three-times higher levels than the initial values at the third day of treatment. The increase in benzphetamine N-demethylase activity by picrotoxin was somewhat higher than the increase produced by phenobarbital. Supporting these results, immunoblot analysis showed that CYP2B1 and 2B2 proteins in the liver microsomes were increased by picrotoxin Picrotoxinin and picrotin, which are components of the picrotoxin molecule, had the same ability to induce the hepatic activity of benzphetamine N-demethylation. The liver microsomal activities of testosterone 16 alpha- and 16 beta-hydroxylation were enhanced significantly after treatment with picrotoxinin and picrotin. However, benzo[a]pyrene 3-hydroxylation, aniline 4-hydroxylation, and testosterone hydroxylations at the 2 alpha- and 7 alpha-positions were not increased by picrotoxinin and picrotin treatment. In addition to monooxygenase, significant induction of glutathione S-transferase activity for 1-chloro-2,4-dinitrobenzene and UDP-glucuronyltransferase activity for 4-hydroxybiphenyl and 4-nitrophenol was also observed by pretreatment of picrotoxin. These results clearly indicate that picrotoxin is an inducer of phenobarbital-inducible liver enzymes.
Topics: Animals; Cytochrome P-450 Enzyme System; Enzyme Induction; Male; Microsomes, Liver; Oxidoreductases, N-Demethylating; Phenobarbital; Picrotoxin; Rats; Rats, Wistar; Sesterterpenes; Subcellular Fractions; Testosterone; Toxins, Biological
PubMed: 8494537
DOI: 10.1016/0006-2952(93)90434-x -
Laryngo- Rhino- Otologie Dec 2008In medical long-term treatment of Menière's disease picrotoxin suppositories are an uncommon method of prophylaxis. In spite of its empirical benefit in clinical use... (Comparative Study)
Comparative Study Randomized Controlled Trial
OBJECTIVE
In medical long-term treatment of Menière's disease picrotoxin suppositories are an uncommon method of prophylaxis. In spite of its empirical benefit in clinical use and its lack of side effects, there are few clinical studies about the therapeutical effect of picrotoxin. In this study we evaluate the effectiveness of picrotoxin compared to the therapy with betahistine in Menière's disease.
MATERIAL AND METHODS
In a prospective clinical trial we examined 41 patients, 18 of them were treated with betahistine 3x12 mg, 23 had a therapy with picrotoxin-suppositories at 0.001 g three times a week. Frequency and intensity of the vertigo attacks were evaluated before and under treatment. Mean follow up time was 12 months.
RESULTS
In both groups a reduction of the attacks' frequency and intensity could be noticed, which was statistically significant for all the two groups. Thus, in the course of the treatment we observed a significant stronger effectiveness of picrotoxin, regarding the frequency and intensity of vertigo attacks. Discussing our own results we review the state of the art in medical long-term treatment in Menière's disease.
CONCLUSION
Because of its clinical benefit and the lack of side effects Picrotoxin is a reasonable alternative in medical long- term treatment of Menière's disease, which should have an important role in the treatment cascade.
Topics: Administration, Oral; Adult; Aged; Betahistine; Female; Follow-Up Studies; Humans; Male; Meniere Disease; Middle Aged; Picrotoxin; Prospective Studies; Suppositories
PubMed: 18720328
DOI: 10.1055/s-2008-1077389 -
Journal of Food Science Oct 2008Picrotoxin is a neurotoxin found in the berries of Anamirta cocculus, a plant native to Southeast Asia. Picrotoxin has potential for being used as a biological weapon...
Picrotoxin is a neurotoxin found in the berries of Anamirta cocculus, a plant native to Southeast Asia. Picrotoxin has potential for being used as a biological weapon since the toxin is relatively easy to isolate and purify. Limited information exists on the stability and detection of picrotoxin added to foods before or after processing. The objective of this study was to determine the stability of picrotoxin during yogurt manufacture and storage. Direct, cup-set yogurt was produced by using methods that mimic the conditions used in full-scale production of yogurt. Milk (full-fat or low-fat) was pasteurized at 85 degrees C for 30 min, and then cooled to 43 degrees C. Yogurt starter culture (thermophilic culture or thermophilic + probiotic culture) and picrotoxin (200 mug/mL milk) were added. Samples of yogurt during fermentation (5 to 6 h, 43 degrees C) and during 30 d refrigerated (4 to 6 degrees C) storage were analyzed for pH, titratable acidity, and picrototoxin levels. Regardless of starter culture used or fat content of milk, there were no significant differences in the pH and titratable acidities of the picrotoxin-spiked yogurt and the control yogurt (no added picrotoxin) during fermentation and up to 4 wk of refrigerated storage. The color or texture of the yogurt was not affected by addition of picrotoxin. Levels of picrotoxinin and picrotin (components of picrotoxin) in yogurt, as measured by LC/MS (APCI(+)/SIR) did not change significantly during fermentation and storage. A separate experiment determined that addition of picrotoxin to milk before pasteurization (85 degrees C, 30 min) did not affect picrotoxin stability. These results indicate that picrotoxin is stable in yogurt during manufacture and storage.
Topics: Cold Temperature; Drug Stability; Fermentation; Food Handling; Food Preservation; Hot Temperature; Hydrogen-Ion Concentration; Picrotoxin; Time Factors; Yogurt
PubMed: 19019133
DOI: 10.1111/j.1750-3841.2008.00911.x -
Revista. Universidad Nacional Mayor de... 1948
Topics: Barbital; Barbiturates; Picrotoxin
PubMed: 18118246
DOI: No ID Found -
Pharmacology, Biochemistry, and Behavior Sep 1992The action of MK-801 (NMDA antagonist; 0.1 and 0.5 mg/kg, IP) was tested against picrotoxin-induced seizures (3-6 mg/kg, IP) in rats aged 7, 12, 18, 25, and 90 days. We...
The action of MK-801 (NMDA antagonist; 0.1 and 0.5 mg/kg, IP) was tested against picrotoxin-induced seizures (3-6 mg/kg, IP) in rats aged 7, 12, 18, 25, and 90 days. We found MK-801 only inconsistently affected clonic seizures in 12- and 25-day-old rats, whereas tonic-clonic seizures were suppressed or delayed in almost all age groups. In addition, the lethality of picrotoxin was diminished by the higher dose of MK-801 in all age groups. The results suggest: a) different generators for both seizure patterns (clonic and tonic-clonic), b) an involvement of NMDA receptors in the genesis of tonic-clonic seizure pattern, and c) an interaction of MK-801 with GABAergic transmission throughout the entire development studied.
Topics: Aging; Animals; Ataxia; Behavior, Animal; Dizocilpine Maleate; Dose-Response Relationship, Drug; Epilepsy, Tonic-Clonic; Male; Picrotoxin; Rats; Rats, Wistar
PubMed: 1409814
DOI: 10.1016/0091-3057(92)90670-b -
Anesthesiology Jun 2013
Topics: Animals; Drug Industry; Fishes; GABA Antagonists; History, 20th Century; Humans; Museums; Picrotoxin
PubMed: 23695089
DOI: 10.1097/ALN.0b013e31829a0b4b