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Picrotoxin

A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.

Also Known As:

3,6-Methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione, hexahydro-2a-hydroxy-9-(1-hydroxy-1-methylethyl)-8b-methyl-, (1aR-(1aalpha,2abeta,3beta,6beta,6abeta,8aS*,8bbeta,9S*))-, compd. with (1aR-(1aalpha,2abeta,3beta,6beta,6abeta,8aS*,8bbeta,9R*))-hexahydro-2a-hydroxy-8b-methyl-9-(1-methylethenyl)-3,6-methano-8H-1,5,7-trioxacyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione (1:1)

Networked: 851 relevant articles (66 outcomes, 65 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Yakimovskii, A F: 7 articles (04/2011 - 08/2002)
2.	Pericić, Danka: 6 articles (06/2008 - 09/2002)
3.	Ojewole, John A O: 6 articles (04/2008 - 12/2005)
4.	Paul, Vanaja: 6 articles (03/2005 - 06/2002)
5.	Sierra-Paredes, Germán: 5 articles (10/2007 - 05/2005)
6.	Sierra-Marcuño, Germán: 5 articles (10/2007 - 05/2005)
7.	Rogawski, Michael A: 4 articles (02/2015 - 05/2002)
8.	Kombian, Samuel B: 4 articles (01/2014 - 09/2007)
9.	Dhir, Ashish: 4 articles (10/2013 - 04/2006)
10.	Rakotonirina, A: 4 articles (07/2012 - 07/2001)

Related Diseases

1.	Seizures (Seizure) 06/01/2008 - "The drug was more potent against PTZ- than against picrotoxin-induced seizures. " 09/26/2008 - "This monoterpene was also capable to promote an increase of latency for development of convulsions induced by picrotoxin (PIC) at 300 or 400 mg/kg and presented a significant protection against convulsions at doses of 200, 300 or 400 mg/kg, resulting in 12.5%, 12.5% and 100% of protection, respectively. " 12/01/1985 - "Administered intracerebroventricularly, it is also effective in protecting mice from picrotoxin-induced convulsions with an ED50 of 0.17 mumol." 09/01/2012 - "The anticonvulsant activity for 15 of the synthesized compounds was evaluated and 6 compounds showed protection against picrotoxin-induced convulsion. " 03/26/1985 - "HQC administered intracerebroventricularly caused a dose dependent delay in the occurrence of picrotoxin induced convulsions and afforded protection against picrotoxin induced death. "
2.	Ganglion Cysts (Ganglion) 03/23/2007 - "Application of picrotoxin could evoke the dual-peak responses in transient ganglion cells. " 02/01/2003 - "The effect of GABAergic blockade by picrotoxin on ganglion cells (GC) activity was investigated in perfused dark adapted eyecups of frog (Rana ridibunda). " 09/01/1984 - "Picrotoxin (10(-5) M) did not block transient inhibitory events in any ganglion cells, but did affect other components of their responses. " 08/01/1981 - "Effects of picrotoxin on sensitivity and receptive field properties of ganglion cells in the frog retina." 12/01/1980 - "1. Picrotoxin (PTX) (10(-7)-10(-6) M) completely blocked most inhibitory synapses in the pyloric pattern generator of the lobster (Panulirus interruptus) stomatogastric ganglion. "
3.	Tonic-Clonic Epilepsy (Epilepsy, Tonic Clonic) 01/01/1983 - "Considering the incidence of tonic-clonic convulsions, tolerance to the protective effects of diazepam was evident by day 5 if the mice were challenged with PTZ (120 mg/kg), by day 10 if the challenge was picrotoxin (8 mg/kg) and by day 20 if the challenge was PTZ (105 mg/kg). " 09/01/2014 - "MJ (50-400 mg/kg) did not protect the mice against tonic-clonic convulsions induced by picrotoxin (10 mg/kg, i.p.) or strychnine (3 mg/kg, i.p.). " 06/12/1999 - "The total dose of drug infused prior to either electrical seizures (lidocaine, PTZ, and picrotoxin) or tonic-clonic convulsions (all drugs) were noted. " 08/01/2007 - "However, cefazolin (500 or 1000 mg/kg, i.v.) when administered before different doses of pentylenetetrazol (PTZ; 40 or 60 mg/kg, i.p.) or picrotoxin (PTX; 4 or 8 mg/kg, i.p.), it produced severe tonic-clonic convulsions in mice. " 01/01/2013 - "However, it did not did not offer any protection against seizure episodes, as it failed to prevent the animals, from exhibiting tonic-clonic convulsions caused by pentylenetetrazole (85 mg/kg, i.p.), strychnine (2 mg/kg) or picrotoxin (6 mg/kg, i.p.). "
4.	Pain (Aches) 12/01/1996 - "In this study, we report the possibility of producing marked electrocorticographic changes and "pain-like" reactions, when the GABAA antagonist picrotoxin is microinjected unilateraly into the rat somato-motor Sml cortex in the region of the hind paw. " 09/26/1994 - "In this study, we reported that the microinjection of the GABAA antagonist picrotoxin into the rat thalamic reticular nucleus produced a 'pain-like' behavior. " 12/01/2011 - "Picrotoxin significantly (P<0.05) increased pain sensitivity in all stages of estrous cycle, and such a hyperalgesic effect was lower during proestrus and estrus stages of estrous cycle than that during metestrus and diestrus stages. " 12/01/1997 - "Cholinergic modulation of the picrotoxin-induced electrocorticographical events and behavioral "pain-like" symptoms at somatomotor cortical level in the rat." 12/01/1996 - "Picrotoxin produces a "central" pain-like syndrome when microinjected into the somato-motor cortex of the rat."
5.	Anoxia (Hypoxia) 03/01/1994 - "In the presence of both GABAergic (picrotoxin, 100 microM) and glutamatergic blockers no significant reduction in resting input resistance was apparent after 2 min of anoxia.(ABSTRACT TRUNCATED AT 400 WORDS)" 04/01/2013 - "Picrotoxin intravenous administration caused the increase of individual resistance to acute hypoxia. " 02/01/2008 - "Administration of picrotoxin to anesthetized rats increased animal resistance to hypoxia. " 02/01/2008 - "Effect of picrotoxin on organism's resistance to acute severe hypoxia." 12/01/1983 - "Picrotoxin (300-400 micrograms/kg intravenous bolus injection) induced a period of stimulated breathing (40-112 min) which was associated with high voltage electrocortical activity, but inhibited by hypoxia. "

Related Drugs and Biologics

1.	Bicuculline
2.	Pentylenetetrazole (Metrazol)
3.	Strychnine
4.	Diazepam (Valium)
5.	Phenobarbital (Luminal)
6.	Kainic Acid (Kainate)
7.	N-Methylaspartate (NMDA)
8.	gamma-Aminobutyric Acid (GABA)
9.	Pentobarbital (Nembutal)
10.	Muscimol

Related Therapies and Procedures

1.	Injections
2.	Traction
3.	Intraperitoneal Injections
4.	Electrodes (Electrode)
5.	Oral Administration