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20-September-2008 09:55:56 - Pentylenetetrazol Redirected from Pentetrazol Pentylenetetrazol Systematic IUPAC name 6,7,8,9-tetrahydro-5H-Tetrazolo1,5-aazepine Identifiers CAS number 54-95-5 ATC code R07AB03 PubChem 5917 Chemical data Formula C6H10N4 Mol. mass 138.171 SMILES eMolecules PubChem Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? Pentylenetetrazol PTZ is the International Nonproprietary Name of Metrazol and also known as pentetrazol or pentamethylenetetrazol. It is a drug used as a circulatory and respiratory stimulant another commercial name is Cardiazol. Larger doses cause convulsions, thus it has been used in shock therapy, as discovered by the Hungarian-American neurologist and psychiatrist Ladislas J. Meduna in 1934. It was never considered to be effective, and side-effects such as seizures are difficult to avoid. Its approval by FDA was revoked in 1982.1 Contents 1 Mechanism 2 Uses 3 Alternatives 4 References Mechanism It is considered a GABA antagonist.2 The mechanism of the epileptogenic action of PTZ at the cellular neuronal level is still unclear. Electrophysiological studies have shown it acts at cell membrane level decreasing the recovery time between action potentials by increasing potassium permeability of the axon. Other studies have implicated an increase in membrane currents of several other ions, such as sodium and calcium, leading to an overall increase in excitability of the neuron membrane. Uses Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility. PTZ is also a prototypical anxiogenic drug and, has been extensively utilized in animal models of anxiety. PTZ produces a reliable discriminative stimulus which is largely mediated by the GABAA receptor. Several classes of compounds can modulate the PTZ discriminative stimulus including 5-HT1A, 5-HT3, NMDA, glycine, and L-type calcium channel ligands.3 Recently, it has been shown that pentetrazol at non-epileptic doses, along with two other compounds Picrotoxin and bilobalide can restore the cognitive function learning and memory of a mouse model of Down syndrome by inhibiting GABAA receptor without inducing seizures.4 These results caused renewed interest in pentetrazol as a potential drug candidate for Down syndrome, although clinical trials are probably still a couple of years away.1 Alternatives In 1939, Metrazol also known as Cardiazol was replaced by electroconvulsive therapy as the preferred method for inducing seizures in England's mental hospitals. References ^ a b JR Minkel February 25, 2007. Drug May Counteract Down Syndrome, Scientific American. Retrieved on 2007-03-20. ^ Entry for Pentylenetetrazole in the MeSH database ^ Jung M, Lal H, Gatch M 2002. The discriminative stimulus effects of pentylenetetrazol as a model of anxiety: recent developments. Neurosci Biobehav Rev 26 4: 429-39. doi:10.1016/S0149-76340200010-6. PMID 12204190. ^ Fernandez F, Morishita W, Zuniga E, Nguyen J, Blank M, Malenka R, Garner C 2007. Pharmacotherapy for cognitive impairment in a mouse model of Down syndrome. Nat Neurosci. doi:10.1038/nn1860. PMID 17322876. v d e Other respiratory system products R07 Lung surfactants Colfosceril palmitate Respiratory stimulants Almitrine - Bemegride - Dimefline - Doxapram - Etamivan - Mepixanox - Nikethamide - Pentylenetetrazol - Prethcamide 5-HT4 receptor agonists BIMU-8 - Zacopride Other agents for treating respiratory depression BW373U86 - CX-546 - CX-717 Retrieved from http://en..org/wiki/Pentylenetetrazol Categories: Stimulants | GABA antagonists | Withdrawn drugs | Respiratory agents Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages EspaƱol This page was last modified on 24 July 2008, at 00:40
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