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Encyclopedia > Pentetrazol
Systematic (IUPAC) name
5H-Tetrazolo(1,5-a)azepine, 6,7,8,9-tetrahydro-[1]
CAS number 54-95-5
ATC code R07AB03
PubChem 5917
Chemical data
Formula C6H10N4 
Mol. mass 138.171
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

? Image File history File links Metrazol. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number nitrogen, N, 7 Chemical series nonmetals Group, Period, Block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... The molecular mass (abbreviated MM) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status
Routes  ?

Metrazol is the commercial trademark of pentetrazol, pentamethylenetetrazol, or pentylenetetrazol (PTZ), 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.[2] The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... This article is about the medical condition. ... Shock therapy is the deliberate and controlled induction of some form of physiological state of shock in an individual for the purpose of psychiatric treatment. ... Ladislas Joseph Meduna (1896-1964) was a Hungarian neurologist who discovered the first effective drugs for the treatment of schizophrenia. ... Seizures are temporary abnormal electro-physiologic phenomena of the brain, resulting in abnormal synchronization of electrical neuronal activity. ...

It is considered a non-competitive GABA antagonist.[3] 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. Gaba may refer to: Gabâ or gabaa (Philippines), the concept of negative karma of the Cebuano people GABA, the gamma-amino-butyric acid neurotransmitter GABA receptor, in biology, receptors with GABA as their endogenous ligand Gaba 1 to 1, an English conversational school in Japan Marianne Gaba, a US model... Neurons (also called nerve cells) are the primary cells of the nervous system. ... Current Clamp is a common technique in electrophysiology. ... The cell membrane (also called the plasma membrane or plasmalemma) is a semipermeable lipid bilayer common to all living cells. ... A. A schematic view of an idealized action potential illustrates its various phases as the action potential passes a point on a cell membrane. ... General Name, Symbol, Number potassium, K, 19 Chemical series alkali metals Group, Period, Block 1, 4, s Appearance silvery white Atomic mass 39. ... Permeability has several meanings: In electromagnetism, permeability is the degree of magnetisation of a material in response to a magnetic field. ... An axon or nerve fiber, is a long, slender projection of a nerve cell, or neuron, that conducts electrical impulses away from the neurons cell body or soma. ... General Name, Symbol, Number sodium, Na, 11 Chemical series alkali metals Group, Period, Block 1, 3, s Appearance silvery white Atomic mass 22. ... General Name, Symbol, Number calcium, Ca, 20 Chemical series alkaline earth metals Group, Period, Block 2, 4, s Appearance silvery white Atomic mass 40. ...

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.[4] This article includes a list of works cited but its sources remain unclear because it lacks in-text citations. ... The GABAA receptor is one of the three ligand-gated ion channels responsible for mediating the effects of Gamma-AminoButyric Acid (GABA), the major inhibitory neurotransmitter in the brain. ... NMDA (N-methyl-D-aspartic acid) is an amino acid derivative acting as a specific agonist at the NMDA receptor, and therefore mimics the action of the neurotransmitter glutamate on that receptor. ... For the plant, see Glycine (plant). ... The L-type calcium channel is a type of voltage-dependent calcium channel. ... In chemistry, a ligand is an atom, ion or functional group that is bonded to one or more central atoms or ions, usually metals generally through co-ordinate covalent bond. ...

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.[5] 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.[2] Picrotoxin is an antagonist of GABA receptors. ... Bilobalide is bilogically active terpenic trilactone present in Ginkgo biloba. ... The GABAA receptor is one of the three ligand-gated ion channels responsible for mediating the effects of Gamma-AminoButyric Acid (GABA), the major inhibitory neurotransmitter in the brain. ... Seizures are temporary abnormal electro-physiologic phenomena of the brain, resulting in abnormal synchronization of electrical neuronal activity. ...


  1. ^ Pentylenetetrazole in the Super Drug Database
  2. ^ a b JR Minkel. "Drug May Counteract Down Syndrome", Scientific American, February 25, 2007. Retrieved on 2007-03-20.
  3. ^ Entry for Pentylenetetrazole in the MeSH database
  4. ^ 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. PMID 12204190. 
  5. ^ 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. PMID 17322876. 

  Results from FactBites:
257. BHC (technical) (WHO Pesticide Residues Series 3) (1954 words)
The 1968 Joint Meeting did not recommend an ADI because technical HCH was not standardized as to its composition of various isomers of differing toxicological potency and action, and because of lack of adequate toxicological data on the different isomers.
EVALUATION FOR ACCEPTABLE DAILY INTAKE Biochemical aspects A single oral dose of 200 mg/kg of BHC enhanced the metabolism of pentetrazol by rat liver homogenates in vitro and hastened the disappearance of this drug in vivo when the BHC was given four days prior to pentetrazol treatment (Vohland and Koransky, 1972a, b).
273: 99-108 Vohland, H. W., Koransky, W. and Zufelde, H. Effect of 1972b ý-hexachlorocyclohexane on the convulsive activity of pentetrazol (cardiozol) in the rat.
  More results at FactBites »



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