Pentetrazol

Pentetrazol (also known as pentylenetetrazole or PTZ) is a small molecule central nervous system and respiratory stimulant that acts primarily as a non-competitive antagonist of the gamma-aminobutyric acid type A (GABA-A) receptor. It was formerly used clinically as a circulatory and respiratory stimulant and cough suppressant but has been withdrawn from the market. Pentetrazol binds to the picrotoxin site on the GABA-A receptor complex, inhibiting GABA-mediated chloride currents, which leads to neuronal excitation and can induce convulsions at high doses. It also increases calcium and sodium influx in neurons by acting at calcium channels, causing depolarization. Pentetrazol has been widely used in research to induce seizures in animal models for studying epilepsy and screening anticonvulsant drugs. It is also considered a prototypical anxiogenic agent in preclinical anxiety models[1][2][3][4][5][6][7].

Brand names

Metrazol

Other names

pentylenetetrazolepentamethylenetetrazolePTZ