Pentylenetetrazole is a central nervous system stimulant, which is thought to be a non-competitive antagonist of the γ-aminobutyric acid type A (GABA_A) receptor by acting at the picrotoxin site of the GABA_A receptor. Pentylenetetrazole has been used to experimentally induce seizures in animals and screen for antiepileptic compounds.

References:

1. Huang RQ, Bell-Horner CL, Dibas MI, et al. Pentylenetetrazole-induced inhibition of recombinant gamma-aminobutyric acid type A (GABA_A) receptors: mechanism and site of action. Journal of Pharmacology and Experimental Therapeutics, 2001, 298(3): 986-995.

2. Löscher W. Critical review of current animal models of seizures and epilepsy used in the discovery and development of new antiepileptic drugs. Seizure. 2011, 20(5): 359-368.

3. Kaufmann K, Romaine I, Days E, et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chemical Neuroscience, 2013, 4(9): 1278-1286.

4. Sheng F, Chen M, Tan Y, et al. Protective effects of Otophylloside N on pentylenetetrazol-induced neuronal injury in vitro and in vivo. Frontiers in Pharmacology, 2016, 7: 224.

5. Walsh LA, Li M, Zhao TJ, et al. Acute pentylenetetrazol injection reduces rat GABAA receptor mRNA levels and GABA stimulation of benzodiazepine binding with No effect on benzodiazepine binding site density Journal of Pharmacology and Experimental Therapeutics, 1999, 289(3): 1626-1633.