Pitrazepin 

Pitrazepin is a GABA_A receptor antagonist and glycine receptor antagonist. Pitrazepin blocks synaptic GABA action, induces neuronal bursting and reduces inhibitory postsynaptic potentials. Pitrazepin can be used in research on depression and psychosis^[1][2][3][4].

Pitrazepin potently inhibits [³H]muscimol binding to GABA_A receptors with an IC₅₀ of 0.24 μM^[1].
Pitrazepin acts as a competitive GABA_A receptor antagonist in rat cortex membranes, with a mean K_i value of 80 nM, and directly inhibits [³H]diazepam binding with an IC₅₀ of 730 nM^[2].
Pitrazepin (25°C for 180 min) acts as a competitive GABAₐ receptor antagonist coupled to the chloride gating mechanism in rat cortex membranes, with a mean K_i value of 84 nM, and does not directly interact with the [³⁵S]TBPS-binding chloride gating site^[2].
Pitrazepin (0°C for 30 min) inhibits high-affinity [³H]GABA binding to rat cortex membranes with an IC₅₀ of 470 nM^[2].
Pitrazepin (25°C for 30 min) does not interact with the [³H]avermectin B_1a-binding site in rat cortex membranes^[2].
Pitrazepin (on ice for 20 min) acts as a competitive inhibitor of [³H]strychnine binding to glycine receptors in rat pons + medulla membranes, with K_i values ranging from 71 nM and an IC₅₀ of 210 nM^[2].
Pitrazepin displaces [³H]muscimol from rat cerebellar membrane binding sites with an IC₅₀ of 240 nM (no ammonium thiocyanate) or 35 nM (with 50 nM ammonium thiocyanate), and displaces [³H]flunitrazepam from total rat brain homogenate (no cerebellum) binding sites with an IC₅₀ of 410 nM^[4].
Pitrazepin (1-10 μM) induces persistent bursting activity in cultured rat hypothalamic neurones and hippocampal pyramidal cells, reduces inhibitory postsynaptic potentials in hippocampal pyramidal cells, blocks chloride-dependent exogenous GABA responses, and does not interfere with GABA_B receptor-mediated baclofen effects^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

317.39

C₁₉H₁₉N₅

90685-01-1

C1(N2CCNCC2)=NN=C3N1C4=C(C=CC=C4)CC5=C3C=CC=C5

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• [1]. Rognan D, et al. Structure and molecular modeling of GABAA receptor antagonists. J Med Chem. 1992 May 29;35(11):1969-77.

  [2]. Braestrup C, et al. Interaction of pitrazepin with the GABA/benzodiazepine receptor complex and with glycine receptors. Eur J Pharmacol. 1985;118(1-2):115-121.

  [3]. Demuro A, et al. Antagonistic action of pitrazepin on human and rat GABA(A) receptors. Br J Pharmacol. 1999;127(1):57-64.

  [4]. Gähwiler BH, et al. Pitrazepin, a novel GABAA antagonist. Neurosci Lett. 1984;45(3):311-316.