ZJ43

ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC₅₀ of 2.4 nM and K_i of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury^[1][2][3][4]. IC50 & Target:IC₅₀: 2.4 nM (NAAG)^[1] In Vitro:ZJ43 (range sufficient to generate dose-response curves; 2 h) potently inhibits cloned human GCP II with a K_i of 0.8 nM^[1].
ZJ43 (range sufficient to generate dose-response curves) inhibits cloned mouse GCP III with a K_i of 23 nM^[1].
ZJ43 (2 h) inhibits cloned rat GCPII with a K_i of 3 nM^[3]. In Vivo:ZJ43 (150 mg/kg; i.p.; single dose) significantly reduces multiple PCP-induced schizophrenia-like behavioral symptoms in male Sprague-Dawley rats^[1].
ZJ43 (10-100 mg/kg; i.v.; single dose) produces dose-dependent analgesia in the rat formalin inflammatory pain model^[3].
ZJ43 (10-100 mg/kg; i.v.; single dose) produces dose-dependent antiallodynic effects in the rat partial sciatic nerve ligation neuropathic pain model^[3].
ZJ43 (100 mg/kg; i.v.; single dose) does not alter acute nociceptive responses to noxious mechanical or thermal stimulation in healthy rats^[3].
ZJ43 (50-150 mg/kg; i.p.; every 8 h; 3 total doses) significantly reduces ipsilateral neuronal degeneration in rat lateral fluid percussion TBI^[4].