N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID Struktur

N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID

Bezeichnung:N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID

CAS-Nr723331-20-2

Englisch Name:N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID

CBNumberCB92453434

SummenformelC12H20N2O7

Molgewicht304.3

MOL-Datei723331-20-2.mol

N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO (up to at least mg/ml) or in Water (up to at least 25 mg/ml)
Aggregatzustand	solid
Farbe	White
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 2 months.

N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
ZJ43 (723331-20-2) is potent inhibitor of glutamate carboxypeptidases II (Ki = 0.8 nM) and III (Ki = 23 nM).1?It potently (IC50?= 2.4 nM) inhibited the ability of glutamate carboxypeptidase II to hydrolyze the neurotransmitter N-acetylaspartylglutamate (NAAG) resulting in an increase in synaptic levels of group II mGluRs. Peripherally administered ZJ43 increased the activation of mGluR3 by NAAG released from peripheral sensory neurites resulting in analgesia.2,3?ZJ43 has also shown efficacy in other inflammatory pain models.4,5
Biologische Aktivität
Potent inhibitor of glutamate carboxypeptidase II and III (GCP II and III/NAAG peptidase/NAALADase) (K i values are 0.8 and 23 nM respectively) that inhibits the hydrolysis of NAAG (IC 50 = 2.4 nM) . Does not directly interact with NMDA or metabotropic glutamate receptors. Reduces neuronal degeneration in a rat model of? traumatic brain injury (TBI) and reduces locomotor activity in the PCP-model of schizophrenia.
in vitro
as a potent inhibitor of glutamate carboxypeptidase ii and iii (gcp ii and iii) with kivalues of 0.8 and 23 nm respectively, zj-43 inhibited the hydrolysis of naag via indirect interactions with nmda or metabotropic glutamate receptors [1].
in vivo
intravenous injection of zj-43 coiuld suppress both phases of the agitation behaviour induced by paw formalin injection in the rat neuropathic pain model. moreover, intravenous administration of zj-43 attenuated the level of mechanical allodynia induced by the nerve ligation. these effects of zj-43 in both the formalin test and the partial sciatic nerve ligation model were completely antagonized by pretreatment with ly-341495, which was a highly selective group ii mglur antagonist [1].
IC 50
2.4 nm
Lager
Store at -20°C
Einzelnachweise
1) Olszewski?et al.?(2004),?NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR; J. Neurochem.?89?876 2) Yamamoto?et al.?(2004),?Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model;?Eur. J. Neurosci.?20?483 3) Yamamoto?et al.?(2007),?Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats; Eur. J. Neurosci.?25?147 4) Yamamoto?et al.?(2008),?Intracerebroventricular administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in inflammatory pain; Mol. Pain?4?31 5) Nonaka?et al.?(2017),?A role for the locus coeruleus in the analgesic efficacy of N-acetylaspartylglutamate peptidase (GCPII) inhibitors ZJ43 and 2-PMPA; Mol.Pain?13?1

N-[[[(1S)-1-CARBOXY-3-METHYLBUTYL]AMINO]CARBONYL]-L-GLUTAMIC ACID Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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