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(RS)-(Tetrazol-5-yl)glycine


CAS No. : 138199-51-6

(Synonyms: D,L-(tetrazol-5-yl)glycine; LY 285265)

138199-51-6
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Cat. No. : HY-100839
M.Wt: 143.10
Formula: C3H5N5O2
Purity: >98 %
Solubility: 10 mM in DMSO
Introduction of 138199-51-6 :

(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist[1]. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively[2]. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice[3]. IC50 & Target:EC50: 99 nM (GluN1/GluN2D) and 1.7 μM (GluN1/GluN2A)[1] In Vitro:(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a agonist of N-methyl-D-aspartate (NMDA) subtype of excitatory amino acid receptor. (RS)-(Tetrazol-5-yl)glycine displaces NMDA receptor binding to rat brain membranes as measured using [3H]CGS19755 (IC50=98 nM) and [3H]glutamate (IC50=36 nM) as ligands[1].
(RS)-(Tetrazol-5-yl)glycine does not appreciably inhibit the binding of D,L-alpha-[5-methyl-3H] amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), [3H]kainate, or [3H]glycine (IC50s>30 μM)[1].
In Vivo:(RS)-(Tetrazol-5-yl)glycine can be used in animal modeling to construct epilepsy models.

(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine; 1.25, 1.5 mg/kg; IP) induces seizure responses and Fos in the NR1+/+ and NR1-/- mice[3].
(RS)-(Tetrazol-5-yl)glycine is a highly potent convulsant when given to neonatal rats (ED50=0.071 mg/kg; i.p.)[1].

(RS)-(Tetrazol-5-yl)glycine can penetrate the blood-brain barrier[4].
(RS)-(Tetrazol-5-yl) glycine can be used for animal modeling and constructing epilepsy models.

1. Induction of epilepsy[4]
致病原理
(RS)-(Tetrazol-5-yl)glycine can stimulate NMDA receptors, causing hippocampal neurotoxic damage and leading to epilepsy.
具体造模方法
Rat: Sprague-Dawley • male or female • 2-6 months old
Administration: 0.2 and 0.4 μL of a 0.7 mM (RS)-(Tetrazol-5-yl)glycine solution • ICV
Note
(1) Inject (RS)-(Tetrazol-5-yl) glycine into the right ventricle of rats, and after 10 minutes, remove the needle and suture the wound and scalp.
(2) Among the 11 rats injected with 0.28 nmol (RS) - (Tetrazol-5-yl) glycine, 5 died within a few hours after injection, making it impossible to perfuse and determine the degree of hippocampal lesions.
(3) There was no loss of hippocampal neurons in two of the four rats injected with the lower dose of (RS) - (Tetrazol-5-yl) glycine, whereas the other two showed loss of pyramidal neurons in the medial portion of CA1, and granule neurons in the dentate gyrus.
造模成功指标
Phenotypic observation: All rats injected with the higher dose of TZG showed an extensive loss of pyramidal neurons and GluR1 immunoreactivity in CA1–4 and in the dentate gyrus.
Behavioral observation: Continuous flicking of the tail, rowing movements, and convulsions.
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