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

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(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. (RS)-(Tetrazol-5-yl)glycine has EC₅₀s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice.

For research use only. We do not sell to patients.

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

CAS No. : 138199-51-6

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Purity & Documentation
References
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Description

(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

NMDA Receptor

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].

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

In Vivo

(RS)-(Tetrazol-5-yl)glycine can be used in animal modeling to create epilepsy models and is able to penetrate the blood-brain barrier^[4].

1. Induction of epilepsy^[4]

Background

(RS)-(Tetrazol-5-yl)glycine can stimulate NMDA receptors, causing hippocampal neurotoxic damage and leading to epilepsy.

Specific Mmodeling Methods

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.

Modeling Indicators

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.

Correlated Product(s): /

Opposite Product(s): Suramin (HY-B0879)

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

Animal Model:	C57BL/6 mice^[3]
Dosage:	1.25, 1.5 mg/kg
Administration:	IP
Result:	Induced seizure responses and Fos.

Molecular Weight

143.10

Formula

C₃H₅N₅O₂

CAS No.

138199-51-6

SMILES

O=C(O)C(N)C1=NNN=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Schoepp DD, et al. D,L-(tetrazol-5-yl) glycine: a novel and highly potent NMDA receptor agonist. Eur J Pharmacol. 1991 Oct 15;203(2):237-43. [Content Brief]

[2]. Vance KM, et al. Ligand-specific deactivation time course of GluN1/GluN2D NMDA receptors. Nat Commun. 2011;2:294. [Content Brief]

[3]. Duncan GE, et al. Seizure responses and induction of Fos by the NMDA agonist (tetrazol-5-yl)glycine in a geneticmodel of NMDA receptor hypofunction. Brain Res. 2008 Jul 24;1221:41-8. [Content Brief]

[4]. Ong WY, et al. P2 purinoceptor blocker suramin antagonises NMDA receptors and protects against excitatory behaviour caused by NMDA receptor agonist (RS)-(tetrazol-5-yl)-glycine in rats. J Neurosci Res. 1997 Sep 1;49(5):627-38. [Content Brief]

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

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(RS)-(Tetrazol-5-yl)glycine138199-51-6D,L-(tetrazol-5-yl)glycine LY 285265LY285265LY 285265LY-285265iGluRIonotropic glutamate receptorsN-methyl-D-aspartateNMDAGluN1GluN2DGluN2AseizureFosInhibitorinhibitorinhibit

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