1. Membrane Transporter/Ion Channel Neuronal Signaling
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  3. MDL 100748

MDL 100748 is an NMDA receptor glycine site antagonist. MDL 100748 modulates NMDA receptor function by acting at the strychnine-insensitive glycine site, which is required for NMDA receptor activation alongside glutamate. MDL 100748 decreases response rates in operant conditioning sessions in phencyclidin (PCP)-trained rats. MDL 100748 can be used for reserach on dementias and schizophrenia.

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MDL 100748

MDL 100748 Chemical Structure

CAS No. : 130613-18-2

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Description

MDL 100748 is an NMDA receptor glycine site antagonist. MDL 100748 modulates NMDA receptor function by acting at the strychnine-insensitive glycine site, which is required for NMDA receptor activation alongside glutamate. MDL 100748 decreases response rates in operant conditioning sessions in phencyclidin (PCP)-trained rats. MDL 100748 can be used for reserach on dementias and schizophrenia[1].

IC50 & Target[1]

NMDA Receptor

 

In Vitro

MDL 100748 inhibits [3H]glycine binding to NMDA receptor glycine sites in rat brain membranes with an IC50 of 70 nM[2].

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

In Vivo

MDL 100748 (1-3 mg/kg; i.p.; single dose; 30 minutes prior to test sessions) produces no PCP-like discriminative stimulus effects in PCP-trained rats, with an ED50 of 3 mg/kg for suppressing operant response rates[1].

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

Animal Model: Sprague-Dawley (adult male; trained to discriminate 2 mg/kg PCP from saline via two-lever operant conditioning under FR32)[1]
Dosage: 1 mg/kg; 1.7 mg/kg; 3 mg/kg
Administration: i.p.; single dose; 30 minutes prior to test sessions
Result: Produced 0% PCP-lever selection across all tested doses.
Had an ED50 of 3 mg/kg for suppression of response rates.
Molecular Weight

315.11

Formula

C12H8Cl2N2O4

CAS No.
SMILES

O=C(C1=CC(NCC(O)=O)=C2C(Cl)=CC(Cl)=CC2=N1)O

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
References
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Product Name:
MDL 100748
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HY-182479
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