What question did this study set out to answer?

To characterize the in vitro binding properties, pharmacological selectivity, and anatomical distribution of [3H]Ro 25-6981 in the rat brain.

May 1, 1998Journal of NeurochemistryOpen Access

In Vitro Binding Properties in Rat Brain of 3HRo 25‐6981, a Potent and Selective Antagonist of NMDA Receptors Containing NR2B Subunits

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Authors

VMVincent MutelUniversité Claude Bernard Lyon 1 DBDanièle BuchyRoche (Switzerland)AKAgnès KlingelschmidtRoche (Switzerland)

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Implication

Radioligand binding study demonstrates selective, high-affinity binding of Ro 25-6981 to NR2B NMDA receptors in rat brain, indicating its utility for studying receptor expression.

Key Points

To characterize the in vitro binding properties, pharmacological selectivity, and anatomical distribution of [3H]Ro 25-6981 in the rat brain.
Conducted radioligand binding assays using [3H]Ro 25-6981 on rat brain membranes, defining specific binding with 10 µM Ro 04-5595.
Mapped anatomical receptor localization via quantitative autoradiography on rat brain sections and compared distribution against NR2A and NR2B transcript patterns determined by in situ hybridization.
[3H]Ro 25-6981 bound to a single site in rat brain membranes with a dissociation constant KD of 3 nM and a maximum binding capacity Bmax of 1.6 pmol/mg of protein.
Specific binding was fully inhibited by selective antagonists in rank order: Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol, and partially inhibited by competitive glutamate site antagonists.
High densities of binding sites occurred in the cerebral cortex, hippocampus, and caudate putamen, mirroring the anatomical expression of NR2B, but not NR2A, mRNA.

Cite This Study

Mutel et al. (1998) studied this question.

synapsesocial.com/papers/6a83f9663fd01c19a6c58b9c https://doi.org/10.1046/j.1471-4159.1998.70052147.x

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Implication

Radioligand binding study demonstrates selective, high-affinity binding of Ro 25-6981 to NR2B NMDA receptors in rat brain, indicating its utility for studying receptor expression.

In Vitro Binding Properties in Rat Brain of 3HRo 25‐6981, a Potent and Selective Antagonist of NMDA Receptors Containing NR2B Subunits

Discussion

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Implication

Key Points

Cite This Study

In Vitro Binding Properties in Rat Brain of 3HRo 25‐6981, a Potent and Selective Antagonist of NMDA Receptors Containing NR2B Subunits

Discussion

Member takes

Implication

Key Points

Cite This Study

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