What question did this study set out to answer?

To characterize the pharmacological profile, binding kinetics, and anatomical distribution of the radioligand [3H]DCG IV in rat brain cortex homogenates and tissue sections.

December 1, 1998Journal of NeurochemistryOpen Access

Characterization of (2S,2′R,3′R)‐2‐(2′,3′‐3H‐Dicarboxycyclopropyl)glycine Binding in Rat Brain

View Full Paper

Ask AI

Bookmark

Authors

VMVincent MutelUniversité Claude Bernard Lyon 1 GAGeo AdamUniversity of Singaperbangsa Karawang SCSylvie ChabozRoche (Switzerland)

Discussion

Member takes

Implication

In vitro binding assays demonstrate selective labeling of group II metabotropic glutamate receptors in rat brain, highlighting its utility as a pharmacological probe.

Key Points

To characterize the pharmacological profile, binding kinetics, and anatomical distribution of the radioligand [3H]DCG IV in rat brain cortex homogenates and tissue sections.
Conducted saturation and competitive binding assays in vitro using rat brain cortex homogenates with [3H]DCG IV in the presence of various glutamate receptor ligands.
Evaluated the regulatory effects of GTPgammaS, reducing agents, and CdCl2 on radioligand binding.
Mapped receptor distribution across rat brain regions using autoradiography on parasagittal brain sections.
Saturation binding in cortex homogenates identified a single saturable binding site with a KD of 180 +/- 33 nM, a Bmax of 780 +/- 70 fmol/mg protein, and nonspecific binding <30%.
Competitive inhibition revealed high affinity for group II metabotropic ligands (potency rank order: LY341495 = LY354740 > DCG IV = L-CCG-I), while NMDA, AMPA, and kainate were inactive up to 1 mM.
Autoradiography revealed high specific binding in the accessory olfactory bulb, caudate putamen, cerebellar granular layer, specific cortical layers (1, 3, and 4 > 2, 5, and 6), and hippocampal molecular layers.

Cite This Study

Mutel et al. (1998) studied this question.

synapsesocial.com/papers/6ab0e96ea36f39afe37ff14d https://doi.org/10.1046/j.1471-4159.1998.71062558.x

View Full Paper

Ask AI

Bookmark

Implication

In vitro binding assays demonstrate selective labeling of group II metabotropic glutamate receptors in rat brain, highlighting its utility as a pharmacological probe.

Characterization of (2S,2′R,3′R)‐2‐(2′,3′‐3H‐Dicarboxycyclopropyl)glycine Binding in Rat Brain

Discussion

Member takes

Implication

Key Points

Cite This Study

Characterization of (2S,2′R,3′R)‐2‐(2′,3′‐3H‐Dicarboxycyclopropyl)glycine Binding in Rat Brain

Discussion

Member takes

Implication

Key Points

Cite This Study

Also Consider

Also Consider