Re‐evaluation of phencyclidine low‐affinity or “non‐NMDA” binding sites

@article{Hirbec2002ReevaluationOP,
  title={Re‐evaluation of phencyclidine low‐affinity or “non‐NMDA” binding sites},
  author={H{\'e}l{\`e}ne Hirbec and A L Mausset and Jean Marc Kamenka and Alain Privat and Jacques Vignon},
  journal={Journal of Neuroscience Research},
  year={2002},
  volume={68}
}
TCP and its derivative gacyclidine (± GK11) are high‐affinity non‐competitive antagonists of N‐methyl‐D‐aspartate (NMDA) receptors (NMDARs) and as such exhibit significant neuroprotective properties. These compounds also bind with a low affinity to binding sites whose pharmacological profiles are different from that of NMDARs. With the intention to develop new strategies of neuroprotection, we found it mandatory to investigate whether 1‐[1‐(2‐thienyl)cyclohexyl]piperidine (TCP) and gacyclidine… 
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This study demonstrates that the gacyclidine ‘non‐NMDA’ binding sites are associated with the dendritic trees of Purkinje cells, and shows that the radioligand binding to both cerebellar and telencephalic structures could be modulated by endogeneous factors which can be removed by a stringent prewashing procedure.
Differentiation of σ ligand‐activated receptor subtypes that modulate NMDA‐evoked [3H]‐noradrenaline release in rat hippocampal slices
1 It is now widely accepted that there are two classes of sigma (σ) binding sites, denoted σ1 and σ2, and recently σ3 subtype has been proposed. Selective σ1 and σ2 receptor agonists are known to
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