Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists

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Abstract

Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.

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Acknowledgments

SSK was supported by a NIH-visiting fellowship. We thank Dr. Mu-Fa Zou for critically reading this manuscript. We acknowledge Ms. Barbara Nightingale for technical assistance, Dr. Bryan Roth, Director of the National Institute on Mental Health-Psychoactive Drug Screening Program (PDSP), for his support and Ms. Estela Lopez for help with the PDSP database. This work was supported by the NIDA-IRP, NIH.

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