Literature DB >> 9886688

Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1alpha metabotropic glutamate receptor.

E Hermans1, S R Nahorski, R A Challiss.   

Abstract

In transfected CHO cells expressing the human metabotropic glutamate receptor mGlu1alpha, 7-(hydroxyimino)cyclopropan[b]-chromen-1a-carboxylic acid ethylester (CPCCOEt) was found to antagonize L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner (apparent pKi value, 4.76+/-0.18; n=3). This suggests that CPCCOEt antagonizes type 1alpha metabotropic glutamate receptor activation by interacting with a site distinct from the agonist binding site.

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Year:  1998        PMID： 9886688     DOI： 10.1016/s0028-3908(98)00132-4

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN： 0028-3908            Impact factor:   5.250


  9 in total

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8.  Improved Visualization and Specific Binding for Metabotropic Glutamate Receptor Subtype 1 (mGluR1) Using [11C]ITMM with Ultra-High Specific Activity in Small-Animal PET.

Authors:  Tomoteru Yamasaki; Masayuki Fujinaga; Joji Yui; Hidekatsu Wakizaka; Tomoyuki Ohya; Nobuki Nengaki; Masanao Ogawa; Yoko Ikoma; Akiko Hatori; Lin Xie; Kazunori Kawamura; Ming-Rong Zhang
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Review 9.  Presynaptic Release-regulating Metabotropic Glutamate Receptors: An Update.

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  9 in total

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