Phenylglycine derivatives as new pharmacological tools for investigating the role of metabotropic glutamate receptors in the central nervous system

Birse, E. F.; Eaton, S.A.; Jane, David E.; Jones, P. L. Saint J.; Porter, Richard H.; Pook, Peter C.K.; Sunter, David; Udvarhelyi, Peter M.; Wharton, B A; Roberts, Peter; Salt, Thomas E.; Watkins, Johnathan

doi:10.1016/0306-4522(93)90400-a

Cited by 141 publications

(79 citation statements)

References 33 publications

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“…In parallel with the cloning and functional characterization of the eight mGluRs which presently constitute the mGluR family (Nakanishi, 1994;Pin & Duvoisin, 1995) has been the synthesis of an increasing array of molecules which exhibit selective agonist or antagonist properties at this class of receptor (Hayashi et al, 1992;1994;Schoepp & Conn, 1993;Birse et al, 1994;Pin & Duvoisin, 1995). Although heterologous expression of specific mGluR subtypes can in theory provide almost unlimited supplies of material for pharmacological characterization of putative mGluR agonists/antagonists using radioligand binding methods, few studies have adopted this approach (Thomsen et al, 1993;Laurie et al, 1995) (Schoepp et al, 1991;Manzoni et al, 1992;Jones & Roberts, 1993;Challiss et al, 1994b).…”

Section: Discussionmentioning

confidence: 99%

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Mistry

Challiss

1996

British J Pharmacology

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Section: Discussionmentioning

confidence: 99%

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Mistry

Challiss

1996

British J Pharmacology

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“…[ 4 , 5 mM HEPES, and 10 mM D-glucose, pH 7.4, after equilibration with 95% O 2 /5% CO 2 ) at 37°. Where GPT and pyruvate were added to decrease medium glutamate concentrations, these agents were present for Ն15 min before any other manipulations were performed and Ն30 min before agonist challenge.…”

Section: Methodsmentioning

confidence: 99%

Enhanced Type 1α Metabotropic Glutamate Receptor-Stimulated Phosphoinositide Signaling after Pertussis Toxin Treatment

et al. 1997

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SUMMARYThe regulation of phosphoinositide hydrolysis by the type 1␣ metabotropic glutamate receptor (mGluR1␣) was investigated in stably transfected baby hamster kidney (BHK) cells. Incubation of the cells with L-glutamate, quisqualate, and 1-aminocyclopentane-1S,3R-dicarboxylic acid resulted in a marked accumulation of 3 H]InsP 1 responses were similar in control and PTXtreated BHK-mGluR1␣ cells. These changes in the concentration-effect curves for mGluR agonists are consistent with a model in which the receptor associates with PTX-sensitive inhibitory (G i/o ) and PTX-insensitive stimulatory (G q/11 ) G proteins that can each influence PIC activity. The present observations are consistent with a dual regulation of mGluR1␣-mediated PIC activity that could be fundamental in controlling the output of phosphoinositide-derived messengers.The recent cloning of eight subtypes of mGluR has not only opened up new avenues for exploration of the central actions of this excitatory neurotransmitter but also expanded the potential to target drugs against specific receptor-mediated actions (1-3). Recently, novel synthetic glutamate analogues have been developed as ligands at different mGluRs, and of particular significance has been the development of competitive antagonists (4 -7) and their use in identifying the involvement and roles of different mGluR subtypes in fundamental mechanisms such as long term potentiation and long term depression (8 -12).The mGluRs form a distinct branch of the G protein-coupled receptor superfamily, sharing topological organization but little sequence homology with other G protein-coupled receptors. Sequence homology and pharmacological profiling have allowed three subgroups of mGluRs, termed I, II, and III, to be described (2, 3). Group II mGluRs (types 2 and 3) and group III MGluRs (types 4, 6, 7 and 8) both couple to G proteins of the G i/o family to inhibit adenylyl cyclase or modulate ion channel activities (2, 3); in contrast, group I mGluRs (types 1 and 5) activate PIC with the subsequent generation of the second messengers Ins(1,4,5)P 3 and diacylglycerol (2, 3, 13-17). The G protein or proteins responsible for coupling group I mGluRs to PIC have been the subject of some debate. Thus, although the phosphoinositide responses elicited by agonist stimulation of mGluR5 and the mGluR1␤ splice variant seem to be little affected by PTX treatment (14,15), the response to mGluR1␣ activation is substantially

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“…In those papers the active compounds were named cyclopropylglutamate stereoisomers (CGA), to stress the analogy with glutamate; (lS,3S,4S)-CGA corresponded to L-CGA B and is here named L-CCG-I. The nomenclature used by Shinozaki et al (1989) (Ito et al, 1992;Eaton et al, 1993;Birse et al, 1993).…”

Section: Methodsmentioning

confidence: 99%

Pharmacological characterization of the metabotropic glutamate receptor inhibiting d‐[³H]‐aspartate output in rat striatum

Lombardi

Alesiani

Leonardi

et al. 1993

British J Pharmacology

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Phenylglycine derivatives as new pharmacological tools for investigating the role of metabotropic glutamate receptors in the central nervous system

Cited by 141 publications

References 33 publications

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Enhanced Type 1α Metabotropic Glutamate Receptor-Stimulated Phosphoinositide Signaling after Pertussis Toxin Treatment

Pharmacological characterization of the metabotropic glutamate receptor inhibiting d‐[³H]‐aspartate output in rat striatum

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Phenylglycine derivatives as new pharmacological tools for investigating the role of metabotropic glutamate receptors in the central nervous system

Cited by 141 publications

References 33 publications

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Differences in agonist and antagonist activities for two indices of metabotropic glutamate receptor‐stimulated phosphoinositide turnover

Enhanced Type 1α Metabotropic Glutamate Receptor-Stimulated Phosphoinositide Signaling after Pertussis Toxin Treatment

Pharmacological characterization of the metabotropic glutamate receptor inhibiting d‐[3H]‐aspartate output in rat striatum

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Pharmacological characterization of the metabotropic glutamate receptor inhibiting d‐[³H]‐aspartate output in rat striatum