The effects of (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG), a potent and selective metabotropic glutamate receptor antagonist
1 In this study we describe the potent antagonist activity of a novel metabotropic glutamate (mGlu) receptor antagonist (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) which exhibits selectivity for mGlu receptors (group II and III) negatively coupled to adenylyl cyclase in the adult rat cor...
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| Veröffentlicht in: | British journal of pharmacology 1996-11, Vol.119 (5), p.851-854 |
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| container_title | British journal of pharmacology |
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| creator | Toms, Nicholas J. Jane, David E. Kemp, Martyn C. Bedingfield, Jennifer S. Roberts, Peter J. |
| description | 1
In this study we describe the potent antagonist activity of a novel metabotropic glutamate (mGlu) receptor antagonist (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) which exhibits selectivity for mGlu receptors (group II and III) negatively coupled to adenylyl cyclase in the adult rat cortex.
2
Both the L‐2‐amino‐4‐phosphonobutyrate (L‐AP4) and (2S, 1′S, 2′S)‐2‐(carboxycyclopropyl)glycine (L‐CCG‐1) inhibition of forskolin‐stimulated cyclic AMP accumulation were potently reversed by (RS)‐CPPG (IC50 values: 2.2 ± 0.6 nM and 46.2 ± 18.2 nM, respectively).
3
In contrast, (RS)‐CPPG acted as a weak antagonist against group I mGlu receptors. In neonatal rat cortical slices, (RS)‐CPPG antagonized (KB = 0.65 ± 0.07 mM) (1S, 3R)‐1‐aminocyclopentane‐1, 3‐dicarboxylic acid ((1S, 3R)‐ACPD)‐stimulated phosphoinositide hydrolysis. (RS)‐CPPG (100 μm) failed to influence L‐quisqualate‐stimulated phosphoinositide hydrolysis in cultured cerebellar granule cells.
4
In the rat cerebral cortex, (RS)‐CPPG is the most potent antagonist of group II/III mGlu receptors yet described (with 20 fold selectivity for group III mGlu receptors), having negligible activity at group I mGlu receptors. |
| doi_str_mv | 10.1111/j.1476-5381.1996.tb15750.x |
| format | Article |
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In this study we describe the potent antagonist activity of a novel metabotropic glutamate (mGlu) receptor antagonist (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) which exhibits selectivity for mGlu receptors (group II and III) negatively coupled to adenylyl cyclase in the adult rat cortex.
2
Both the L‐2‐amino‐4‐phosphonobutyrate (L‐AP4) and (2S, 1′S, 2′S)‐2‐(carboxycyclopropyl)glycine (L‐CCG‐1) inhibition of forskolin‐stimulated cyclic AMP accumulation were potently reversed by (RS)‐CPPG (IC50 values: 2.2 ± 0.6 nM and 46.2 ± 18.2 nM, respectively).
3
In contrast, (RS)‐CPPG acted as a weak antagonist against group I mGlu receptors. In neonatal rat cortical slices, (RS)‐CPPG antagonized (KB = 0.65 ± 0.07 mM) (1S, 3R)‐1‐aminocyclopentane‐1, 3‐dicarboxylic acid ((1S, 3R)‐ACPD)‐stimulated phosphoinositide hydrolysis. (RS)‐CPPG (100 μm) failed to influence L‐quisqualate‐stimulated phosphoinositide hydrolysis in cultured cerebellar granule cells.
4
In the rat cerebral cortex, (RS)‐CPPG is the most potent antagonist of group II/III mGlu receptors yet described (with 20 fold selectivity for group III mGlu receptors), having negligible activity at group I mGlu receptors.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1996.tb15750.x</identifier><identifier>PMID: 8922731</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>(RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) ; Animals ; Biological and medical sciences ; Cells, Cultured ; Cerebral Cortex - cytology ; Cerebral Cortex - drug effects ; Cerebral Cortex - metabolism ; cyclic AMP ; Excitatory Amino Acid Antagonists - pharmacology ; Glutamatergic system (aspartate and other excitatory aminoacids) ; Glycine - analogs & derivatives ; Glycine - pharmacology ; In Vitro Techniques ; Medical sciences ; metabotropic glutamate receptor antagonist ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; phosphoinositide hydrolysis ; Rats ; Receptors, Metabotropic Glutamate - antagonists & inhibitors</subject><ispartof>British journal of pharmacology, 1996-11, Vol.119 (5), p.851-854</ispartof><rights>1996 British Pharmacological Society</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5380-879cb4ddc5171c3843d267279d5941b07f84eabc2b23753647e83371b7fb7c603</citedby><cites>FETCH-LOGICAL-c5380-879cb4ddc5171c3843d267279d5941b07f84eabc2b23753647e83371b7fb7c603</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1915959/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1915959/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,1411,27901,27902,45550,45551,53766,53768</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3253385$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8922731$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Toms, Nicholas J.</creatorcontrib><creatorcontrib>Jane, David E.</creatorcontrib><creatorcontrib>Kemp, Martyn C.</creatorcontrib><creatorcontrib>Bedingfield, Jennifer S.</creatorcontrib><creatorcontrib>Roberts, Peter J.</creatorcontrib><title>The effects of (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG), a potent and selective metabotropic glutamate receptor antagonist</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
In this study we describe the potent antagonist activity of a novel metabotropic glutamate (mGlu) receptor antagonist (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) which exhibits selectivity for mGlu receptors (group II and III) negatively coupled to adenylyl cyclase in the adult rat cortex.
2
Both the L‐2‐amino‐4‐phosphonobutyrate (L‐AP4) and (2S, 1′S, 2′S)‐2‐(carboxycyclopropyl)glycine (L‐CCG‐1) inhibition of forskolin‐stimulated cyclic AMP accumulation were potently reversed by (RS)‐CPPG (IC50 values: 2.2 ± 0.6 nM and 46.2 ± 18.2 nM, respectively).
3
In contrast, (RS)‐CPPG acted as a weak antagonist against group I mGlu receptors. In neonatal rat cortical slices, (RS)‐CPPG antagonized (KB = 0.65 ± 0.07 mM) (1S, 3R)‐1‐aminocyclopentane‐1, 3‐dicarboxylic acid ((1S, 3R)‐ACPD)‐stimulated phosphoinositide hydrolysis. (RS)‐CPPG (100 μm) failed to influence L‐quisqualate‐stimulated phosphoinositide hydrolysis in cultured cerebellar granule cells.
4
In the rat cerebral cortex, (RS)‐CPPG is the most potent antagonist of group II/III mGlu receptors yet described (with 20 fold selectivity for group III mGlu receptors), having negligible activity at group I mGlu receptors.</description><subject>(RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG)</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cells, Cultured</subject><subject>Cerebral Cortex - cytology</subject><subject>Cerebral Cortex - drug effects</subject><subject>Cerebral Cortex - metabolism</subject><subject>cyclic AMP</subject><subject>Excitatory Amino Acid Antagonists - pharmacology</subject><subject>Glutamatergic system (aspartate and other excitatory aminoacids)</subject><subject>Glycine - analogs & derivatives</subject><subject>Glycine - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Medical sciences</subject><subject>metabotropic glutamate receptor antagonist</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>phosphoinositide hydrolysis</subject><subject>Rats</subject><subject>Receptors, Metabotropic Glutamate - antagonists & inhibitors</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkdGK1DAYhYso67j6CEIQkV2wNWmapvVC1EF3hQUHXa9Dmv6dyZBpuklm3d75CF74Ir6ID-GTmHHKoFdiIU3COf_hhC9JHhGckfg9W2ek4GXKaEUyUtdlFhrCOMPZza1kdpBuJzOMMU8Jqaq7yT3v1xhHkbOj5Kiq85xTMku-Xa4AQdeBCh7ZDp18-Hj688vXH9_jT43K2MHZYTTxVsQ1rKyPq7fDCvrRLM2odA_oZJqaLxZnp0-RRIMN0Ack-xZ5MDFbXwPaQJCNDTFPK7Q02yA3MgByoGAI1kV3kEvbax_uJ3c6aTw8mPbj5NPbN5fz8_Ti_dm7-auLVMX34bTitWqKtlWMcKJoVdA2L3nO65bVBWkw76oCZKPyJqec0bLgUFHKScO7hqsS0-PkxT532DYbaFXs7KQRg9Mb6UZhpRZ_K71eiaW9FqQmrGZ1DHgyBTh7tQUfxEZ7BcbIHuzWC16xIlZl_zRGfJEfI9H4fG9UznrvoDu0IVjs4Iu12BEWO8JiB19M8MVNHH7453sOoxPtqD-edOmVNJ2TvdL-YKM5o_uyL_e2z9rA-B8FxOvF-e8j_QW3ndRh</recordid><startdate>199611</startdate><enddate>199611</enddate><creator>Toms, Nicholas J.</creator><creator>Jane, David E.</creator><creator>Kemp, Martyn C.</creator><creator>Bedingfield, Jennifer S.</creator><creator>Roberts, Peter J.</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>199611</creationdate><title>The effects of (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG), a potent and selective metabotropic glutamate receptor antagonist</title><author>Toms, Nicholas J. ; Jane, David E. ; Kemp, Martyn C. ; Bedingfield, Jennifer S. ; Roberts, Peter J.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5380-879cb4ddc5171c3843d267279d5941b07f84eabc2b23753647e83371b7fb7c603</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>(RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG)</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cells, Cultured</topic><topic>Cerebral Cortex - cytology</topic><topic>Cerebral Cortex - drug effects</topic><topic>Cerebral Cortex - metabolism</topic><topic>cyclic AMP</topic><topic>Excitatory Amino Acid Antagonists - pharmacology</topic><topic>Glutamatergic system (aspartate and other excitatory aminoacids)</topic><topic>Glycine - analogs & derivatives</topic><topic>Glycine - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Medical sciences</topic><topic>metabotropic glutamate receptor antagonist</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. Drug treatments</topic><topic>phosphoinositide hydrolysis</topic><topic>Rats</topic><topic>Receptors, Metabotropic Glutamate - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Toms, Nicholas J.</creatorcontrib><creatorcontrib>Jane, David E.</creatorcontrib><creatorcontrib>Kemp, Martyn C.</creatorcontrib><creatorcontrib>Bedingfield, Jennifer S.</creatorcontrib><creatorcontrib>Roberts, Peter J.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Toms, Nicholas J.</au><au>Jane, David E.</au><au>Kemp, Martyn C.</au><au>Bedingfield, Jennifer S.</au><au>Roberts, Peter J.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effects of (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG), a potent and selective metabotropic glutamate receptor antagonist</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1996-11</date><risdate>1996</risdate><volume>119</volume><issue>5</issue><spage>851</spage><epage>854</epage><pages>851-854</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
In this study we describe the potent antagonist activity of a novel metabotropic glutamate (mGlu) receptor antagonist (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) which exhibits selectivity for mGlu receptors (group II and III) negatively coupled to adenylyl cyclase in the adult rat cortex.
2
Both the L‐2‐amino‐4‐phosphonobutyrate (L‐AP4) and (2S, 1′S, 2′S)‐2‐(carboxycyclopropyl)glycine (L‐CCG‐1) inhibition of forskolin‐stimulated cyclic AMP accumulation were potently reversed by (RS)‐CPPG (IC50 values: 2.2 ± 0.6 nM and 46.2 ± 18.2 nM, respectively).
3
In contrast, (RS)‐CPPG acted as a weak antagonist against group I mGlu receptors. In neonatal rat cortical slices, (RS)‐CPPG antagonized (KB = 0.65 ± 0.07 mM) (1S, 3R)‐1‐aminocyclopentane‐1, 3‐dicarboxylic acid ((1S, 3R)‐ACPD)‐stimulated phosphoinositide hydrolysis. (RS)‐CPPG (100 μm) failed to influence L‐quisqualate‐stimulated phosphoinositide hydrolysis in cultured cerebellar granule cells.
4
In the rat cerebral cortex, (RS)‐CPPG is the most potent antagonist of group II/III mGlu receptors yet described (with 20 fold selectivity for group III mGlu receptors), having negligible activity at group I mGlu receptors.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>8922731</pmid><doi>10.1111/j.1476-5381.1996.tb15750.x</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Wiley Online Library Journals Frontfile Complete; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Alma/SFX Local Collection |
| subjects | (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG) Animals Biological and medical sciences Cells, Cultured Cerebral Cortex - cytology Cerebral Cortex - drug effects Cerebral Cortex - metabolism cyclic AMP Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Glycine - analogs & derivatives Glycine - pharmacology In Vitro Techniques Medical sciences metabotropic glutamate receptor antagonist Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments phosphoinositide hydrolysis Rats Receptors, Metabotropic Glutamate - antagonists & inhibitors |
| title | The effects of (RS)‐α‐cyclopropyl‐4‐phosphonophenylglycine ((RS)‐CPPG), a potent and selective metabotropic glutamate receptor antagonist |
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