{"title":"鉴定2-氨基-2-甲基-4-磷酸丁酸作为mGlu4a受体拮抗剂","authors":"Patricia A. Johansen , Michael B. Robinson","doi":"10.1016/0922-4106(95)90032-2","DOIUrl":null,"url":null,"abstract":"<div><p>2-Amino-2-methyl-4-phosphonobutanoic acid (MAP4) was tested for interactions with the mGlu<sub>4a</sub> receptor which when expressed in baby hamster kidney (BHK570) cells couples to inhibition of forskolin-stimulated cAMP production. MAP4 had no agonist activity at this receptor and caused a concentration-dependent inhibition of the reduction in forskolin-stimulated cyclic AMP formation elicited by L-2-amino-4-phosphonobutanoic acid (L-AP4). Inhibition by MAP4 was consistent with a competitive mechanism of action (Schild slope = 1.2) with a <em>K</em><sub>i</sub> of 190 μM. MAP4 is the first antagonist identified for the mGlu<sub>4a</sub> receptor.</p></div>","PeriodicalId":100502,"journal":{"name":"European Journal of Pharmacology: Molecular Pharmacology","volume":"290 2","pages":"Pages R1-R3"},"PeriodicalIF":0.0000,"publicationDate":"1995-07-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0922-4106(95)90032-2","citationCount":"21","resultStr":"{\"title\":\"Identification of 2-amino-2-methyl-4-phosphonobutanoic acid as an antagonist at the mGlu4a receptor\",\"authors\":\"Patricia A. Johansen , Michael B. Robinson\",\"doi\":\"10.1016/0922-4106(95)90032-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>2-Amino-2-methyl-4-phosphonobutanoic acid (MAP4) was tested for interactions with the mGlu<sub>4a</sub> receptor which when expressed in baby hamster kidney (BHK570) cells couples to inhibition of forskolin-stimulated cAMP production. MAP4 had no agonist activity at this receptor and caused a concentration-dependent inhibition of the reduction in forskolin-stimulated cyclic AMP formation elicited by L-2-amino-4-phosphonobutanoic acid (L-AP4). Inhibition by MAP4 was consistent with a competitive mechanism of action (Schild slope = 1.2) with a <em>K</em><sub>i</sub> of 190 μM. MAP4 is the first antagonist identified for the mGlu<sub>4a</sub> receptor.</p></div>\",\"PeriodicalId\":100502,\"journal\":{\"name\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"volume\":\"290 2\",\"pages\":\"Pages R1-R3\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-07-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0922-4106(95)90032-2\",\"citationCount\":\"21\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmacology: Molecular Pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/0922410695900322\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmacology: Molecular Pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0922410695900322","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Identification of 2-amino-2-methyl-4-phosphonobutanoic acid as an antagonist at the mGlu4a receptor
2-Amino-2-methyl-4-phosphonobutanoic acid (MAP4) was tested for interactions with the mGlu4a receptor which when expressed in baby hamster kidney (BHK570) cells couples to inhibition of forskolin-stimulated cAMP production. MAP4 had no agonist activity at this receptor and caused a concentration-dependent inhibition of the reduction in forskolin-stimulated cyclic AMP formation elicited by L-2-amino-4-phosphonobutanoic acid (L-AP4). Inhibition by MAP4 was consistent with a competitive mechanism of action (Schild slope = 1.2) with a Ki of 190 μM. MAP4 is the first antagonist identified for the mGlu4a receptor.
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