The effect of silyl substituted methotrexate in the treatment of experimental allergic encephalomyelitis in rats mediated by T-line cells
The effect of methotrexate and of silyl-methothrexate were compared in the treatment of experimental allergic encephalomyelitis (EAE) mediated by T-line lymphocytes. It was demonstrated that, during the first three days after cell transfer, no difference between methotrexate and its silyl derivative...
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Veröffentlicht in: | Neuropharmacology 1987-02, Vol.26 (2), p.255-260 |
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creator | Przuntek, H. Westarp, M.E. Vohl, M.L. Gerlach, M. Jutzi, P. Wekerle, H. |
description | The effect of methotrexate and of silyl-methothrexate were compared in the treatment of experimental allergic encephalomyelitis (EAE) mediated by T-line lymphocytes. It was demonstrated that, during the first three days after cell transfer, no difference between methotrexate and its silyl derivative could be seen. At a time when the cytotoxic lymphoblasts must have penetrated the blood brain barrier, only silyl methotrexate was able to prevent severe paralysis and death of the animals. It is suggested that the effect of N,N,O,O-Tetrakis (
t-butyldimethylsilyl)-methotrexate, (N-4-N-(2,3-bis-t-butyldimethylsilyl-amino-6-pteridinyl-methyl)-methylamino-benzoyl-glutamic acid-bis-(
t-butyldimethylsilyl)-ester), depends on the increased lipid solubility and permeability of the blood brain barrier of silylated drugs. |
doi_str_mv | 10.1016/0028-3908(87)90216-4 |
format | Article |
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t-butyldimethylsilyl)-methotrexate, (N-4-N-(2,3-bis-t-butyldimethylsilyl-amino-6-pteridinyl-methyl)-methylamino-benzoyl-glutamic acid-bis-(
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t-butyldimethylsilyl)-methotrexate, (N-4-N-(2,3-bis-t-butyldimethylsilyl-amino-6-pteridinyl-methyl)-methylamino-benzoyl-glutamic acid-bis-(
t-butyldimethylsilyl)-ester), depends on the increased lipid solubility and permeability of the blood brain barrier of silylated drugs.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Encephalomyelitis, Autoimmune, Experimental - drug therapy</subject><subject>Female</subject><subject>Immunomodulators</subject><subject>Medical sciences</subject><subject>Methotrexate - analogs & derivatives</subject><subject>Methotrexate - therapeutic use</subject><subject>Mice</subject><subject>Mice, Inbred Strains</subject><subject>Pharmacology. Drug treatments</subject><subject>T-Lymphocytes - physiology</subject><issn>0028-3908</issn><issn>1873-7064</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kc-KFDEQxoMo67j6Bgo5iOihtTJJJ-nLgiz-gwUv4zlkkooTyXSPSVp2HsG3Nr0zzNFTUdTv-6j6ipCXDN4zYPIDwFp3fAD9Vqt3A6yZ7MQjsmJa8U6BFI_J6oI8Jc9K-QUAQjN9Ra64GHolxIr83eyQYgjoKp0CLTEdEy3zttRY54qe7rHupprx3lakcaS18a21dY_jgwTvD5jj0tlEbUqYf0ZHcXR42Nk07Y-YYo1l0WZbSzP00S7O2yPddCmOSB2mVJ6TJ8Gmgi_O9Zr8-Pxpc_u1u_v-5dvtx7vOcS1r50SQgffKAiAgcu_XUnqNAQIMTq8ZY9YPFpTy2GsmLOul6gPbgmQMueXX5M3J95Cn3zOWavaxLBvYEae5GKV6PvCeNVCcQJenUjIGc2h32nw0DMzyAbPEa5Z4jVbm4QNGNNmrs_-8bbdeROfI2_z1eW6LsylkO7pYLpgSA-sVNOzmhGHL4k_EbIqLS6o-5vYs46f4_z3-AZdJpKM</recordid><startdate>19870201</startdate><enddate>19870201</enddate><creator>Przuntek, H.</creator><creator>Westarp, M.E.</creator><creator>Vohl, M.L.</creator><creator>Gerlach, M.</creator><creator>Jutzi, P.</creator><creator>Wekerle, H.</creator><general>Elsevier Ltd</general><general>Elsevier</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>7X8</scope></search><sort><creationdate>19870201</creationdate><title>The effect of silyl substituted methotrexate in the treatment of experimental allergic encephalomyelitis in rats mediated by T-line cells</title><author>Przuntek, H. ; Westarp, M.E. ; Vohl, M.L. ; Gerlach, M. ; Jutzi, P. ; Wekerle, H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-c4f6f357a00e0ee3dd266d8ef0f09c82111ad9a077de5814a15675f1b0611e3a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Encephalomyelitis, Autoimmune, Experimental - drug therapy</topic><topic>Female</topic><topic>Immunomodulators</topic><topic>Medical sciences</topic><topic>Methotrexate - analogs & derivatives</topic><topic>Methotrexate - therapeutic use</topic><topic>Mice</topic><topic>Mice, Inbred Strains</topic><topic>Pharmacology. Drug treatments</topic><topic>T-Lymphocytes - physiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Przuntek, H.</creatorcontrib><creatorcontrib>Westarp, M.E.</creatorcontrib><creatorcontrib>Vohl, M.L.</creatorcontrib><creatorcontrib>Gerlach, M.</creatorcontrib><creatorcontrib>Jutzi, P.</creatorcontrib><creatorcontrib>Wekerle, H.</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>MEDLINE - Academic</collection><jtitle>Neuropharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Przuntek, H.</au><au>Westarp, M.E.</au><au>Vohl, M.L.</au><au>Gerlach, M.</au><au>Jutzi, P.</au><au>Wekerle, H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effect of silyl substituted methotrexate in the treatment of experimental allergic encephalomyelitis in rats mediated by T-line cells</atitle><jtitle>Neuropharmacology</jtitle><addtitle>Neuropharmacology</addtitle><date>1987-02-01</date><risdate>1987</risdate><volume>26</volume><issue>2</issue><spage>255</spage><epage>260</epage><pages>255-260</pages><issn>0028-3908</issn><eissn>1873-7064</eissn><coden>NEPHBW</coden><abstract>The effect of methotrexate and of silyl-methothrexate were compared in the treatment of experimental allergic encephalomyelitis (EAE) mediated by T-line lymphocytes. It was demonstrated that, during the first three days after cell transfer, no difference between methotrexate and its silyl derivative could be seen. At a time when the cytotoxic lymphoblasts must have penetrated the blood brain barrier, only silyl methotrexate was able to prevent severe paralysis and death of the animals. It is suggested that the effect of N,N,O,O-Tetrakis (
t-butyldimethylsilyl)-methotrexate, (N-4-N-(2,3-bis-t-butyldimethylsilyl-amino-6-pteridinyl-methyl)-methylamino-benzoyl-glutamic acid-bis-(
t-butyldimethylsilyl)-ester), depends on the increased lipid solubility and permeability of the blood brain barrier of silylated drugs.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>3495744</pmid><doi>10.1016/0028-3908(87)90216-4</doi><tpages>6</tpages></addata></record> |
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subjects | Animals Biological and medical sciences Encephalomyelitis, Autoimmune, Experimental - drug therapy Female Immunomodulators Medical sciences Methotrexate - analogs & derivatives Methotrexate - therapeutic use Mice Mice, Inbred Strains Pharmacology. Drug treatments T-Lymphocytes - physiology |
title | The effect of silyl substituted methotrexate in the treatment of experimental allergic encephalomyelitis in rats mediated by T-line cells |
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