New Pharmacologic Aspects of β-Diethyl-Aminoethyl 2,2-Diphenylpentanoate
In a comparison with atropine and structurally related adiphenine using a gross in vivo screen in rats, β-diethyl-aminoethyl 2,2-diphenylpentanoate (SKF 525-A) appeared to act peripherally as a parasympatholytic and/or sympathomimetic. SKF 525-A apparently has some selective activity on the central...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 1966-06, Vol.55 (6), p.563-567 |
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| container_title | Journal of pharmaceutical sciences |
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| creator | Carrano, Richard A. Malone, Marvin H. |
| description | In a comparison with atropine and structurally related adiphenine using a gross in vivo screen in rats, β-diethyl-aminoethyl 2,2-diphenylpentanoate (SKF 525-A) appeared to act peripherally as a parasympatholytic and/or sympathomimetic. SKF 525-A apparently has some selective activity on the central nervous system (blepharoptosis, hypothermia) indicating a capacity to cross the blood-brain barrier. Drug-receptor interactions were studied on the isolated rat jejunum using furtrethonium as the agonist. SKF 525-A was primarily a noncompetitive antagonist with a competitive component and qualitatively different from the activities of atropine, adiphenine, and papaverine. The respective pA2 and pD'2 values are reported. The SKF 525-A receptor appears composed of the cholinergic receptor plus another spasmogen receptor. SKF 525-A did not inhibit the action of acetylcholinesterase, but was a potent inhibitor of monoamine oxidase at physiological concentrations. |
| doi_str_mv | 10.1002/jps.2600550606 |
| format | Article |
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SKF 525-A apparently has some selective activity on the central nervous system (blepharoptosis, hypothermia) indicating a capacity to cross the blood-brain barrier. Drug-receptor interactions were studied on the isolated rat jejunum using furtrethonium as the agonist. SKF 525-A was primarily a noncompetitive antagonist with a competitive component and qualitatively different from the activities of atropine, adiphenine, and papaverine. The respective pA2 and pD'2 values are reported. The SKF 525-A receptor appears composed of the cholinergic receptor plus another spasmogen receptor. SKF 525-A did not inhibit the action of acetylcholinesterase, but was a potent inhibitor of monoamine oxidase at physiological concentrations.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600550606</identifier><identifier>PMID: 4380795</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>Animals ; Atropine - pharmacology ; Diphenylacetic Acids - pharmacology ; In Vitro Techniques ; Jejunum - drug effects ; Monoamine Oxidase Inhibitors - pharmacology ; Parasympatholytics - pharmacology ; Proadifen - pharmacology ; Rats ; Spectrophotometry ; Sympathomimetics - pharmacology</subject><ispartof>Journal of pharmaceutical sciences, 1966-06, Vol.55 (6), p.563-567</ispartof><rights>1966 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1966 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3426-e1152273deac5bc4262bc347371827543195b82682a7c00caed481d4d363e1433</citedby><cites>FETCH-LOGICAL-c3426-e1152273deac5bc4262bc347371827543195b82682a7c00caed481d4d363e1433</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.2600550606$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600550606$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4380795$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Carrano, Richard A.</creatorcontrib><creatorcontrib>Malone, Marvin H.</creatorcontrib><title>New Pharmacologic Aspects of β-Diethyl-Aminoethyl 2,2-Diphenylpentanoate</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>In a comparison with atropine and structurally related adiphenine using a gross in vivo screen in rats, β-diethyl-aminoethyl 2,2-diphenylpentanoate (SKF 525-A) appeared to act peripherally as a parasympatholytic and/or sympathomimetic. SKF 525-A apparently has some selective activity on the central nervous system (blepharoptosis, hypothermia) indicating a capacity to cross the blood-brain barrier. Drug-receptor interactions were studied on the isolated rat jejunum using furtrethonium as the agonist. SKF 525-A was primarily a noncompetitive antagonist with a competitive component and qualitatively different from the activities of atropine, adiphenine, and papaverine. The respective pA2 and pD'2 values are reported. The SKF 525-A receptor appears composed of the cholinergic receptor plus another spasmogen receptor. SKF 525-A did not inhibit the action of acetylcholinesterase, but was a potent inhibitor of monoamine oxidase at physiological concentrations.</description><subject>Animals</subject><subject>Atropine - pharmacology</subject><subject>Diphenylacetic Acids - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Jejunum - drug effects</subject><subject>Monoamine Oxidase Inhibitors - pharmacology</subject><subject>Parasympatholytics - pharmacology</subject><subject>Proadifen - pharmacology</subject><subject>Rats</subject><subject>Spectrophotometry</subject><subject>Sympathomimetics - pharmacology</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1966</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc2O0zAUhS3EqHQKW3ZIWbEixT9x4i7L_JQyVRlKEewsx7mlLkkc7HRKXosH4ZnGQ6oiFoiVrXu-c-R7jNBzgscEY_p61_gxTTHmHKc4fYSGhFMcp5hkj9EwADRmPJk8Qefe7zAODOcDNEiYwNmED9F8CYfodqtcpbQt7Vejo6lvQLc-spvo18_40kC77cp4Wpna_r5G9BUN42YLdVc2ULeqtqqFp-hso0oPz47nCH26vlpfvI0X72fzi-ki1iyhaQwkPJBmrAClea7DiOZByVhGBM14wsiE54KmgqpMY6wVFIkgRVKwlAFJGBuhl31u4-z3PfhWVsZrKEtVg917KRLKsaAigOMe1M5672AjG2cq5TpJsHzoTobu5J_uguHFMXmfV1Cc8GNZQZ_0-sGU0P0nTb67_fhXdtx7jW_hx8mr3DeZht25_LycyZsP6y9r_mYlV4EXPQ-hyjsDTnptoNZQGBd-RxbW_GuNewE_m84</recordid><startdate>196606</startdate><enddate>196606</enddate><creator>Carrano, Richard A.</creator><creator>Malone, Marvin H.</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>BSCLL</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>196606</creationdate><title>New Pharmacologic Aspects of β-Diethyl-Aminoethyl 2,2-Diphenylpentanoate</title><author>Carrano, Richard A. ; Malone, Marvin H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3426-e1152273deac5bc4262bc347371827543195b82682a7c00caed481d4d363e1433</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1966</creationdate><topic>Animals</topic><topic>Atropine - pharmacology</topic><topic>Diphenylacetic Acids - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Jejunum - drug effects</topic><topic>Monoamine Oxidase Inhibitors - pharmacology</topic><topic>Parasympatholytics - pharmacology</topic><topic>Proadifen - pharmacology</topic><topic>Rats</topic><topic>Spectrophotometry</topic><topic>Sympathomimetics - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Carrano, Richard A.</creatorcontrib><creatorcontrib>Malone, Marvin H.</creatorcontrib><collection>Istex</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>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Carrano, Richard A.</au><au>Malone, Marvin H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>New Pharmacologic Aspects of β-Diethyl-Aminoethyl 2,2-Diphenylpentanoate</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1966-06</date><risdate>1966</risdate><volume>55</volume><issue>6</issue><spage>563</spage><epage>567</epage><pages>563-567</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>In a comparison with atropine and structurally related adiphenine using a gross in vivo screen in rats, β-diethyl-aminoethyl 2,2-diphenylpentanoate (SKF 525-A) appeared to act peripherally as a parasympatholytic and/or sympathomimetic. SKF 525-A apparently has some selective activity on the central nervous system (blepharoptosis, hypothermia) indicating a capacity to cross the blood-brain barrier. Drug-receptor interactions were studied on the isolated rat jejunum using furtrethonium as the agonist. SKF 525-A was primarily a noncompetitive antagonist with a competitive component and qualitatively different from the activities of atropine, adiphenine, and papaverine. The respective pA2 and pD'2 values are reported. The SKF 525-A receptor appears composed of the cholinergic receptor plus another spasmogen receptor. SKF 525-A did not inhibit the action of acetylcholinesterase, but was a potent inhibitor of monoamine oxidase at physiological concentrations.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>4380795</pmid><doi>10.1002/jps.2600550606</doi><tpages>5</tpages></addata></record> |
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| ispartof | Journal of pharmaceutical sciences, 1966-06, Vol.55 (6), p.563-567 |
| issn | 0022-3549 1520-6017 |
| language | eng |
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| source | MEDLINE; Access via Wiley Online Library; Alma/SFX Local Collection |
| subjects | Animals Atropine - pharmacology Diphenylacetic Acids - pharmacology In Vitro Techniques Jejunum - drug effects Monoamine Oxidase Inhibitors - pharmacology Parasympatholytics - pharmacology Proadifen - pharmacology Rats Spectrophotometry Sympathomimetics - pharmacology |
| title | New Pharmacologic Aspects of β-Diethyl-Aminoethyl 2,2-Diphenylpentanoate |
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