Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats
The effects of bifemelane hydrochloride (BF) upon various cholinergic markers, muscarinic receptors, acetylcholinesterase (AChE) and choline acetyl-transferase (CAT), in the aged rat brain were examined. Marked reduction of the density of muscarinic receptors (Bmax) as well as AChE and CAT activity...
Gespeichert in:
| Veröffentlicht in: | Japanese Journal of Pharmacology 1989-01, Vol.51 (2), p.211-218 |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 218 |
|---|---|
| container_issue | 2 |
| container_start_page | 211 |
| container_title | Japanese Journal of Pharmacology |
| container_volume | 51 |
| creator | EGASHIRA, Tom NAGAI, Takayuki KIMBA, Yoshihira TAKANO, Ritsuko YAMANAKA, Yasumitsu |
| description | The effects of bifemelane hydrochloride (BF) upon various cholinergic markers, muscarinic receptors, acetylcholinesterase (AChE) and choline acetyl-transferase (CAT), in the aged rat brain were examined. Marked reduction of the density of muscarinic receptors (Bmax) as well as AChE and CAT activity concomitant with aging was observed. Administration of BF in daily doses of 10 mg/kg for 4 weeks to aged rats significantly decreased the apparent dissociation constant (K4) for QNB in muscarinic receptors in the forebrain, but did not affect the value of Bmax. CAT activity also increased significantly compared with that of control aged rats, but administration of BF did not alter AChE activity. These results indicate that long-term treatment with BF enhances the affinity of muscarinic receptors for QNB as well as CAT activity and that BF may have therapeutic application in the treatment of CNS cholinergic dysfunctions. |
| doi_str_mv | 10.1016/S0021-5198(19)40118-2 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_79364962</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0021519819401182</els_id><sourcerecordid>15484478</sourcerecordid><originalsourceid>FETCH-LOGICAL-c4532-eeee3ebfbaf7d53a12da73388605f3fb9fcf997222152e82338f9a06e60d8a8c3</originalsourceid><addsrcrecordid>eNqNkk1vEzEQhi0EKmnhJ1TyASF6WPDH2mufUIlKi1SE1AJXy_GOU4eNHewsUv893iTkWnzwyJrX73jmMULnlLynhMoP94Qw2giq1TuqL1pCqWrYMzSjvO0aLoh8jmZHyUt0WsqqHhWh7Qk6YUJz3qkZKlfeg9sWnDz-FDysYbAR8M1jn5N7GFIOPeAU8U-bQxoLnj-kIUTIy-DwV5t_QS44RDxPeRucHbCNPb4fF-7f-Q6WIcWd_eUSenxnt-UVeuHtUOD1IZ6hH5-vvs9vmttv11_ml7eNawVnDdTFYeEX1ne94Jay3nacKyWJ8NwvtHde644xRgUDxWrKa0skSNIrqxw_Q2_3vpucfo9QtmYdioNh6rD2YjrNZasle1JIheJSdOo_hK1q251Q7IUup1IyeLPJYW3zo6HETPjMDp-Z2BiqzQ6fmV5yfigwLtbQH28deNX8m0Peljpen210oRxlUlJGBK-y672sekwYUpygmVUac6wTN87L1SpthlpaaUOIoITVoEx9E502RQmRXddWp497J6ig_gTIprgA0VXfXP-N6VN4oqW_WRzM7w</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>15484478</pqid></control><display><type>article</type><title>Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats</title><source>MEDLINE</source><source>J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Free Full-Text Journals in Chemistry</source><creator>EGASHIRA, Tom ; NAGAI, Takayuki ; KIMBA, Yoshihira ; TAKANO, Ritsuko ; YAMANAKA, Yasumitsu</creator><creatorcontrib>EGASHIRA, Tom ; NAGAI, Takayuki ; KIMBA, Yoshihira ; TAKANO, Ritsuko ; YAMANAKA, Yasumitsu ; Medical College of Oita ; Department of Pharmacology</creatorcontrib><description>The effects of bifemelane hydrochloride (BF) upon various cholinergic markers, muscarinic receptors, acetylcholinesterase (AChE) and choline acetyl-transferase (CAT), in the aged rat brain were examined. Marked reduction of the density of muscarinic receptors (Bmax) as well as AChE and CAT activity concomitant with aging was observed. Administration of BF in daily doses of 10 mg/kg for 4 weeks to aged rats significantly decreased the apparent dissociation constant (K4) for QNB in muscarinic receptors in the forebrain, but did not affect the value of Bmax. CAT activity also increased significantly compared with that of control aged rats, but administration of BF did not alter AChE activity. These results indicate that long-term treatment with BF enhances the affinity of muscarinic receptors for QNB as well as CAT activity and that BF may have therapeutic application in the treatment of CNS cholinergic dysfunctions.</description><identifier>ISSN: 0021-5198</identifier><identifier>EISSN: 1347-3506</identifier><identifier>DOI: 10.1016/S0021-5198(19)40118-2</identifier><identifier>PMID: 2593378</identifier><identifier>CODEN: JJPAAZ</identifier><language>eng</language><publisher>Kyoto: The Japanese Pharmacological Society</publisher><subject>Acetylcholinesterase - metabolism ; Aging - physiology ; Animals ; Antidepressive Agents - pharmacology ; Benzhydryl Compounds - pharmacology ; Biological and medical sciences ; Brain - drug effects ; Brain - enzymology ; Cerebral Cortex - drug effects ; Cerebral Cortex - enzymology ; Choline O-Acetyltransferase - antagonists & inhibitors ; Cholinesterase Inhibitors - pharmacology ; Kinetics ; Male ; Medical sciences ; Nerve Tissue Proteins - metabolism ; Neuropharmacology ; Parasympathetic Nervous System - drug effects ; Pharmacology. Drug treatments ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Rats ; Rats, Inbred Strains ; Receptors, Muscarinic - drug effects</subject><ispartof>Japanese Journal of Pharmacology, 1989-01, Vol.51 (2), p.211-218</ispartof><rights>1989 Elsevier B.V.</rights><rights>1990 INIST-CNRS</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4532-eeee3ebfbaf7d53a12da73388605f3fb9fcf997222152e82338f9a06e60d8a8c3</citedby><cites>FETCH-LOGICAL-c4532-eeee3ebfbaf7d53a12da73388605f3fb9fcf997222152e82338f9a06e60d8a8c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=6612053$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2593378$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>EGASHIRA, Tom</creatorcontrib><creatorcontrib>NAGAI, Takayuki</creatorcontrib><creatorcontrib>KIMBA, Yoshihira</creatorcontrib><creatorcontrib>TAKANO, Ritsuko</creatorcontrib><creatorcontrib>YAMANAKA, Yasumitsu</creatorcontrib><creatorcontrib>Medical College of Oita</creatorcontrib><creatorcontrib>Department of Pharmacology</creatorcontrib><title>Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats</title><title>Japanese Journal of Pharmacology</title><addtitle>Jpn J Pharmacol</addtitle><description>The effects of bifemelane hydrochloride (BF) upon various cholinergic markers, muscarinic receptors, acetylcholinesterase (AChE) and choline acetyl-transferase (CAT), in the aged rat brain were examined. Marked reduction of the density of muscarinic receptors (Bmax) as well as AChE and CAT activity concomitant with aging was observed. Administration of BF in daily doses of 10 mg/kg for 4 weeks to aged rats significantly decreased the apparent dissociation constant (K4) for QNB in muscarinic receptors in the forebrain, but did not affect the value of Bmax. CAT activity also increased significantly compared with that of control aged rats, but administration of BF did not alter AChE activity. These results indicate that long-term treatment with BF enhances the affinity of muscarinic receptors for QNB as well as CAT activity and that BF may have therapeutic application in the treatment of CNS cholinergic dysfunctions.</description><subject>Acetylcholinesterase - metabolism</subject><subject>Aging - physiology</subject><subject>Animals</subject><subject>Antidepressive Agents - pharmacology</subject><subject>Benzhydryl Compounds - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Brain - drug effects</subject><subject>Brain - enzymology</subject><subject>Cerebral Cortex - drug effects</subject><subject>Cerebral Cortex - enzymology</subject><subject>Choline O-Acetyltransferase - antagonists & inhibitors</subject><subject>Cholinesterase Inhibitors - pharmacology</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Nerve Tissue Proteins - metabolism</subject><subject>Neuropharmacology</subject><subject>Parasympathetic Nervous System - drug effects</subject><subject>Pharmacology. Drug treatments</subject><subject>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Muscarinic - drug effects</subject><issn>0021-5198</issn><issn>1347-3506</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkk1vEzEQhi0EKmnhJ1TyASF6WPDH2mufUIlKi1SE1AJXy_GOU4eNHewsUv893iTkWnzwyJrX73jmMULnlLynhMoP94Qw2giq1TuqL1pCqWrYMzSjvO0aLoh8jmZHyUt0WsqqHhWh7Qk6YUJz3qkZKlfeg9sWnDz-FDysYbAR8M1jn5N7GFIOPeAU8U-bQxoLnj-kIUTIy-DwV5t_QS44RDxPeRucHbCNPb4fF-7f-Q6WIcWd_eUSenxnt-UVeuHtUOD1IZ6hH5-vvs9vmttv11_ml7eNawVnDdTFYeEX1ne94Jay3nacKyWJ8NwvtHde644xRgUDxWrKa0skSNIrqxw_Q2_3vpucfo9QtmYdioNh6rD2YjrNZasle1JIheJSdOo_hK1q251Q7IUup1IyeLPJYW3zo6HETPjMDp-Z2BiqzQ6fmV5yfigwLtbQH28deNX8m0Peljpen210oRxlUlJGBK-y672sekwYUpygmVUac6wTN87L1SpthlpaaUOIoITVoEx9E502RQmRXddWp497J6ig_gTIprgA0VXfXP-N6VN4oqW_WRzM7w</recordid><startdate>19890101</startdate><enddate>19890101</enddate><creator>EGASHIRA, Tom</creator><creator>NAGAI, Takayuki</creator><creator>KIMBA, Yoshihira</creator><creator>TAKANO, Ritsuko</creator><creator>YAMANAKA, Yasumitsu</creator><general>The Japanese Pharmacological Society</general><general>Japanese Pharmacological Society</general><scope>6I.</scope><scope>AAFTH</scope><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></search><sort><creationdate>19890101</creationdate><title>Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats</title><author>EGASHIRA, Tom ; NAGAI, Takayuki ; KIMBA, Yoshihira ; TAKANO, Ritsuko ; YAMANAKA, Yasumitsu</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4532-eeee3ebfbaf7d53a12da73388605f3fb9fcf997222152e82338f9a06e60d8a8c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Acetylcholinesterase - metabolism</topic><topic>Aging - physiology</topic><topic>Animals</topic><topic>Antidepressive Agents - pharmacology</topic><topic>Benzhydryl Compounds - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Brain - drug effects</topic><topic>Brain - enzymology</topic><topic>Cerebral Cortex - drug effects</topic><topic>Cerebral Cortex - enzymology</topic><topic>Choline O-Acetyltransferase - antagonists & inhibitors</topic><topic>Cholinesterase Inhibitors - pharmacology</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Nerve Tissue Proteins - metabolism</topic><topic>Neuropharmacology</topic><topic>Parasympathetic Nervous System - drug effects</topic><topic>Pharmacology. Drug treatments</topic><topic>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Muscarinic - drug effects</topic><toplevel>online_resources</toplevel><creatorcontrib>EGASHIRA, Tom</creatorcontrib><creatorcontrib>NAGAI, Takayuki</creatorcontrib><creatorcontrib>KIMBA, Yoshihira</creatorcontrib><creatorcontrib>TAKANO, Ritsuko</creatorcontrib><creatorcontrib>YAMANAKA, Yasumitsu</creatorcontrib><creatorcontrib>Medical College of Oita</creatorcontrib><creatorcontrib>Department of Pharmacology</creatorcontrib><collection>ScienceDirect Open Access Titles</collection><collection>Elsevier:ScienceDirect:Open Access</collection><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><jtitle>Japanese Journal of Pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>EGASHIRA, Tom</au><au>NAGAI, Takayuki</au><au>KIMBA, Yoshihira</au><au>TAKANO, Ritsuko</au><au>YAMANAKA, Yasumitsu</au><aucorp>Medical College of Oita</aucorp><aucorp>Department of Pharmacology</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats</atitle><jtitle>Japanese Journal of Pharmacology</jtitle><addtitle>Jpn J Pharmacol</addtitle><date>1989-01-01</date><risdate>1989</risdate><volume>51</volume><issue>2</issue><spage>211</spage><epage>218</epage><pages>211-218</pages><issn>0021-5198</issn><eissn>1347-3506</eissn><coden>JJPAAZ</coden><abstract>The effects of bifemelane hydrochloride (BF) upon various cholinergic markers, muscarinic receptors, acetylcholinesterase (AChE) and choline acetyl-transferase (CAT), in the aged rat brain were examined. Marked reduction of the density of muscarinic receptors (Bmax) as well as AChE and CAT activity concomitant with aging was observed. Administration of BF in daily doses of 10 mg/kg for 4 weeks to aged rats significantly decreased the apparent dissociation constant (K4) for QNB in muscarinic receptors in the forebrain, but did not affect the value of Bmax. CAT activity also increased significantly compared with that of control aged rats, but administration of BF did not alter AChE activity. These results indicate that long-term treatment with BF enhances the affinity of muscarinic receptors for QNB as well as CAT activity and that BF may have therapeutic application in the treatment of CNS cholinergic dysfunctions.</abstract><cop>Kyoto</cop><pub>The Japanese Pharmacological Society</pub><pmid>2593378</pmid><doi>10.1016/S0021-5198(19)40118-2</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0021-5198 |
| ispartof | Japanese Journal of Pharmacology, 1989-01, Vol.51 (2), p.211-218 |
| issn | 0021-5198 1347-3506 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_79364962 |
| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Acetylcholinesterase - metabolism Aging - physiology Animals Antidepressive Agents - pharmacology Benzhydryl Compounds - pharmacology Biological and medical sciences Brain - drug effects Brain - enzymology Cerebral Cortex - drug effects Cerebral Cortex - enzymology Choline O-Acetyltransferase - antagonists & inhibitors Cholinesterase Inhibitors - pharmacology Kinetics Male Medical sciences Nerve Tissue Proteins - metabolism Neuropharmacology Parasympathetic Nervous System - drug effects Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rats Rats, Inbred Strains Receptors, Muscarinic - drug effects |
| title | Effects of Bifemelane Hydrochloride on Various Cholinergic Markers in Cortical and Subcortical Regions of Aged Rats |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-23T04%3A16%3A07IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Effects%20of%20Bifemelane%20Hydrochloride%20on%20Various%20Cholinergic%20Markers%20in%20Cortical%20and%20Subcortical%20Regions%20of%20Aged%20Rats&rft.jtitle=Japanese%20Journal%20of%20Pharmacology&rft.au=EGASHIRA,%20Tom&rft.aucorp=Medical%20College%20of%20Oita&rft.date=1989-01-01&rft.volume=51&rft.issue=2&rft.spage=211&rft.epage=218&rft.pages=211-218&rft.issn=0021-5198&rft.eissn=1347-3506&rft.coden=JJPAAZ&rft_id=info:doi/10.1016/S0021-5198(19)40118-2&rft_dat=%3Cproquest_cross%3E15484478%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=15484478&rft_id=info:pmid/2593378&rft_els_id=S0021519819401182&rfr_iscdi=true |