EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN
The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [3H] nicotine and [3H] cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at...
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| Veröffentlicht in: | Journal of Pharmacobio-Dynamics 1986, Vol.9(7), pp.620-625 |
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| container_title | Journal of Pharmacobio-Dynamics |
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| creator | YAMADA, SHIZUO KAGAWA, YOSHIYUKI USHIJIMA, HIDETO TAKAYANAGI, NORIYASU HAYASHI, EIICHI |
| description | The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [3H] nicotine and [3H] cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1μM-30 mM completed dosedependently with [3H] nicotine and [3H] CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [3H] nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [3H] nicotine binding sites in the rat cerebral cortex than of [3H] CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [3H] CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [3H] nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [3H] nicotine binding between species such as rat, mouse, guinea-pig and rabbit. Thus, the present study demonstrates a high affinity of piperidine for nicotinic cholinoceptors in the mammalian brain. |
| doi_str_mv | 10.1248/bpb1978.9.620 |
| format | Article |
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Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1μM-30 mM completed dosedependently with [3H] nicotine and [3H] CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [3H] nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [3H] nicotine binding sites in the rat cerebral cortex than of [3H] CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [3H] CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [3H] nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [3H] nicotine binding between species such as rat, mouse, guinea-pig and rabbit. Thus, the present study demonstrates a high affinity of piperidine for nicotinic cholinoceptors in the mammalian brain.</description><identifier>ISSN: 0386-846X</identifier><identifier>EISSN: 1881-1353</identifier><identifier>DOI: 10.1248/bpb1978.9.620</identifier><identifier>PMID: 3772718</identifier><identifier>CODEN: JOPHDQ</identifier><language>eng</language><publisher>Tokyo: The Pharmaceutical Society of Japan</publisher><subject>[3H] nicotine ; Amines - pharmacology ; Animals ; Animals, Newborn ; Binding, Competitive - drug effects ; Biological and medical sciences ; Brain - metabolism ; Guinea Pigs ; In Vitro Techniques ; Medical sciences ; Mice ; Nicotine - metabolism ; Parasympathomimetics - pharmacology ; Pharmacology. Drug treatments ; Piperidines - pharmacology ; Rabbits ; Rats ; Rats, Inbred Strains ; Receptors, Muscarinic - drug effects ; Receptors, Nicotinic - drug effects ; Species Specificity</subject><ispartof>Journal of Pharmacobio-Dynamics, 1986, Vol.9(7), pp.620-625</ispartof><rights>The Pharmaceutical Society of Japan</rights><rights>1987 INIST-CNRS</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c571t-665159841574d7a60bbd39b114dc577799185d409ad9535c935884e828b8cf7a3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,1877,4010,27900,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8157028$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3772718$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>YAMADA, SHIZUO</creatorcontrib><creatorcontrib>KAGAWA, YOSHIYUKI</creatorcontrib><creatorcontrib>USHIJIMA, HIDETO</creatorcontrib><creatorcontrib>TAKAYANAGI, NORIYASU</creatorcontrib><creatorcontrib>HAYASHI, EIICHI</creatorcontrib><title>EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN</title><title>Journal of Pharmacobio-Dynamics</title><addtitle>Journal of Pharmacobio-Dynamics</addtitle><description>The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [3H] nicotine and [3H] cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1μM-30 mM completed dosedependently with [3H] nicotine and [3H] CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [3H] nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [3H] nicotine binding sites in the rat cerebral cortex than of [3H] CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [3H] CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [3H] nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [3H] nicotine binding between species such as rat, mouse, guinea-pig and rabbit. Thus, the present study demonstrates a high affinity of piperidine for nicotinic cholinoceptors in the mammalian brain.</description><subject>[3H] nicotine</subject><subject>Amines - pharmacology</subject><subject>Animals</subject><subject>Animals, Newborn</subject><subject>Binding, Competitive - drug effects</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Guinea Pigs</subject><subject>In Vitro Techniques</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Nicotine - metabolism</subject><subject>Parasympathomimetics - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - pharmacology</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Receptors, Muscarinic - drug effects</subject><subject>Receptors, Nicotinic - drug effects</subject><subject>Species Specificity</subject><issn>0386-846X</issn><issn>1881-1353</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpNkM2P0zAQxS0EWsrCkSOSD4hbih3HsX30pmnXUuOs2qwEJ8txXOgq_SBuD_DX49Ko4uCxPO83b-QHwEeMpjjN-Nf22GLB-FRM8xS9AhPMOU4woeQ1mCDC84Rn-be34F0ILwhlglN8B-4IYynDfAL-lPN5WTSwnsMn9VSu1EzpEko9g6tyKZtyBuVSFd-LWKCsoraGtYZaFXWj9KUXyep5XcjV9bmotVo38EHpaLSAa9XECaVh81jCSlZVdJMaPqyk0u_Bm43tg_8w3vfgeV42xWOyrBeqkMvEUYZPSZ5TTAXPMGVZx2yO2rYjosU46yLAmBCY0y5DwnaCEuoEoZxnnqe85W7DLLkHX66-x-Hw6-zDyey2wfm-t3t_OAfDGE5RRmkEkyvohkMIg9-Y47Dd2eG3wchcsjZj1kaYmHXkP43G53bnuxs9hhv1z6Nug7P9ZrB7tw03jMcfofSCySv2Ek72h7_pdjhtXe__W8r-nbj6prmfdjB-T_4CFP2SHg</recordid><startdate>1986</startdate><enddate>1986</enddate><creator>YAMADA, SHIZUO</creator><creator>KAGAWA, YOSHIYUKI</creator><creator>USHIJIMA, HIDETO</creator><creator>TAKAYANAGI, NORIYASU</creator><creator>HAYASHI, EIICHI</creator><general>The Pharmaceutical Society of Japan</general><general>Pharmaceutical Society of Japan</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>1986</creationdate><title>EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN</title><author>YAMADA, SHIZUO ; KAGAWA, YOSHIYUKI ; USHIJIMA, HIDETO ; TAKAYANAGI, NORIYASU ; HAYASHI, EIICHI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c571t-665159841574d7a60bbd39b114dc577799185d409ad9535c935884e828b8cf7a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>[3H] nicotine</topic><topic>Amines - pharmacology</topic><topic>Animals</topic><topic>Animals, Newborn</topic><topic>Binding, Competitive - drug effects</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Guinea Pigs</topic><topic>In Vitro Techniques</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Nicotine - metabolism</topic><topic>Parasympathomimetics - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperidines - pharmacology</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Receptors, Muscarinic - drug effects</topic><topic>Receptors, Nicotinic - drug effects</topic><topic>Species Specificity</topic><toplevel>online_resources</toplevel><creatorcontrib>YAMADA, SHIZUO</creatorcontrib><creatorcontrib>KAGAWA, YOSHIYUKI</creatorcontrib><creatorcontrib>USHIJIMA, HIDETO</creatorcontrib><creatorcontrib>TAKAYANAGI, NORIYASU</creatorcontrib><creatorcontrib>HAYASHI, EIICHI</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>Journal of Pharmacobio-Dynamics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>YAMADA, SHIZUO</au><au>KAGAWA, YOSHIYUKI</au><au>USHIJIMA, HIDETO</au><au>TAKAYANAGI, NORIYASU</au><au>HAYASHI, EIICHI</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN</atitle><jtitle>Journal of Pharmacobio-Dynamics</jtitle><addtitle>Journal of Pharmacobio-Dynamics</addtitle><date>1986</date><risdate>1986</risdate><volume>9</volume><issue>7</issue><spage>620</spage><epage>625</epage><pages>620-625</pages><issn>0386-846X</issn><eissn>1881-1353</eissn><coden>JOPHDQ</coden><abstract>The effect of piperidine and related alicyclic amines on central nicotinic and muscarinic cholinoceptors was investigated by measuring specific binding of [3H] nicotine and [3H] cismethyldioxolane (CD) in rat cerebral cortical membranes. Piperidine, pyrrolidine, 4-hydroxypiperidine and piperazine at concentrations of 1μM-30 mM completed dosedependently with [3H] nicotine and [3H] CD for the binding sites. Among these compounds, piperidine was the most potent competitor of brain [3H] nicotine binding sites. Piperidine and pyrrolidine showed a greater affinity for [3H] nicotine binding sites in the rat cerebral cortex than of [3H] CD binding sites. In contrast, 4-hydroxypiperidine and piperazine displayed approximately 10 times greater affinity for [3H] CD binding sites. Pipecolic acid had little effect on these cholinoceptor agonist binding sites. The inhibitory effect of brain [3H] nicotine binding by piperidine did not differ between brain regions or during development. In addition, there was little difference in the piperidine-induced inhibition of brain [3H] nicotine binding between species such as rat, mouse, guinea-pig and rabbit. 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| ispartof | Journal of Pharmacobio-Dynamics, 1986, Vol.9(7), pp.620-625 |
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| source | J-STAGE Free; MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | [3H] nicotine Amines - pharmacology Animals Animals, Newborn Binding, Competitive - drug effects Biological and medical sciences Brain - metabolism Guinea Pigs In Vitro Techniques Medical sciences Mice Nicotine - metabolism Parasympathomimetics - pharmacology Pharmacology. Drug treatments Piperidines - pharmacology Rabbits Rats Rats, Inbred Strains Receptors, Muscarinic - drug effects Receptors, Nicotinic - drug effects Species Specificity |
| title | EFFECT OF PIPERIDINE AND RELATED ALICYCLIC AMINES ON NICOTINIC AND MUSCARINIC AGONIST BINDING SITES IN THE MAMMALIAN BRAIN |
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