Characterization and tissue location of the neural adenosine receptor in the rat ileum
The aim of the present investigation was to characterize and determine the tissue location of the adenosine receptors present in the rat ileum using a method that detects drug action on the cholinergic nerves innervating the longitudinal and circular muscles. The non‐selective adenosine agonist, NEC...
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| Veröffentlicht in: | British journal of pharmacology 1999-03, Vol.126 (5), p.1269-1275 |
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| description | The aim of the present investigation was to characterize and determine the tissue location of the adenosine receptors present in the rat ileum using a method that detects drug action on the cholinergic nerves innervating the longitudinal and circular muscles.
The non‐selective adenosine agonist, NECA (10 and 100 nM) caused significant concentration‐related reductions in the circular muscle responses to transmural stimulation over the frequency range of 2.5–40 Hz, but did not affect the responses of the longitudinal muscle, nor did it reduce the muscle responses of the guinea‐pig ileum.
The affinity order of antagonists at inhibiting the effect of NECA on the circular muscle was: CPDPX>8‐PT>DMPX with apparent pA2 values of 9.31, 7.54 and 5.63 respectively. CPDPX (10–100 nM) caused parallel displacements of the concentration‐effect curves to CPA with a pKb value of 9.15 and Schild slope of 1.03.
The agonists previously tested in the rat jejunum peristaltic reflex preparation were also shown to inhibit responses of the rat ileum in the following decreasing order of potency: CPA>NECA>2‐CADO>R‐PIA>S‐PIA>>PAA. In addition, CHA and CCPA were also potent agonists. NECA (100 nM) and CPA (32 nM) did not inhibit carbachol (1 μM)‐induced tone of tissues pre‐treated with TTX (1 μM).
In conclusion, the rat ileum contains inhibitory A1 adenosine receptors situated on cholinergic nerve endings innervating the circular muscle.
British Journal of Pharmacology (1999) 126, 1269–1275; doi:10.1038/sj.bjp.0702411 |
| doi_str_mv | 10.1038/sj.bjp.0702411 |
| format | Article |
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The non‐selective adenosine agonist, NECA (10 and 100 nM) caused significant concentration‐related reductions in the circular muscle responses to transmural stimulation over the frequency range of 2.5–40 Hz, but did not affect the responses of the longitudinal muscle, nor did it reduce the muscle responses of the guinea‐pig ileum.
The affinity order of antagonists at inhibiting the effect of NECA on the circular muscle was: CPDPX>8‐PT>DMPX with apparent pA2 values of 9.31, 7.54 and 5.63 respectively. CPDPX (10–100 nM) caused parallel displacements of the concentration‐effect curves to CPA with a pKb value of 9.15 and Schild slope of 1.03.
The agonists previously tested in the rat jejunum peristaltic reflex preparation were also shown to inhibit responses of the rat ileum in the following decreasing order of potency: CPA>NECA>2‐CADO>R‐PIA>S‐PIA>>PAA. In addition, CHA and CCPA were also potent agonists. NECA (100 nM) and CPA (32 nM) did not inhibit carbachol (1 μM)‐induced tone of tissues pre‐treated with TTX (1 μM).
In conclusion, the rat ileum contains inhibitory A1 adenosine receptors situated on cholinergic nerve endings innervating the circular muscle.
British Journal of Pharmacology (1999) 126, 1269–1275; doi:10.1038/sj.bjp.0702411</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1038/sj.bjp.0702411</identifier><identifier>PMID: 10205018</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>8‐PT ; Adenosine - analogs & derivatives ; Adenosine - pharmacology ; adenosine agonists ; adenosine antagonists ; Adenosine receptors ; Adenosine-5'-(N-ethylcarboxamide) - pharmacology ; Analysis of Variance ; Animals ; Biological and medical sciences ; cholinergic nerves ; circular muscle ; CPA ; CPDPX ; Female ; Fundamental and applied biological sciences. Psychology ; Ileum - drug effects ; Ileum - metabolism ; Intestine. Mesentery ; Male ; NECA ; Neurons - drug effects ; Neurons - metabolism ; rat ileum ; Rats ; Rats, Wistar ; Receptors, Purinergic P1 - metabolism ; Vertebrates: digestive system ; Xanthines - pharmacology</subject><ispartof>British journal of pharmacology, 1999-03, Vol.126 (5), p.1269-1275</ispartof><rights>1999 Nature Publishing Group</rights><rights>1999 INIST-CNRS</rights><rights>Copyright 1999, Nature Publishing Group 1999 Nature Publishing Group</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4590-5e89d73e68436b3a24421c391790c2b28a3fe2c647504773624ef38bf805ffe3</citedby><cites>FETCH-LOGICAL-c4590-5e89d73e68436b3a24421c391790c2b28a3fe2c647504773624ef38bf805ffe3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1565885/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1565885/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,724,777,781,882,1412,1428,27905,27906,45555,45556,46390,46814,53772,53774</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1722067$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10205018$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Coupar, Ian M</creatorcontrib><title>Characterization and tissue location of the neural adenosine receptor in the rat ileum</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>The aim of the present investigation was to characterize and determine the tissue location of the adenosine receptors present in the rat ileum using a method that detects drug action on the cholinergic nerves innervating the longitudinal and circular muscles.
The non‐selective adenosine agonist, NECA (10 and 100 nM) caused significant concentration‐related reductions in the circular muscle responses to transmural stimulation over the frequency range of 2.5–40 Hz, but did not affect the responses of the longitudinal muscle, nor did it reduce the muscle responses of the guinea‐pig ileum.
The affinity order of antagonists at inhibiting the effect of NECA on the circular muscle was: CPDPX>8‐PT>DMPX with apparent pA2 values of 9.31, 7.54 and 5.63 respectively. CPDPX (10–100 nM) caused parallel displacements of the concentration‐effect curves to CPA with a pKb value of 9.15 and Schild slope of 1.03.
The agonists previously tested in the rat jejunum peristaltic reflex preparation were also shown to inhibit responses of the rat ileum in the following decreasing order of potency: CPA>NECA>2‐CADO>R‐PIA>S‐PIA>>PAA. In addition, CHA and CCPA were also potent agonists. NECA (100 nM) and CPA (32 nM) did not inhibit carbachol (1 μM)‐induced tone of tissues pre‐treated with TTX (1 μM).
In conclusion, the rat ileum contains inhibitory A1 adenosine receptors situated on cholinergic nerve endings innervating the circular muscle.
British Journal of Pharmacology (1999) 126, 1269–1275; doi:10.1038/sj.bjp.0702411</description><subject>8‐PT</subject><subject>Adenosine - analogs & derivatives</subject><subject>Adenosine - pharmacology</subject><subject>adenosine agonists</subject><subject>adenosine antagonists</subject><subject>Adenosine receptors</subject><subject>Adenosine-5'-(N-ethylcarboxamide) - pharmacology</subject><subject>Analysis of Variance</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>cholinergic nerves</subject><subject>circular muscle</subject><subject>CPA</subject><subject>CPDPX</subject><subject>Female</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Ileum - drug effects</subject><subject>Ileum - metabolism</subject><subject>Intestine. Mesentery</subject><subject>Male</subject><subject>NECA</subject><subject>Neurons - drug effects</subject><subject>Neurons - metabolism</subject><subject>rat ileum</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Purinergic P1 - metabolism</subject><subject>Vertebrates: digestive system</subject><subject>Xanthines - pharmacology</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkb1vFDEQxS0EIkegpUQuEN1exl-73gYJTkCQIkER0Vpe35jzac8-7F1Q-Otj2BMkVaqRZn7z5mkeIS8ZrBkIfVH262F_XEMHXDL2iKyY7NpGCc0ekxUAdA1jWp-RZ6XsAeqwU0_JGQMOCphekW-bnc3WTZjDbzuFFKmNWzqFUmakY3JLL3k67ZBGnLMdqd1iTCVEpBkdHqeUaYh_gWwnGkacD8_JE2_Hgi9O9Zxcf_xwvblsrr58-rx5d9U4qXpoFOp-2wlstRTtICyXkjMnetb14PjAtRUeuWtlp6BaFy2X6IUevAblPYpz8naRPc7DAbcO41QNmmMOB5tvTLLB3J_EsDPf00_DVKu0VlXgzUkgpx8zlskcQnE4jjZimotp-7aXWogKrhfQ5VRKRv_vCAPzJwlT9qYmYU5J1IVXd63dwZfXV-D1CbDF2dFnG10o_7mOc2i7iokF-1Ufe_PAVfP-6yUDCeIWo-WjCg</recordid><startdate>199903</startdate><enddate>199903</enddate><creator>Coupar, Ian M</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</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><scope>5PM</scope></search><sort><creationdate>199903</creationdate><title>Characterization and tissue location of the neural adenosine receptor in the rat ileum</title><author>Coupar, Ian M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4590-5e89d73e68436b3a24421c391790c2b28a3fe2c647504773624ef38bf805ffe3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>8‐PT</topic><topic>Adenosine - analogs & derivatives</topic><topic>Adenosine - pharmacology</topic><topic>adenosine agonists</topic><topic>adenosine antagonists</topic><topic>Adenosine receptors</topic><topic>Adenosine-5'-(N-ethylcarboxamide) - pharmacology</topic><topic>Analysis of Variance</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>cholinergic nerves</topic><topic>circular muscle</topic><topic>CPA</topic><topic>CPDPX</topic><topic>Female</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Ileum - drug effects</topic><topic>Ileum - metabolism</topic><topic>Intestine. Mesentery</topic><topic>Male</topic><topic>NECA</topic><topic>Neurons - drug effects</topic><topic>Neurons - metabolism</topic><topic>rat ileum</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Purinergic P1 - metabolism</topic><topic>Vertebrates: digestive system</topic><topic>Xanthines - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Coupar, Ian M</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><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Coupar, Ian M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characterization and tissue location of the neural adenosine receptor in the rat ileum</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1999-03</date><risdate>1999</risdate><volume>126</volume><issue>5</issue><spage>1269</spage><epage>1275</epage><pages>1269-1275</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>The aim of the present investigation was to characterize and determine the tissue location of the adenosine receptors present in the rat ileum using a method that detects drug action on the cholinergic nerves innervating the longitudinal and circular muscles.
The non‐selective adenosine agonist, NECA (10 and 100 nM) caused significant concentration‐related reductions in the circular muscle responses to transmural stimulation over the frequency range of 2.5–40 Hz, but did not affect the responses of the longitudinal muscle, nor did it reduce the muscle responses of the guinea‐pig ileum.
The affinity order of antagonists at inhibiting the effect of NECA on the circular muscle was: CPDPX>8‐PT>DMPX with apparent pA2 values of 9.31, 7.54 and 5.63 respectively. CPDPX (10–100 nM) caused parallel displacements of the concentration‐effect curves to CPA with a pKb value of 9.15 and Schild slope of 1.03.
The agonists previously tested in the rat jejunum peristaltic reflex preparation were also shown to inhibit responses of the rat ileum in the following decreasing order of potency: CPA>NECA>2‐CADO>R‐PIA>S‐PIA>>PAA. In addition, CHA and CCPA were also potent agonists. NECA (100 nM) and CPA (32 nM) did not inhibit carbachol (1 μM)‐induced tone of tissues pre‐treated with TTX (1 μM).
In conclusion, the rat ileum contains inhibitory A1 adenosine receptors situated on cholinergic nerve endings innervating the circular muscle.
British Journal of Pharmacology (1999) 126, 1269–1275; doi:10.1038/sj.bjp.0702411</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>10205018</pmid><doi>10.1038/sj.bjp.0702411</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Wiley Online Library Journals Frontfile Complete; Wiley Free Content; EZB-FREE-00999 freely available EZB journals; PubMed Central; Alma/SFX Local Collection |
| subjects | 8‐PT Adenosine - analogs & derivatives Adenosine - pharmacology adenosine agonists adenosine antagonists Adenosine receptors Adenosine-5'-(N-ethylcarboxamide) - pharmacology Analysis of Variance Animals Biological and medical sciences cholinergic nerves circular muscle CPA CPDPX Female Fundamental and applied biological sciences. Psychology Ileum - drug effects Ileum - metabolism Intestine. Mesentery Male NECA Neurons - drug effects Neurons - metabolism rat ileum Rats Rats, Wistar Receptors, Purinergic P1 - metabolism Vertebrates: digestive system Xanthines - pharmacology |
| title | Characterization and tissue location of the neural adenosine receptor in the rat ileum |
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