Effects of (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), sigma (σ) ligands, on micturition in anaesthetized rats
The effects of two sigma (σ) binding site ligands, (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), on bladder functions were examined in rats. Cystometry using urethane‐anaesthetized rats showed that (+)‐pentazocine (1–5 mg kg−1, i.v.) and DTG (1–5 mg kg−1, i.v.) prolonged micturition intervals,...
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| creator | Shimizu, Isao Kawashima, Katsuyoshi Ishii, Daisuke Oka, Makoto |
| description | The effects of two sigma (σ) binding site ligands, (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), on bladder functions were examined in rats.
Cystometry using urethane‐anaesthetized rats showed that (+)‐pentazocine (1–5 mg kg−1, i.v.) and DTG (1–5 mg kg−1, i.v.) prolonged micturition intervals, indicating increased bladder capacity and raised the threshold pressure.
The effects of (+)‐pentazocine (2 mg kg−1, i.v.) on micturition were not influenced by naloxone (0.5 mg kg−1, i.v.), which antagonized similar effects of morphine (2 mg kg−1, i.v.).
When administered intracerebroventricularly (i.c.v.), DTG (1 μg) and (+)‐pentazocine (30 μg) prolonged micturition intervals with increased threshold pressure on the cystometrogram.
In isolated bladder detrusor strips of rats, (+)‐pentazocine (3 μM) and DTG (1 μM) did not affect contractile responses to electrical field stimulation. A higher concentration of DTG (3 μM) slightly suppressed the response induced by 30 Hz stimulation.
The effects of (+)‐pentazocine and DTG on micturition were abolished by pre‐treatment with pertussis toxin (PTX, 1 μg, i.c.v.).
These results indicate that typical σ ligands, such as (+)‐pentazocine and DTG, increase bladder capacity in anaesthetized rats. Moreover, the mechanism by which σ ligands change the urinary storage properties in rats may involve pathways in which the function of Gi/o proteins is necessary.
British Journal of Pharmacology (2000) 131, 610–616; doi:10.1038/sj.bjp.0703593 |
| doi_str_mv | 10.1038/sj.bjp.0703593 |
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Cystometry using urethane‐anaesthetized rats showed that (+)‐pentazocine (1–5 mg kg−1, i.v.) and DTG (1–5 mg kg−1, i.v.) prolonged micturition intervals, indicating increased bladder capacity and raised the threshold pressure.
The effects of (+)‐pentazocine (2 mg kg−1, i.v.) on micturition were not influenced by naloxone (0.5 mg kg−1, i.v.), which antagonized similar effects of morphine (2 mg kg−1, i.v.).
When administered intracerebroventricularly (i.c.v.), DTG (1 μg) and (+)‐pentazocine (30 μg) prolonged micturition intervals with increased threshold pressure on the cystometrogram.
In isolated bladder detrusor strips of rats, (+)‐pentazocine (3 μM) and DTG (1 μM) did not affect contractile responses to electrical field stimulation. A higher concentration of DTG (3 μM) slightly suppressed the response induced by 30 Hz stimulation.
The effects of (+)‐pentazocine and DTG on micturition were abolished by pre‐treatment with pertussis toxin (PTX, 1 μg, i.c.v.).
These results indicate that typical σ ligands, such as (+)‐pentazocine and DTG, increase bladder capacity in anaesthetized rats. Moreover, the mechanism by which σ ligands change the urinary storage properties in rats may involve pathways in which the function of Gi/o proteins is necessary.
British Journal of Pharmacology (2000) 131, 610–616; doi:10.1038/sj.bjp.0703593</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1038/sj.bjp.0703593</identifier><identifier>PMID: 11015314</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>(+)‐pentazocine ; Anesthesia ; Animals ; Anticonvulsants - pharmacology ; Anticonvulsants - therapeutic use ; Biological and medical sciences ; cystometry ; DTG ; Electric Stimulation ; Gi/o proteins ; Guanidines - pharmacology ; Ligands ; Male ; Medical sciences ; micturition ; Muscle Contraction - drug effects ; Narcotic Antagonists - pharmacology ; Narcotic Antagonists - therapeutic use ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pentazocine - pharmacology ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pertussis Toxin ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; Receptors, sigma - metabolism ; Syncope - chemically induced ; Syncope - drug therapy ; Urinary Bladder - drug effects ; Urinary Bladder - metabolism ; Virulence Factors, Bordetella - pharmacology ; σ binding sites</subject><ispartof>British journal of pharmacology, 2000-10, Vol.131 (3), p.610-616</ispartof><rights>2000 British Pharmacological Society</rights><rights>2000 INIST-CNRS</rights><rights>Copyright Nature Publishing Group Oct 2000</rights><rights>Copyright 2000, Nature Publishing Group 2000 Nature Publishing Group</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4867-e8d1242330a15c0ab4427588d88685648359d22120d25a4803e0a3212f3a6d8d3</citedby><cites>FETCH-LOGICAL-c4867-e8d1242330a15c0ab4427588d88685648359d22120d25a4803e0a3212f3a6d8d3</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/PMC1572351/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1572351/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,1411,1427,27901,27902,45550,45551,46384,46808,53766,53768</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1502478$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11015314$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shimizu, Isao</creatorcontrib><creatorcontrib>Kawashima, Katsuyoshi</creatorcontrib><creatorcontrib>Ishii, Daisuke</creatorcontrib><creatorcontrib>Oka, Makoto</creatorcontrib><title>Effects of (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), sigma (σ) ligands, on micturition in anaesthetized rats</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>The effects of two sigma (σ) binding site ligands, (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), on bladder functions were examined in rats.
Cystometry using urethane‐anaesthetized rats showed that (+)‐pentazocine (1–5 mg kg−1, i.v.) and DTG (1–5 mg kg−1, i.v.) prolonged micturition intervals, indicating increased bladder capacity and raised the threshold pressure.
The effects of (+)‐pentazocine (2 mg kg−1, i.v.) on micturition were not influenced by naloxone (0.5 mg kg−1, i.v.), which antagonized similar effects of morphine (2 mg kg−1, i.v.).
When administered intracerebroventricularly (i.c.v.), DTG (1 μg) and (+)‐pentazocine (30 μg) prolonged micturition intervals with increased threshold pressure on the cystometrogram.
In isolated bladder detrusor strips of rats, (+)‐pentazocine (3 μM) and DTG (1 μM) did not affect contractile responses to electrical field stimulation. A higher concentration of DTG (3 μM) slightly suppressed the response induced by 30 Hz stimulation.
The effects of (+)‐pentazocine and DTG on micturition were abolished by pre‐treatment with pertussis toxin (PTX, 1 μg, i.c.v.).
These results indicate that typical σ ligands, such as (+)‐pentazocine and DTG, increase bladder capacity in anaesthetized rats. Moreover, the mechanism by which σ ligands change the urinary storage properties in rats may involve pathways in which the function of Gi/o proteins is necessary.
British Journal of Pharmacology (2000) 131, 610–616; doi:10.1038/sj.bjp.0703593</description><subject>(+)‐pentazocine</subject><subject>Anesthesia</subject><subject>Animals</subject><subject>Anticonvulsants - pharmacology</subject><subject>Anticonvulsants - therapeutic use</subject><subject>Biological and medical sciences</subject><subject>cystometry</subject><subject>DTG</subject><subject>Electric Stimulation</subject><subject>Gi/o proteins</subject><subject>Guanidines - pharmacology</subject><subject>Ligands</subject><subject>Male</subject><subject>Medical sciences</subject><subject>micturition</subject><subject>Muscle Contraction - drug effects</subject><subject>Narcotic Antagonists - pharmacology</subject><subject>Narcotic Antagonists - therapeutic use</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pentazocine - pharmacology</subject><subject>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</subject><subject>Pertussis Toxin</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, sigma - metabolism</subject><subject>Syncope - chemically induced</subject><subject>Syncope - drug therapy</subject><subject>Urinary Bladder - drug effects</subject><subject>Urinary Bladder - metabolism</subject><subject>Virulence Factors, Bordetella - pharmacology</subject><subject>σ binding sites</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNqFkc9uEzEQxi0EoiFw5YgsxCER2eCx12vnglRKaZEqwaGcLcf2pl5t1sHepUoPCIkX4M14B54EV1lROHHw3_nNNzP6EHoKZAmEyVepWa6b3ZIIwviK3UMTKEVVcCbhPpoQQkQBIOURepRSQ0gOCv4QHQEQ4AzKCfp6WtfO9AmHGs9ezn99-7FzXa9vgvGdw7qzGBYs_1qft5BXH9p9uxl05-0tMXt7eTZf4OQ3W41nP7_Pces3OS0tcOjw1pt-iL73-e67LKdd6q9c72-cxVH36TF6UOs2uSfjOUWf3p1enpwXFx_O3p8cXxSmlJUonLRAS8oY0cAN0euypIJLaaWsJK9KmYe3lAIllnJdSsIc0Sy_a6YrKy2botcH3d2w3jpr8oxRt2oX_VbHvQraq38jnb9Sm_BFAReUccgCz0eBGD4PeQrVhCF2uWdFQcCK8Fx0ipYHyMSQUnT1nwJA1K1dKjUq26VGu3LCs7_busNHfzLwYgR0Mrqto-6MT3ccJ7QUMmPsgF371u3_U1W9-XgO1Uqw37XKsTw</recordid><startdate>200010</startdate><enddate>200010</enddate><creator>Shimizu, Isao</creator><creator>Kawashima, Katsuyoshi</creator><creator>Ishii, Daisuke</creator><creator>Oka, Makoto</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>3V.</scope><scope>7QP</scope><scope>7RV</scope><scope>7TK</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7P</scope><scope>NAPCQ</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>5PM</scope></search><sort><creationdate>200010</creationdate><title>Effects of (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), sigma (σ) ligands, on micturition in anaesthetized rats</title><author>Shimizu, Isao ; Kawashima, Katsuyoshi ; Ishii, Daisuke ; Oka, Makoto</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4867-e8d1242330a15c0ab4427588d88685648359d22120d25a4803e0a3212f3a6d8d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>(+)‐pentazocine</topic><topic>Anesthesia</topic><topic>Animals</topic><topic>Anticonvulsants - pharmacology</topic><topic>Anticonvulsants - therapeutic use</topic><topic>Biological and medical sciences</topic><topic>cystometry</topic><topic>DTG</topic><topic>Electric Stimulation</topic><topic>Gi/o proteins</topic><topic>Guanidines - pharmacology</topic><topic>Ligands</topic><topic>Male</topic><topic>Medical sciences</topic><topic>micturition</topic><topic>Muscle Contraction - drug effects</topic><topic>Narcotic Antagonists - pharmacology</topic><topic>Narcotic Antagonists - therapeutic use</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pentazocine - pharmacology</topic><topic>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</topic><topic>Pertussis Toxin</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, sigma - metabolism</topic><topic>Syncope - chemically induced</topic><topic>Syncope - drug therapy</topic><topic>Urinary Bladder - drug effects</topic><topic>Urinary Bladder - metabolism</topic><topic>Virulence Factors, Bordetella - pharmacology</topic><topic>σ binding sites</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shimizu, Isao</creatorcontrib><creatorcontrib>Kawashima, Katsuyoshi</creatorcontrib><creatorcontrib>Ishii, Daisuke</creatorcontrib><creatorcontrib>Oka, Makoto</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>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>Neurosciences Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Biological Science Database</collection><collection>Nursing & Allied Health Premium</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</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>Shimizu, Isao</au><au>Kawashima, Katsuyoshi</au><au>Ishii, Daisuke</au><au>Oka, Makoto</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), sigma (σ) ligands, on micturition in anaesthetized rats</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>2000-10</date><risdate>2000</risdate><volume>131</volume><issue>3</issue><spage>610</spage><epage>616</epage><pages>610-616</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>The effects of two sigma (σ) binding site ligands, (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), on bladder functions were examined in rats.
Cystometry using urethane‐anaesthetized rats showed that (+)‐pentazocine (1–5 mg kg−1, i.v.) and DTG (1–5 mg kg−1, i.v.) prolonged micturition intervals, indicating increased bladder capacity and raised the threshold pressure.
The effects of (+)‐pentazocine (2 mg kg−1, i.v.) on micturition were not influenced by naloxone (0.5 mg kg−1, i.v.), which antagonized similar effects of morphine (2 mg kg−1, i.v.).
When administered intracerebroventricularly (i.c.v.), DTG (1 μg) and (+)‐pentazocine (30 μg) prolonged micturition intervals with increased threshold pressure on the cystometrogram.
In isolated bladder detrusor strips of rats, (+)‐pentazocine (3 μM) and DTG (1 μM) did not affect contractile responses to electrical field stimulation. A higher concentration of DTG (3 μM) slightly suppressed the response induced by 30 Hz stimulation.
The effects of (+)‐pentazocine and DTG on micturition were abolished by pre‐treatment with pertussis toxin (PTX, 1 μg, i.c.v.).
These results indicate that typical σ ligands, such as (+)‐pentazocine and DTG, increase bladder capacity in anaesthetized rats. Moreover, the mechanism by which σ ligands change the urinary storage properties in rats may involve pathways in which the function of Gi/o proteins is necessary.
British Journal of Pharmacology (2000) 131, 610–616; doi:10.1038/sj.bjp.0703593</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>11015314</pmid><doi>10.1038/sj.bjp.0703593</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | (+)‐pentazocine Anesthesia Animals Anticonvulsants - pharmacology Anticonvulsants - therapeutic use Biological and medical sciences cystometry DTG Electric Stimulation Gi/o proteins Guanidines - pharmacology Ligands Male Medical sciences micturition Muscle Contraction - drug effects Narcotic Antagonists - pharmacology Narcotic Antagonists - therapeutic use Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pentazocine - pharmacology Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pertussis Toxin Pharmacology. Drug treatments Rats Rats, Wistar Receptors, sigma - metabolism Syncope - chemically induced Syncope - drug therapy Urinary Bladder - drug effects Urinary Bladder - metabolism Virulence Factors, Bordetella - pharmacology σ binding sites |
| title | Effects of (+)‐pentazocine and 1,3‐di‐o‐tolylguanidine (DTG), sigma (σ) ligands, on micturition in anaesthetized rats |
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