Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs
Droperidol (D) is effective in the treatment of patients with status asthmaticus. It has been reported that D inhibits the bronchoconstriction induced by serotonin (5-HT) but not that by histamine (H) or acetylcholine. However, haloperidol, another butyrophenone, is known to interact with and inhibi...
Gespeichert in:
| Veröffentlicht in: | Canadian journal of anesthesia 1996-02, Vol.43 (2), p.172-178 |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 178 |
|---|---|
| container_issue | 2 |
| container_start_page | 172 |
| container_title | Canadian journal of anesthesia |
| container_volume | 43 |
| creator | SATO, T HIROTA, K MATSUKI, A ZSIGMOND, E. K RABITO, S. F |
| description | Droperidol (D) is effective in the treatment of patients with status asthmaticus. It has been reported that D inhibits the bronchoconstriction induced by serotonin (5-HT) but not that by histamine (H) or acetylcholine. However, haloperidol, another butyrophenone, is known to interact with and inhibit calmodulin, an intracellular Ca(++)-binding protein which is important in the contraction of smooth muscles. The present study was designed to investigate the effects of D on tracheal contractions induced by 5-HT, H or carbachol (C) and to determine the contribution of alpha-adrenoceptors to the relaxant effect of D in vitro.
Tracheas of female guinea pigs were cut spirally into strips and mounted in water-jacketed organ baths in Tyrode's solution, aerated with a mixture of 95% O2 and 5% CO2 at 37 degrees C. The changes in isometric tension induced by each spasmogen in the strips were measured with a transducer and a polygraph.
We found that D inhibited the tracheal contractions induced by 5-HT, H or C in a concentration-dependent manner. At 1.25 x 10(-6) M D blocked the effect of 10(-4) M 5-HT by 44.1 +/- 4.3% and at 2.5 x 10(-6) M by 63.8 +/- 3.8%. Similarly, at 5.0 x 10(-6) M concentration, D blocked the effect of 10(-5) M H by 27.7 +/- 5.3% and at 10(-5) M by 56.2 +/- 2.6%. Furthermore, 5 x 10(-6) M of D reduced the contractions produced by 10(-7) M C by 37.1 +/- 3.0% and 10(-5) M of D by 76.1 +/- 3.2%. The inhibiting effect of D was strongest on contractions induced by 5-HT. Prazosin (10(-6) M) affected neither 5-HT-induced contractions nor the inhibition by D.
Our data indicate that D partially blocks the contractile responses not only to 5-HT, an effect which would be mediated through a blockade of the 5-HT receptors, but also to H or C, probably through inhibition of calmodulin. Our data support previous reports indicating that droperidol may be an important therapeutic agent in the treatment of patients with hyperreactive airways. |
| doi_str_mv | 10.1007/BF03011259 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_78356599</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>78356599</sourcerecordid><originalsourceid>FETCH-LOGICAL-c347t-6342fbe4fe152da90d3bd79cd233c9f9d70c150621559dcac369b9c331b1a8ab3</originalsourceid><addsrcrecordid>eNpFkDtPwzAURi0EKqWwsCN5QAyIgB9xbI9QnlIlFpDYIr_SGiVxsZOh_56URmW6V_ec-w0fAOcY3WKE-N3DM6IIY8LkAZjiXBaZkJwdgikSlGQFRl_H4CSlb4SQKJiYgIkQhLGcToF9jGHtorehhr5dee27BLuozMqpGprQbvfOh3agtjfOQr2BycXQhda3N3DlU6ca3zoYIjQq6uHzLwou--Gq4Nov0yk4qlSd3Nk4Z-Dz-elj_pot3l_e5veLzNCcd1lBc1Jpl1cOM2KVRJZqy6WxhFIjK2k5MpihgmDGpDXK0EJqaSjFGiuhNJ2Bq13uOoaf3qWubHwyrq5V60KfSi4oK5iUg3i9E00MKUVXlevoGxU3JUblttLyv9JBvhhTe904u1fHDgd-OXKVjKqrqFrj014jUuSEc_oLHZ9-9Q</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>78356599</pqid></control><display><type>article</type><title>Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs</title><source>MEDLINE</source><source>SpringerLink Journals - AutoHoldings</source><creator>SATO, T ; HIROTA, K ; MATSUKI, A ; ZSIGMOND, E. K ; RABITO, S. F</creator><creatorcontrib>SATO, T ; HIROTA, K ; MATSUKI, A ; ZSIGMOND, E. K ; RABITO, S. F</creatorcontrib><description>Droperidol (D) is effective in the treatment of patients with status asthmaticus. It has been reported that D inhibits the bronchoconstriction induced by serotonin (5-HT) but not that by histamine (H) or acetylcholine. However, haloperidol, another butyrophenone, is known to interact with and inhibit calmodulin, an intracellular Ca(++)-binding protein which is important in the contraction of smooth muscles. The present study was designed to investigate the effects of D on tracheal contractions induced by 5-HT, H or carbachol (C) and to determine the contribution of alpha-adrenoceptors to the relaxant effect of D in vitro.
Tracheas of female guinea pigs were cut spirally into strips and mounted in water-jacketed organ baths in Tyrode's solution, aerated with a mixture of 95% O2 and 5% CO2 at 37 degrees C. The changes in isometric tension induced by each spasmogen in the strips were measured with a transducer and a polygraph.
We found that D inhibited the tracheal contractions induced by 5-HT, H or C in a concentration-dependent manner. At 1.25 x 10(-6) M D blocked the effect of 10(-4) M 5-HT by 44.1 +/- 4.3% and at 2.5 x 10(-6) M by 63.8 +/- 3.8%. Similarly, at 5.0 x 10(-6) M concentration, D blocked the effect of 10(-5) M H by 27.7 +/- 5.3% and at 10(-5) M by 56.2 +/- 2.6%. Furthermore, 5 x 10(-6) M of D reduced the contractions produced by 10(-7) M C by 37.1 +/- 3.0% and 10(-5) M of D by 76.1 +/- 3.2%. The inhibiting effect of D was strongest on contractions induced by 5-HT. Prazosin (10(-6) M) affected neither 5-HT-induced contractions nor the inhibition by D.
Our data indicate that D partially blocks the contractile responses not only to 5-HT, an effect which would be mediated through a blockade of the 5-HT receptors, but also to H or C, probably through inhibition of calmodulin. Our data support previous reports indicating that droperidol may be an important therapeutic agent in the treatment of patients with hyperreactive airways.</description><identifier>ISSN: 0832-610X</identifier><identifier>EISSN: 1496-8975</identifier><identifier>DOI: 10.1007/BF03011259</identifier><identifier>PMID: 8825543</identifier><identifier>CODEN: CJOAEP</identifier><language>eng</language><publisher>Toronto, ON: Canadian Anesthesiologists' Society</publisher><subject>Anesthetics, Intravenous - pharmacology ; Animals ; Biological and medical sciences ; Carbachol - pharmacology ; Droperidol - pharmacology ; Female ; Guinea Pigs ; Histamine - pharmacology ; In Vitro Techniques ; Medical sciences ; Muscarinic Agonists - pharmacology ; Muscle Contraction - drug effects ; Pharmacology. Drug treatments ; Prazosin - pharmacology ; Respiratory system ; Serotonin - pharmacology ; Trachea - drug effects ; Trachea - physiology</subject><ispartof>Canadian journal of anesthesia, 1996-02, Vol.43 (2), p.172-178</ispartof><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c347t-6342fbe4fe152da90d3bd79cd233c9f9d70c150621559dcac369b9c331b1a8ab3</citedby><cites>FETCH-LOGICAL-c347t-6342fbe4fe152da90d3bd79cd233c9f9d70c150621559dcac369b9c331b1a8ab3</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=2984277$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8825543$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SATO, T</creatorcontrib><creatorcontrib>HIROTA, K</creatorcontrib><creatorcontrib>MATSUKI, A</creatorcontrib><creatorcontrib>ZSIGMOND, E. K</creatorcontrib><creatorcontrib>RABITO, S. F</creatorcontrib><title>Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs</title><title>Canadian journal of anesthesia</title><addtitle>Can J Anaesth</addtitle><description>Droperidol (D) is effective in the treatment of patients with status asthmaticus. It has been reported that D inhibits the bronchoconstriction induced by serotonin (5-HT) but not that by histamine (H) or acetylcholine. However, haloperidol, another butyrophenone, is known to interact with and inhibit calmodulin, an intracellular Ca(++)-binding protein which is important in the contraction of smooth muscles. The present study was designed to investigate the effects of D on tracheal contractions induced by 5-HT, H or carbachol (C) and to determine the contribution of alpha-adrenoceptors to the relaxant effect of D in vitro.
Tracheas of female guinea pigs were cut spirally into strips and mounted in water-jacketed organ baths in Tyrode's solution, aerated with a mixture of 95% O2 and 5% CO2 at 37 degrees C. The changes in isometric tension induced by each spasmogen in the strips were measured with a transducer and a polygraph.
We found that D inhibited the tracheal contractions induced by 5-HT, H or C in a concentration-dependent manner. At 1.25 x 10(-6) M D blocked the effect of 10(-4) M 5-HT by 44.1 +/- 4.3% and at 2.5 x 10(-6) M by 63.8 +/- 3.8%. Similarly, at 5.0 x 10(-6) M concentration, D blocked the effect of 10(-5) M H by 27.7 +/- 5.3% and at 10(-5) M by 56.2 +/- 2.6%. Furthermore, 5 x 10(-6) M of D reduced the contractions produced by 10(-7) M C by 37.1 +/- 3.0% and 10(-5) M of D by 76.1 +/- 3.2%. The inhibiting effect of D was strongest on contractions induced by 5-HT. Prazosin (10(-6) M) affected neither 5-HT-induced contractions nor the inhibition by D.
Our data indicate that D partially blocks the contractile responses not only to 5-HT, an effect which would be mediated through a blockade of the 5-HT receptors, but also to H or C, probably through inhibition of calmodulin. Our data support previous reports indicating that droperidol may be an important therapeutic agent in the treatment of patients with hyperreactive airways.</description><subject>Anesthetics, Intravenous - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Carbachol - pharmacology</subject><subject>Droperidol - pharmacology</subject><subject>Female</subject><subject>Guinea Pigs</subject><subject>Histamine - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Medical sciences</subject><subject>Muscarinic Agonists - pharmacology</subject><subject>Muscle Contraction - drug effects</subject><subject>Pharmacology. Drug treatments</subject><subject>Prazosin - pharmacology</subject><subject>Respiratory system</subject><subject>Serotonin - pharmacology</subject><subject>Trachea - drug effects</subject><subject>Trachea - physiology</subject><issn>0832-610X</issn><issn>1496-8975</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkDtPwzAURi0EKqWwsCN5QAyIgB9xbI9QnlIlFpDYIr_SGiVxsZOh_56URmW6V_ec-w0fAOcY3WKE-N3DM6IIY8LkAZjiXBaZkJwdgikSlGQFRl_H4CSlb4SQKJiYgIkQhLGcToF9jGHtorehhr5dee27BLuozMqpGprQbvfOh3agtjfOQr2BycXQhda3N3DlU6ca3zoYIjQq6uHzLwou--Gq4Nov0yk4qlSd3Nk4Z-Dz-elj_pot3l_e5veLzNCcd1lBc1Jpl1cOM2KVRJZqy6WxhFIjK2k5MpihgmDGpDXK0EJqaSjFGiuhNJ2Bq13uOoaf3qWubHwyrq5V60KfSi4oK5iUg3i9E00MKUVXlevoGxU3JUblttLyv9JBvhhTe904u1fHDgd-OXKVjKqrqFrj014jUuSEc_oLHZ9-9Q</recordid><startdate>19960201</startdate><enddate>19960201</enddate><creator>SATO, T</creator><creator>HIROTA, K</creator><creator>MATSUKI, A</creator><creator>ZSIGMOND, E. K</creator><creator>RABITO, S. F</creator><general>Canadian Anesthesiologists' Society</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>19960201</creationdate><title>Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs</title><author>SATO, T ; HIROTA, K ; MATSUKI, A ; ZSIGMOND, E. K ; RABITO, S. F</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c347t-6342fbe4fe152da90d3bd79cd233c9f9d70c150621559dcac369b9c331b1a8ab3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Anesthetics, Intravenous - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Carbachol - pharmacology</topic><topic>Droperidol - pharmacology</topic><topic>Female</topic><topic>Guinea Pigs</topic><topic>Histamine - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Medical sciences</topic><topic>Muscarinic Agonists - pharmacology</topic><topic>Muscle Contraction - drug effects</topic><topic>Pharmacology. Drug treatments</topic><topic>Prazosin - pharmacology</topic><topic>Respiratory system</topic><topic>Serotonin - pharmacology</topic><topic>Trachea - drug effects</topic><topic>Trachea - physiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SATO, T</creatorcontrib><creatorcontrib>HIROTA, K</creatorcontrib><creatorcontrib>MATSUKI, A</creatorcontrib><creatorcontrib>ZSIGMOND, E. K</creatorcontrib><creatorcontrib>RABITO, S. F</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>Canadian journal of anesthesia</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SATO, T</au><au>HIROTA, K</au><au>MATSUKI, A</au><au>ZSIGMOND, E. K</au><au>RABITO, S. F</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs</atitle><jtitle>Canadian journal of anesthesia</jtitle><addtitle>Can J Anaesth</addtitle><date>1996-02-01</date><risdate>1996</risdate><volume>43</volume><issue>2</issue><spage>172</spage><epage>178</epage><pages>172-178</pages><issn>0832-610X</issn><eissn>1496-8975</eissn><coden>CJOAEP</coden><abstract>Droperidol (D) is effective in the treatment of patients with status asthmaticus. It has been reported that D inhibits the bronchoconstriction induced by serotonin (5-HT) but not that by histamine (H) or acetylcholine. However, haloperidol, another butyrophenone, is known to interact with and inhibit calmodulin, an intracellular Ca(++)-binding protein which is important in the contraction of smooth muscles. The present study was designed to investigate the effects of D on tracheal contractions induced by 5-HT, H or carbachol (C) and to determine the contribution of alpha-adrenoceptors to the relaxant effect of D in vitro.
Tracheas of female guinea pigs were cut spirally into strips and mounted in water-jacketed organ baths in Tyrode's solution, aerated with a mixture of 95% O2 and 5% CO2 at 37 degrees C. The changes in isometric tension induced by each spasmogen in the strips were measured with a transducer and a polygraph.
We found that D inhibited the tracheal contractions induced by 5-HT, H or C in a concentration-dependent manner. At 1.25 x 10(-6) M D blocked the effect of 10(-4) M 5-HT by 44.1 +/- 4.3% and at 2.5 x 10(-6) M by 63.8 +/- 3.8%. Similarly, at 5.0 x 10(-6) M concentration, D blocked the effect of 10(-5) M H by 27.7 +/- 5.3% and at 10(-5) M by 56.2 +/- 2.6%. Furthermore, 5 x 10(-6) M of D reduced the contractions produced by 10(-7) M C by 37.1 +/- 3.0% and 10(-5) M of D by 76.1 +/- 3.2%. The inhibiting effect of D was strongest on contractions induced by 5-HT. Prazosin (10(-6) M) affected neither 5-HT-induced contractions nor the inhibition by D.
Our data indicate that D partially blocks the contractile responses not only to 5-HT, an effect which would be mediated through a blockade of the 5-HT receptors, but also to H or C, probably through inhibition of calmodulin. Our data support previous reports indicating that droperidol may be an important therapeutic agent in the treatment of patients with hyperreactive airways.</abstract><cop>Toronto, ON</cop><pub>Canadian Anesthesiologists' Society</pub><pmid>8825543</pmid><doi>10.1007/BF03011259</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0832-610X |
| ispartof | Canadian journal of anesthesia, 1996-02, Vol.43 (2), p.172-178 |
| issn | 0832-610X 1496-8975 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_78356599 |
| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Anesthetics, Intravenous - pharmacology Animals Biological and medical sciences Carbachol - pharmacology Droperidol - pharmacology Female Guinea Pigs Histamine - pharmacology In Vitro Techniques Medical sciences Muscarinic Agonists - pharmacology Muscle Contraction - drug effects Pharmacology. Drug treatments Prazosin - pharmacology Respiratory system Serotonin - pharmacology Trachea - drug effects Trachea - physiology |
| title | Droperidol inhibits tracheal contraction induced by serotonin, histamine or carbachol in guinea pigs |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-20T06%3A58%3A02IST&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=Droperidol%20inhibits%20tracheal%20contraction%20induced%20by%20serotonin,%20histamine%20or%20carbachol%20in%20guinea%20pigs&rft.jtitle=Canadian%20journal%20of%20anesthesia&rft.au=SATO,%20T&rft.date=1996-02-01&rft.volume=43&rft.issue=2&rft.spage=172&rft.epage=178&rft.pages=172-178&rft.issn=0832-610X&rft.eissn=1496-8975&rft.coden=CJOAEP&rft_id=info:doi/10.1007/BF03011259&rft_dat=%3Cproquest_cross%3E78356599%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=78356599&rft_id=info:pmid/8825543&rfr_iscdi=true |