Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts
1. The effects of two positively charged local anaesthetic amines, tetracaine and propranolol, on cation permeability were studied in resealed human red cell ghosts prepared from metabolically depleted erythrocytes. 2. The K permeability was reduced by tetracaine but increased by propranolol. The ef...
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| Veröffentlicht in: | The Journal of physiology 1975-07, Vol.249 (1), p.27-49 |
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| description | 1. The effects of two positively charged local anaesthetic amines, tetracaine and propranolol, on cation permeability were
studied in resealed human red cell ghosts prepared from metabolically depleted erythrocytes. 2. The K permeability was reduced
by tetracaine but increased by propranolol. The effect of tetracaine was independent of extracellular Ca concentration but
was raised to 2-5 x 10(-7) M. The effect of propranolol, which was enhanced when the external Ca concentration was raised,
could be completely inhibited by lowering the internal free Ca to less than 10(-7) M. 3. Propranolol, but not tetracaine,
increased the intracellular Ca ion concentration by releasing up to 20% of the membrane-bound Ca to the cell interior. This
increase in intracellular Ca was sufficient to mediate the observed change in K permeability. 4. Tetracaine and propranolol
reduced the Ca binding capacity of the ghost membrane by about 20 and 40% respectively. The Ca permeability was increased
by propranolol and was slightly reduced by tetracaine. 5. In high concentrations (2-7 mM) propranolol by itself moderately
increased K and Na permeability, but supressed completely the Ca-induced increase in K permeability. Tetracaine in concentrations
up to 4 mM enhanced the Ca-induced increase in K permeability. Higher concentrations of the drug caused lysis of the cells.
6. Maximally effective concentrations of tetracaine and propranolol inhibited the ATP-dependent Ca outward transport by 30
and 70% respectively. 7. The effects of tetracaine on K permeability were shared by the local anaesthetics prilocaine and
lidocaine, those of propranolol were shared by practolol, a beta-adrenergic antagonist and tetraethylammonium, a ganglionic
blocking agent. 8. It is suggested that the differences in the effects of tetracaine and propranolol on cation permeability
reflect qualitatively different interactions of the two drugs with Ca binding sites on the inner surface of the membrane. |
| doi_str_mv | 10.1113/jphysiol.1975.sp011001 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_1309556</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>82937177</sourcerecordid><originalsourceid>FETCH-LOGICAL-c4987-967331ea7beb919ad8865c3748fe09496e171c467cde2d1f84ccd64e6f921eb13</originalsourceid><addsrcrecordid>eNqNUUtv1DAQthCoLIWfAPKJW5ZMHnZ8QapW5aVKcChny-tMNq6cONjOVvn3OEpL4cZpNP4eM-OPkHeQ7wGg_HA39Uswzu5B8Hofphwgz-EZ2UHFRMa5KJ-TXZ4XRVbyGl6SVyHcJUKZC3FBLgBqaBjsSDy4YVJeRXNGGuLcLtR1NPZIsetQx7C2k3eTV6OzzlI1tjRi9EorMyJ1I9VJnMrgzjjgmBRmpB4DKost7edBrW1LNVpLT70LMbwmLzplA755qJfk56fr28OX7Ob756-Hq5tMV6LhmWC8LAEVP-JRgFBt07Bal7xqOsxFJRgCB10xrlssWuiaSuuWVcg6UQAeobwkHzffaT4O2Oq0nVdWTt4Myi_SKSP_RUbTy5M7y_Wb6polg_cPBt79mjFEOZiwHqJGdHOQTSFKDpwnItuI2rsQPHZ_hkAu17zkY15yzUs-5pWEb_9e8Um2BZTwqw2_NxaX_3SVt99-rA9FJaDgT1f05tTfG49yUwWnDcZFJpoEmYi_AQsaujw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>82937177</pqid></control><display><type>article</type><title>Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts</title><source>MEDLINE</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><source>Wiley Online Library All Journals</source><source>PubMed Central</source><source>Alma/SFX Local Collection</source><creator>Porzig, H</creator><creatorcontrib>Porzig, H</creatorcontrib><description>1. The effects of two positively charged local anaesthetic amines, tetracaine and propranolol, on cation permeability were
studied in resealed human red cell ghosts prepared from metabolically depleted erythrocytes. 2. The K permeability was reduced
by tetracaine but increased by propranolol. The effect of tetracaine was independent of extracellular Ca concentration but
was raised to 2-5 x 10(-7) M. The effect of propranolol, which was enhanced when the external Ca concentration was raised,
could be completely inhibited by lowering the internal free Ca to less than 10(-7) M. 3. Propranolol, but not tetracaine,
increased the intracellular Ca ion concentration by releasing up to 20% of the membrane-bound Ca to the cell interior. This
increase in intracellular Ca was sufficient to mediate the observed change in K permeability. 4. Tetracaine and propranolol
reduced the Ca binding capacity of the ghost membrane by about 20 and 40% respectively. The Ca permeability was increased
by propranolol and was slightly reduced by tetracaine. 5. In high concentrations (2-7 mM) propranolol by itself moderately
increased K and Na permeability, but supressed completely the Ca-induced increase in K permeability. Tetracaine in concentrations
up to 4 mM enhanced the Ca-induced increase in K permeability. Higher concentrations of the drug caused lysis of the cells.
6. Maximally effective concentrations of tetracaine and propranolol inhibited the ATP-dependent Ca outward transport by 30
and 70% respectively. 7. The effects of tetracaine on K permeability were shared by the local anaesthetics prilocaine and
lidocaine, those of propranolol were shared by practolol, a beta-adrenergic antagonist and tetraethylammonium, a ganglionic
blocking agent. 8. It is suggested that the differences in the effects of tetracaine and propranolol on cation permeability
reflect qualitatively different interactions of the two drugs with Ca binding sites on the inner surface of the membrane.</description><identifier>ISSN: 0022-3751</identifier><identifier>EISSN: 1469-7793</identifier><identifier>DOI: 10.1113/jphysiol.1975.sp011001</identifier><identifier>PMID: 1151861</identifier><language>eng</language><publisher>England: The Physiological Society</publisher><subject>Adenosine Triphosphate - metabolism ; Biological Transport, Active - drug effects ; Calcium - metabolism ; Cell Membrane Permeability - drug effects ; Erythrocytes - drug effects ; Erythrocytes - metabolism ; Humans ; In Vitro Techniques ; Intracellular Fluid - metabolism ; Lidocaine - pharmacology ; Potassium - metabolism ; Practolol - pharmacology ; Prilocaine - pharmacology ; Propranolol - pharmacology ; Sodium - metabolism ; Tetracaine - pharmacology ; Tetraethylammonium Compounds - pharmacology</subject><ispartof>The Journal of physiology, 1975-07, Vol.249 (1), p.27-49</ispartof><rights>1975 The Physiological Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4987-967331ea7beb919ad8865c3748fe09496e171c467cde2d1f84ccd64e6f921eb13</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1309556/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1309556/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,1417,27924,27925,45574,45575,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1151861$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Porzig, H</creatorcontrib><title>Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts</title><title>The Journal of physiology</title><addtitle>J Physiol</addtitle><description>1. The effects of two positively charged local anaesthetic amines, tetracaine and propranolol, on cation permeability were
studied in resealed human red cell ghosts prepared from metabolically depleted erythrocytes. 2. The K permeability was reduced
by tetracaine but increased by propranolol. The effect of tetracaine was independent of extracellular Ca concentration but
was raised to 2-5 x 10(-7) M. The effect of propranolol, which was enhanced when the external Ca concentration was raised,
could be completely inhibited by lowering the internal free Ca to less than 10(-7) M. 3. Propranolol, but not tetracaine,
increased the intracellular Ca ion concentration by releasing up to 20% of the membrane-bound Ca to the cell interior. This
increase in intracellular Ca was sufficient to mediate the observed change in K permeability. 4. Tetracaine and propranolol
reduced the Ca binding capacity of the ghost membrane by about 20 and 40% respectively. The Ca permeability was increased
by propranolol and was slightly reduced by tetracaine. 5. In high concentrations (2-7 mM) propranolol by itself moderately
increased K and Na permeability, but supressed completely the Ca-induced increase in K permeability. Tetracaine in concentrations
up to 4 mM enhanced the Ca-induced increase in K permeability. Higher concentrations of the drug caused lysis of the cells.
6. Maximally effective concentrations of tetracaine and propranolol inhibited the ATP-dependent Ca outward transport by 30
and 70% respectively. 7. The effects of tetracaine on K permeability were shared by the local anaesthetics prilocaine and
lidocaine, those of propranolol were shared by practolol, a beta-adrenergic antagonist and tetraethylammonium, a ganglionic
blocking agent. 8. It is suggested that the differences in the effects of tetracaine and propranolol on cation permeability
reflect qualitatively different interactions of the two drugs with Ca binding sites on the inner surface of the membrane.</description><subject>Adenosine Triphosphate - metabolism</subject><subject>Biological Transport, Active - drug effects</subject><subject>Calcium - metabolism</subject><subject>Cell Membrane Permeability - drug effects</subject><subject>Erythrocytes - drug effects</subject><subject>Erythrocytes - metabolism</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Intracellular Fluid - metabolism</subject><subject>Lidocaine - pharmacology</subject><subject>Potassium - metabolism</subject><subject>Practolol - pharmacology</subject><subject>Prilocaine - pharmacology</subject><subject>Propranolol - pharmacology</subject><subject>Sodium - metabolism</subject><subject>Tetracaine - pharmacology</subject><subject>Tetraethylammonium Compounds - pharmacology</subject><issn>0022-3751</issn><issn>1469-7793</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1975</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNUUtv1DAQthCoLIWfAPKJW5ZMHnZ8QapW5aVKcChny-tMNq6cONjOVvn3OEpL4cZpNP4eM-OPkHeQ7wGg_HA39Uswzu5B8Hofphwgz-EZ2UHFRMa5KJ-TXZ4XRVbyGl6SVyHcJUKZC3FBLgBqaBjsSDy4YVJeRXNGGuLcLtR1NPZIsetQx7C2k3eTV6OzzlI1tjRi9EorMyJ1I9VJnMrgzjjgmBRmpB4DKost7edBrW1LNVpLT70LMbwmLzplA755qJfk56fr28OX7Ob756-Hq5tMV6LhmWC8LAEVP-JRgFBt07Bal7xqOsxFJRgCB10xrlssWuiaSuuWVcg6UQAeobwkHzffaT4O2Oq0nVdWTt4Myi_SKSP_RUbTy5M7y_Wb6polg_cPBt79mjFEOZiwHqJGdHOQTSFKDpwnItuI2rsQPHZ_hkAu17zkY15yzUs-5pWEb_9e8Um2BZTwqw2_NxaX_3SVt99-rA9FJaDgT1f05tTfG49yUwWnDcZFJpoEmYi_AQsaujw</recordid><startdate>19750701</startdate><enddate>19750701</enddate><creator>Porzig, H</creator><general>The Physiological Society</general><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>19750701</creationdate><title>Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts</title><author>Porzig, H</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4987-967331ea7beb919ad8865c3748fe09496e171c467cde2d1f84ccd64e6f921eb13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1975</creationdate><topic>Adenosine Triphosphate - metabolism</topic><topic>Biological Transport, Active - drug effects</topic><topic>Calcium - metabolism</topic><topic>Cell Membrane Permeability - drug effects</topic><topic>Erythrocytes - drug effects</topic><topic>Erythrocytes - metabolism</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Intracellular Fluid - metabolism</topic><topic>Lidocaine - pharmacology</topic><topic>Potassium - metabolism</topic><topic>Practolol - pharmacology</topic><topic>Prilocaine - pharmacology</topic><topic>Propranolol - pharmacology</topic><topic>Sodium - metabolism</topic><topic>Tetracaine - pharmacology</topic><topic>Tetraethylammonium Compounds - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Porzig, H</creatorcontrib><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>The Journal of physiology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Porzig, H</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts</atitle><jtitle>The Journal of physiology</jtitle><addtitle>J Physiol</addtitle><date>1975-07-01</date><risdate>1975</risdate><volume>249</volume><issue>1</issue><spage>27</spage><epage>49</epage><pages>27-49</pages><issn>0022-3751</issn><eissn>1469-7793</eissn><abstract>1. The effects of two positively charged local anaesthetic amines, tetracaine and propranolol, on cation permeability were
studied in resealed human red cell ghosts prepared from metabolically depleted erythrocytes. 2. The K permeability was reduced
by tetracaine but increased by propranolol. The effect of tetracaine was independent of extracellular Ca concentration but
was raised to 2-5 x 10(-7) M. The effect of propranolol, which was enhanced when the external Ca concentration was raised,
could be completely inhibited by lowering the internal free Ca to less than 10(-7) M. 3. Propranolol, but not tetracaine,
increased the intracellular Ca ion concentration by releasing up to 20% of the membrane-bound Ca to the cell interior. This
increase in intracellular Ca was sufficient to mediate the observed change in K permeability. 4. Tetracaine and propranolol
reduced the Ca binding capacity of the ghost membrane by about 20 and 40% respectively. The Ca permeability was increased
by propranolol and was slightly reduced by tetracaine. 5. In high concentrations (2-7 mM) propranolol by itself moderately
increased K and Na permeability, but supressed completely the Ca-induced increase in K permeability. Tetracaine in concentrations
up to 4 mM enhanced the Ca-induced increase in K permeability. Higher concentrations of the drug caused lysis of the cells.
6. Maximally effective concentrations of tetracaine and propranolol inhibited the ATP-dependent Ca outward transport by 30
and 70% respectively. 7. The effects of tetracaine on K permeability were shared by the local anaesthetics prilocaine and
lidocaine, those of propranolol were shared by practolol, a beta-adrenergic antagonist and tetraethylammonium, a ganglionic
blocking agent. 8. It is suggested that the differences in the effects of tetracaine and propranolol on cation permeability
reflect qualitatively different interactions of the two drugs with Ca binding sites on the inner surface of the membrane.</abstract><cop>England</cop><pub>The Physiological Society</pub><pmid>1151861</pmid><doi>10.1113/jphysiol.1975.sp011001</doi><tpages>23</tpages><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Wiley Online Library All Journals; PubMed Central; Alma/SFX Local Collection |
| subjects | Adenosine Triphosphate - metabolism Biological Transport, Active - drug effects Calcium - metabolism Cell Membrane Permeability - drug effects Erythrocytes - drug effects Erythrocytes - metabolism Humans In Vitro Techniques Intracellular Fluid - metabolism Lidocaine - pharmacology Potassium - metabolism Practolol - pharmacology Prilocaine - pharmacology Propranolol - pharmacology Sodium - metabolism Tetracaine - pharmacology Tetraethylammonium Compounds - pharmacology |
| title | Comparative study of the effects of propranolol and tetracaine on cation movements in resealed human red cell ghosts |
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