Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644
We have investigated the voltage-dependent effects of the dihydropyridine Bay K8644 on Ca channel currents in calf Purkinje fibers and enzymatically dispersed rat ventricular myocytes. Bay K8644 increases the apparent rate of inactivation of these currents, measured during depolarizing voltage pulse...
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| Veröffentlicht in: | The Journal of general physiology 1986-09, Vol.88 (3), p.369-392 |
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| container_title | The Journal of general physiology |
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| creator | SANGUINETTI, M. C KRAFTE, D. S KASS, R. S |
| description | We have investigated the voltage-dependent effects of the dihydropyridine Bay K8644 on Ca channel currents in calf Purkinje fibers and enzymatically dispersed rat ventricular myocytes. Bay K8644 increases the apparent rate of inactivation of these currents, measured during depolarizing voltage pulses, and shifts both channel activation and inactivation in the hyperpolarizing direction. Consequently, currents measured after hyperpolarizing conditioning pulses are larger in the presence of drug compared with control conditions, but are smaller than control if they are measured after positive conditioning pulses. Most of our experimental observations on macroscopic currents can be explained by a single drug-induced change in one rate constant of a simple kinetic model. The rate constant change is consistent with results obtained by others with single channel recordings. |
| doi_str_mv | 10.1085/jgp.88.3.369 |
| format | Article |
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The rate constant change is consistent with results obtained by others with single channel recordings.</description><identifier>ISSN: 0022-1295</identifier><identifier>EISSN: 1540-7748</identifier><identifier>DOI: 10.1085/jgp.88.3.369</identifier><identifier>PMID: 2428922</identifier><identifier>CODEN: JGPLAD</identifier><language>eng</language><publisher>New York, NY: Rockefeller University Press</publisher><subject>3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology ; Animals ; BAY K 8644 ; Biological and medical sciences ; calcium ; Calcium - metabolism ; Calcium Channel Blockers - pharmacology ; Cattle ; Electric Conductivity ; Fundamental and applied biological sciences. Psychology ; Heart ; Heart - physiology ; Heart Conduction System - physiology ; Heart Ventricles - drug effects ; In Vitro Techniques ; Ion Channels - drug effects ; Ion Channels - physiology ; Kinetics ; Membrane Potentials - drug effects ; Nifedipine - analogs & derivatives ; Nifedipine - pharmacology ; Nisoldipine ; Purkinje Fibers - drug effects ; Purkinje Fibers - physiology ; Rats ; Ventricular Function ; Vertebrates: cardiovascular system</subject><ispartof>The Journal of general physiology, 1986-09, Vol.88 (3), p.369-392</ispartof><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c505t-dece6a7e6050b276a56ce6eed433ac13152f00b185928f0e12eb36c6f826abca3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,776,780,881,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7961134$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2428922$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SANGUINETTI, M. C</creatorcontrib><creatorcontrib>KRAFTE, D. S</creatorcontrib><creatorcontrib>KASS, R. S</creatorcontrib><title>Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644</title><title>The Journal of general physiology</title><addtitle>J Gen Physiol</addtitle><description>We have investigated the voltage-dependent effects of the dihydropyridine Bay K8644 on Ca channel currents in calf Purkinje fibers and enzymatically dispersed rat ventricular myocytes. Bay K8644 increases the apparent rate of inactivation of these currents, measured during depolarizing voltage pulses, and shifts both channel activation and inactivation in the hyperpolarizing direction. Consequently, currents measured after hyperpolarizing conditioning pulses are larger in the presence of drug compared with control conditions, but are smaller than control if they are measured after positive conditioning pulses. Most of our experimental observations on macroscopic currents can be explained by a single drug-induced change in one rate constant of a simple kinetic model. The rate constant change is consistent with results obtained by others with single channel recordings.</description><subject>3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology</subject><subject>Animals</subject><subject>BAY K 8644</subject><subject>Biological and medical sciences</subject><subject>calcium</subject><subject>Calcium - metabolism</subject><subject>Calcium Channel Blockers - pharmacology</subject><subject>Cattle</subject><subject>Electric Conductivity</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Heart</subject><subject>Heart - physiology</subject><subject>Heart Conduction System - physiology</subject><subject>Heart Ventricles - drug effects</subject><subject>In Vitro Techniques</subject><subject>Ion Channels - drug effects</subject><subject>Ion Channels - physiology</subject><subject>Kinetics</subject><subject>Membrane Potentials - drug effects</subject><subject>Nifedipine - analogs & derivatives</subject><subject>Nifedipine - pharmacology</subject><subject>Nisoldipine</subject><subject>Purkinje Fibers - drug effects</subject><subject>Purkinje Fibers - physiology</subject><subject>Rats</subject><subject>Ventricular Function</subject><subject>Vertebrates: cardiovascular system</subject><issn>0022-1295</issn><issn>1540-7748</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1986</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc2P0zAQxS0EWsrCjSuSD4gTKfY4_sgFaan4Eiu4AFdr4kzarFKn2AlS_3tcbVXBibmMNO-nNzN6jD2XYi2F02_utoe1c2u1VqZ5wFZS16KytnYP2UoIgEpCox-zJznfiVIaxBW7ghpcA7BiX39O44xbqjo6UOwoznw_dcuI8zBFPvV8gzzsMEYaeVhSOgFD5DvCNPNA45h5e-Tv8Mi_OFPXT9mjHsdMz879mv348P775lN1--3j583NbRW00HNZFsigJSO0aMEa1KYMiLpaKQxSSQ29EK10ugHXC5JArTLB9A4MtgHVNXt773tY2j11oZyVcPSHNOwxHf2Eg_9XicPOb6ffHgCcA1sMXp0N0vRroTz7_ZBP_2CkacneWmHASvNfUNZaq8IW8PU9GNKUc6L-co0U_hSUL0F557zyJaiCv_j7gwt8TqboL8865oBjnzCGIV8w2xgpVa3-AP_rm5Y</recordid><startdate>19860901</startdate><enddate>19860901</enddate><creator>SANGUINETTI, M. C</creator><creator>KRAFTE, D. S</creator><creator>KASS, R. S</creator><general>Rockefeller University Press</general><general>The Rockefeller University Press</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>7QP</scope><scope>8FD</scope><scope>FR3</scope><scope>M7Z</scope><scope>P64</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>19860901</creationdate><title>Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644</title><author>SANGUINETTI, M. C ; KRAFTE, D. S ; KASS, R. S</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c505t-dece6a7e6050b276a56ce6eed433ac13152f00b185928f0e12eb36c6f826abca3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1986</creationdate><topic>3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology</topic><topic>Animals</topic><topic>BAY K 8644</topic><topic>Biological and medical sciences</topic><topic>calcium</topic><topic>Calcium - metabolism</topic><topic>Calcium Channel Blockers - pharmacology</topic><topic>Cattle</topic><topic>Electric Conductivity</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Heart</topic><topic>Heart - physiology</topic><topic>Heart Conduction System - physiology</topic><topic>Heart Ventricles - drug effects</topic><topic>In Vitro Techniques</topic><topic>Ion Channels - drug effects</topic><topic>Ion Channels - physiology</topic><topic>Kinetics</topic><topic>Membrane Potentials - drug effects</topic><topic>Nifedipine - analogs & derivatives</topic><topic>Nifedipine - pharmacology</topic><topic>Nisoldipine</topic><topic>Purkinje Fibers - drug effects</topic><topic>Purkinje Fibers - physiology</topic><topic>Rats</topic><topic>Ventricular Function</topic><topic>Vertebrates: cardiovascular system</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SANGUINETTI, M. C</creatorcontrib><creatorcontrib>KRAFTE, D. S</creatorcontrib><creatorcontrib>KASS, R. 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S</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644</atitle><jtitle>The Journal of general physiology</jtitle><addtitle>J Gen Physiol</addtitle><date>1986-09-01</date><risdate>1986</risdate><volume>88</volume><issue>3</issue><spage>369</spage><epage>392</epage><pages>369-392</pages><issn>0022-1295</issn><eissn>1540-7748</eissn><coden>JGPLAD</coden><abstract>We have investigated the voltage-dependent effects of the dihydropyridine Bay K8644 on Ca channel currents in calf Purkinje fibers and enzymatically dispersed rat ventricular myocytes. Bay K8644 increases the apparent rate of inactivation of these currents, measured during depolarizing voltage pulses, and shifts both channel activation and inactivation in the hyperpolarizing direction. Consequently, currents measured after hyperpolarizing conditioning pulses are larger in the presence of drug compared with control conditions, but are smaller than control if they are measured after positive conditioning pulses. Most of our experimental observations on macroscopic currents can be explained by a single drug-induced change in one rate constant of a simple kinetic model. The rate constant change is consistent with results obtained by others with single channel recordings.</abstract><cop>New York, NY</cop><pub>Rockefeller University Press</pub><pmid>2428922</pmid><doi>10.1085/jgp.88.3.369</doi><tpages>24</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | The Journal of general physiology, 1986-09, Vol.88 (3), p.369-392 |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection |
| subjects | 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester - pharmacology Animals BAY K 8644 Biological and medical sciences calcium Calcium - metabolism Calcium Channel Blockers - pharmacology Cattle Electric Conductivity Fundamental and applied biological sciences. Psychology Heart Heart - physiology Heart Conduction System - physiology Heart Ventricles - drug effects In Vitro Techniques Ion Channels - drug effects Ion Channels - physiology Kinetics Membrane Potentials - drug effects Nifedipine - analogs & derivatives Nifedipine - pharmacology Nisoldipine Purkinje Fibers - drug effects Purkinje Fibers - physiology Rats Ventricular Function Vertebrates: cardiovascular system |
| title | Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644 |
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