ArticlePflugers Archiv : European journal of physiology1993
The molecular mode of action of the Ca agonist (-) BAY K 8644 on the cardiac Ca channel.
Article in Pflugers Archiv : European journal of physiology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 52 citations in OpenAlex.
- A mathematical model of hiPSC cardiomyocytes electromechanics.Physiological reports · 2021Article
- Structural Basis of the Modulation of the Voltage-Gated Calcium Ion Channel CaAngewandte Chemie (International ed. in English) · 2021Article
- Development of phenotypic assays for identifying novel blockers of L-type calcium channels in neurons.Scientific reports · 2021Article
- CRISPR-Mediated Single Nucleotide Polymorphism Modeling in Rats Reveals Insight Into Reduced Cardiovascular Risk Associated With MediterraneanHypertension (Dallas, Tex. : 1979) · 2020Article
- Developmental Synaptic Changes at the Transient Olivocochlear-Inner Hair Cell Synapse.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2019Article
- Beta-Estradiol Regulates Voltage-Gated Calcium Channels and Estrogen Receptors in Telocytes from Human Myometrium.International journal of molecular sciences · 2018Article
- Differential CaMKII regulation by voltage-gated calcium channels in the striatum.Molecular and cellular neurosciences · 2015Article
- Activity-dependent phosphorylation of GABAA receptors regulates receptor insertion and tonic current.The EMBO journal · 2012Article
- Revisiting the ionic mechanisms of early afterdepolarizations in cardiomyocytes: predominant by Ca waves or Ca currents?American journal of physiology. Heart and circulatory physiology · 2012Article
- Maturation of rat cerebellar Purkinje cells reveals an atypical Ca2+ channel current that is inhibited by omega-agatoxin IVA and the dihydropyridine (-)-(S)-Bay K8644.The Journal of physiology · 2007Article
- Molecular mechanisms of vasoselectivity of the 1,4-dihydropyridine lercanidipine.British journal of pharmacology · 2004Article
- Molecular pharmacology of high voltage-activated calcium channels.Journal of bioenergetics and biomembranes · 2003Review
- Barnidipine block of L-type Ca(2+) channel currents in rat ventricular cardiomyocytes.British journal of pharmacology · 2000Article
- Dihydropyridine-induced Ca2+ release from ryanodine-sensitive Ca2+ pools in human skeletal muscle cells.The Journal of physiology · 2000Article
- A dihydropyridine-sensitive voltage-dependent calcium channel in the sarcolemmal membrane of crustacean muscle.The Journal of general physiology · 1997Article
- Long Ca2+ channel opening induced by large depolarization and Bay K 8644 in smooth muscle cells isolated from guinea-pig detrusor.British journal of pharmacology · 1996Article
- L-type Ca2+ channels access multiple open states to produce two components of Bay K 8644-dependent current in GH3 cells.The Journal of general physiology · 1996Article
- Bay K 8644 reveals two components of L-type Ca2+ channel current in clonal rat pituitary cells.The Journal of general physiology · 1996Article
- Binding constants determined from Ca2+ current responses to rapid applications and washouts of nifedipine in frog cardiac myocytes.The Journal of physiology · 1996Article
- The IVS6 segment of the L-type calcium channel is critical for the action of dihydropyridines and phenylalkylamines.The EMBO journal · 1996Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The primary drug action of (-) BAY K 8644 on whole-cell Ca current in atrial myocytes was measured under conditions where secondary Ca-mediated changes of Ca channel activity were minimized. The most direct action of (-) BAY K 8644 is the change of gating kinetics which results in a strictly voltage-dependent increase of the peak current in the voltage range between -40 and 0 mV. Peak currents were increased dose dependently in the concentration range from 1 to 30 nM. Analysis of peak current/voltage relations revealed a linear shift of the current activation by approximately 23 mV to more negative membrane potentials, without any change in its voltage dependence and in the current reversal potential or the maximum whole-cell conductance. Measurement of Ca current activation and deactivation time constants suggests that (-) BAY K 8644 prolongs the single-channel open time without affecting the closed time. From the shift of the open time function to more negative voltages by about 50 mV the energy transferred to the gating process is calculated to be 5.4 kJ/mol (1.3 kcal/mol). The drug-induced slow component of tail current has been used to estimate the true dose/response relation for (-) BAY K 8644. A KD value of 4.3 nM and a Hill coefficient of 1.25 were determined. Flash-induced competition experiments with the Ca antagonist nifedipine allowed the measurement of binding kinetics of (-) BAY K 8644. The association rate constant is estimated to about 5 x 10(6) mol-1.s-1 and dissociation time constant is approximately 50-70 s; both are in close agreement with receptor binding studies. Results are discussed in relation to models for drug action of dihydropyridine-type compounds and to implications for the structure of the Ca channel protein.
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