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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Pflügers Archiv 364 (1976), S. 65-70 
    ISSN: 1432-2013
    Keywords: Node of Ranvier ; Voltage clamp ; Procaine ; Saxitoxin ; Na channel ; Independent receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1. Voltage clamp experiments were done on single myelinated nerve fibres of the frog,Rana esculenta. 2. The time course of procaine action (1.0 mM at pH 7.2) was obtained from changes inI Na on changing solutions during repetitive (1 Hz) depolarizing pulses of constant amplitude following hyperpolarizing prepulses. The mean half times of onset and offset of procaine block were 3.7 and 28 s, respectively. In the presence of 1.4 nM saxitoxin (STX) the corresponding times were virtually the same, 3.1 and 27 s. 3. Similarly, the time course of partial relief from procaine block that is obtained by increasing the frequency of the prepulse-test pulse pairs from 1–10 Hz was unaffected in the presence of STX. 4. Comparison of the equilibrium effects of procaine concentrations ranging from 0.03–1.0 mM suggest a one-to-one drug-receptor reaction. The fraction of Na channels blocked at equilibrium with 1.0 mM procaine, 1.4 nM STX, and 1.0 mM procaine + 1.4 nM STX was 0.81, 0.49, and 0.90, respectively. This result and the kinetic behaviour fully agree with the idea of two separate and independent receptors for procaine and STX.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-2013
    Keywords: Node of Ranvier ; Block of Na channels ; Procaine ; Benzocaine ; Procaine-benzocaine interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract 1. Action potentials and their maximum rates of rise, $$\dot V_{\text{A}}$$ , were measured in single myelinated nerve fibres of the frog,Rana esculenta at room temperature. 2. On applying 1 mM procaine (pH 7.2) at 20 Hz stimulus frequency, half of the final $$\dot V_{\text{A}}$$ reduction was reached att on=0.27s; on applying 0.5 mM benzocaine (pH 7.2) at 50 Hz,t on was 0.12s. Increasing the stimulus frequency between 2 and 50 Hz increased the rate of block by procaine but not by benzocaine. 3. Recovery in Ringer solution (pH 7.2) from 30-s treatment with 1 mM procaine (pH 7.2), the equieffective 0.15 mM procaine (pH 8.9) and from 0.5 mM benzocaine (pH 7.2) was 54%, 31% and 70%, respectively, within 1 s. 4. Changing between alkaline Ringer solution (pH 8.9) and 1 mM procaine (pH 7.2) led to transitory excessive block. Changing between 1 mM procaine (pH 7.2) and acid Ringer solution (pH 6.0) and washing out 10 mM procaine (pH 5.5) with neutral Ringer solution also led to a non-monotonic change in $$\dot V_{\text{A}}$$ . 5. If hyperpolarizing pulses (30 ms, 20 mV) preceded the stimuli, changing the frequency of the pulse pairs led to a gradual moderate relief of block in procaine, turning off prepulses (at 10 Hz) to a gradual increase of block. In benzocaine changing from 1 to 10 Hz had no effect but turning off prepulses led to a prompt large increase of block. In procaine + benzocaine the membrane responded much as in benzocaine alone. At 1 Hz (prepulses) $$\dot V_{\text{A}}$$ in 0.4 mM procaine wassmaller than in 0.4 mM procaine + 0.3 mM benzocaine. 6. These phenomena can be explained on the assumption of voltage-dependent binding of benzocaine and procaine to a common receptor. The rate of block appears to be limited by access to the receptor, more in the case of benzocaine than of procaine.
    Type of Medium: Electronic Resource
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