1973
DOI: 10.1254/jjp.23.805
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Some Factors Affecting the Neuron Blocking Action of Guanethidine, Xylocholine, Bretylium and Debrisoquin

Abstract: The uptake of guanethidine (3.3×10-5 M), debrisoquin (8.4×10-4 M), The uptake of noradrenaline (NA) by the adrenergic neuron is energy dependent (1, 2, 3) and sodium dependent (4,5,6, 7,8,9). Guanethidine utilises this NA uptake me chanism for transport across the membrane of neurons (10, 11) and of human platelets (12) which can serve as convenient model for the neuron (13). Support for this common transport mechanism for NA and guanethidine is derived from observations of th… Show more

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Cited by 5 publications
(2 citation statements)
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“…This report would be more convincing if it were based on a larger number of data points and if results obtained with a known competitive inhibitor of uptake were also presented for purposes of comparison. PRASAD et al (1973) presented evidence that the onset of neuron blockade produced by guanethidine (3.3 x 10-5 M), debrisoquin (8.4 x 10-4 M), bretylium (5 x 10-4 M) and xylocholine (10-3 M) in guinea pig vas deferens was prevented by 3 x 10-3 M norepinephrine and by low temperature (0° C). However, they stated that the onset of neuron blockade by only one of these agents, guanethidine, was inhibited by removal of sodium from the incubation medium.…”
mentioning
confidence: 99%
“…This report would be more convincing if it were based on a larger number of data points and if results obtained with a known competitive inhibitor of uptake were also presented for purposes of comparison. PRASAD et al (1973) presented evidence that the onset of neuron blockade produced by guanethidine (3.3 x 10-5 M), debrisoquin (8.4 x 10-4 M), bretylium (5 x 10-4 M) and xylocholine (10-3 M) in guinea pig vas deferens was prevented by 3 x 10-3 M norepinephrine and by low temperature (0° C). However, they stated that the onset of neuron blockade by only one of these agents, guanethidine, was inhibited by removal of sodium from the incubation medium.…”
mentioning
confidence: 99%
“…Various workers (Chang, Costa & Brodie, 1965;Obinawu, Stitzel & Lundborg, 1968;Prasad, Shah & Gulati, 1973) have shown that guanethidine is a substrate for the noradrenaline transport mechanism in the cytoplasmic membrane of adrenergic nerve terminals. By competing with noradrenaline for the uptake process, guanethidine might cause an accumulation of spontaneously released noradrenaline in the extracellular space and hence evoke spasm of the anococcygeus muscle.…”
Section: Introductionmentioning
confidence: 99%