By Howard Rogers and Roy G. Spector (Auth.)
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Extra resources for An Introduction to Mechanisms in Pharmacology and Therapeutics
This proportionality of flux to transmembrane concentration difference is seen in membrane transport by simple diffusion. In saturation kinetics, the particles do not travel by diffusion alone but appear to bind to a larger molecule in the membrane (the carrier), which by movement or other means facilitates the transport process. With this mechanism, increasing the transmembrane difference in concentration results in an increase in velocity of particle flow only up to a certain maximum value. At this 'saturated' state all the carrier sites are associating and dissociating with the particles at their maximum rate and the velocity of flow cannot be further enhanced.
The mechanism for the increase in permeability is not understood, but could be related to a decrease in (positive) charge on the membrane surface. A similar effect also occurs if the fluid bathing the nerve is made alkaline in fact patients with alkalosis do show a similar increase in nerve and 48 MECHANISMS IN PHARMACOLOGY A N D THERAPEUTICS muscle excitability to those suffering from hypocalcaemia. Conversely hypercalcaemia decreases nerve excitability and lowers permeability of the sodium channel.
And Mittag T. W. (1969) Approaches to the molecular nature of pharmacological receptors Pharmac. Rev. 2 1 , 131-81 Kasai M. P. (1971) In vitro excitation of purified membrane fragments by cholinergic agonists I Pharmacological properties of the excitable membrane fragments/. Memb. Biol. 6, 1 - 23. Mackay D. ( 1966) The mathematics of drug-receptor interactions /. Pharm. Pharmac, 18, 201 - 222. , Molinoff P. and Potter T. L. (1971) Isolation of cholinergic receptor protein of Torpedo electric tissue Nature 2 2 9 , 5 5 4 - 557.
An Introduction to Mechanisms in Pharmacology and Therapeutics by Howard Rogers and Roy G. Spector (Auth.)