An Introduction to Mechanisms in Pharmacology and - download pdf or read online

By Howard Rogers and Roy G. Spector (Auth.)

ISBN-10: 1483168034

ISBN-13: 9781483168036

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Extra info for An Introduction to Mechanisms in Pharmacology and Therapeutics

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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. Molecular Properties of Drug Receptors - Ciba Foundation Symposium (1970) Eds.

E. e. [B] = J- This is a useful method of determining K B as it does not rely on any assumptions concerning receptor occupancy or generation of the biological stimulus since the parameter measured experimentally is the size of the tissue's response to the agonist and this is maintained constant throughout. e. e. the negative logarithm of the concentration of antagonist (B) which necessitates doubling the agonist concentration in order to maintain a constant tissue response, p A 2 = l o g 10 K B (17) When χ = 10 A 1ο P io = 8ιο K B - l o Bio = p A 2 - l o g 1 09 9 from (17) hence - p A 1 0 = l O g 1 09 If this relationship between p A 2 and p A 1 0 is found to be valid then the antagonist is competitive.

This work is regarded by many as having come near to the isolation of the cholinergic receptor. The alternative approach using primary tissue fractionation followed by identification of the receptor as a secondary procedure has been used by several groups of workers. A number of candidates for the acetylcholine 38 MECHANISMS IN PHARMACOLOGY A N D THERAPEUTICS receptor of the electric eel electroplax have been put forward which to a certain degree comply with the criteria of receptor identification set out above.

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An Introduction to Mechanisms in Pharmacology and Therapeutics by Howard Rogers and Roy G. Spector (Auth.)


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