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Pharmacokinetics 24 a) O C O O and is shown in Fig. 30 for isoniazid (= isonicotinic acid hydrazide), a tuberculostatic agent. 4. 28. Coenzymes that are important in drug metabolism. The groups transferred to the drugs are shown in red. a: UDPglucuronide (transfers glucuronate), b: PAPS (transfers sulfate), c: S-adenosylmethionine (transfers methyl group). Glucuronidation, sulfation and glutathione conjugation will all increase the polarity of the drug substrate and therefore facilitate renal elimination.

The ligand-bound receptor promotes the formation of a second messenger (M2), so that the concentration of M2 is at all times proportional to the receptor occupancy, with a as their ratio. 6. Possible relationshipsbetween agonist receptor occupancy and corresponding functional effects. A really enlightening figure, isn’t it. 6 Originally described – with some mathematical overhead – by Strickland and Loeb (PNAS 78:1366-70, 1981). Well worth reading. 7. Theoretical model to illustrate the effect of biochemical cascades on dose-effect relationships.

Voltage-gated channels, in particular, are important for the spreading of action potentials over the surface of an entire cell. In most excitable cells, there are high numbers of voltage-gated channels for both sodium and potassium (and, in fact, several subtypes of both). In addition, voltagegated Ca++ channels prominently occur in heart and smooth muscle cells. 5. Ion channels and the formation of the action potential. In each panel, the lower compartment is the cell interior. a: Na+ and K+ permeability of the cytoplasmic membrane under resting conditions (simplified).

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Biochemical Pharmacology. Lecture Notes by MichaelPalmer


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