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Introduction: General Principles-Lecture I, slide 1

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  • Chemical Aspects of Drugs
  • Chirality
  • Anesthetic agents administered as racemic mixtures
  • Drug-Receptor Interactions: Binding Forces
  • Henderson-Hasselbalch Equation


  •  Drug Transfer
    • Aqueous diffusion
    • Lipid diffusion
    • Carrier-mediated Transfer
  • Endocytosis/Exocytosis



Drug shape

  • The shape of the drug is an important factor in defining the nature of the drug-receptor interaction.  The three-dimensional shape of the drug is thought to interact with a complementary structural binding region of the receptor, typically a protein.  The specific nature of the interaction defines whether the drug acts as an agonist promoting a change in cellular function or as an antagonist which blocks the receptor usually resulting in no direct biological effect.

    • For example, let's consider acetylcholine or a synthetic analogue bethanechol (Urecholine).  Interaction of these molecules with receptor (nicotinic or muscarinic cholinergic receptor) causes a physiological response -- a decrease in heartbreak for instance.  By contrast, a muscarinic antagonist such as atropine may bind even more tightly than acetylcholine to muscarinic receptor but causes no direct effect.  However, following administration of antagonist a biological response may be observed as a result of receptor blockade.  

      • A clinical example would be bradycardia following acute myocardial infarction.  Bradycardia in this context might be due to excessive parasympathetic (cholinergic) tone and might cause unacceptably low cardiac output or predispose tomore serious arrhythmias.  Administration of atropine, by blocking the muscarinic receptor blunts the action of acetylcholine and accordingly may reverse bradycardia.

  • Now let's consider the specific example,acetylcholine, as the 2D planar structure:

  • On the left side of the molecule note the quaternary (always positively charged) Nitrogen, which is part of the choline component of acetylcholine. The synthesis of acetylcholine proceeds by combination of choline and acetate (as Acetyl-CoA)-see below

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