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2 Noradrenaline (norepinephrine)

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Pharmaceutical Chemistry
This chapter is in the book Pharmaceutical Chemistry
2 Noradrenaline (norepinephrine)2.1 Goals–To introduce the reader to the concept of false neurotransmitter–To introduce the reader to the concept of structure–activity correlation as a toolfor designing new drugs (responseβversusα, size of the substituents on the ni-trogen atom, etc., from norepinephrine)–To introduce the reader to antihypertensive drugs, peripheral vasodilators, etc.2.2 IntroductionAs indicated in the previous chapter, the ANS is divided into:1. Cholinergic nerves (releasing ACh in their synapses), which cover all the pregangli-onic, parasympathetic postganglionic, and some sympathetic postganglionic fibers,such as those innervating the sweat glands and certain peripheral blood vessels.2. Adrenergic nerves, in which the mediating action was attributed for a long timeto adrenaline (A), secretion of the adrenal medulla, to which Barger and Dale as-signed sympathomimetic properties in 1910. It is now known that the neurotrans-mitter is noradrenaline (NA), also known as norepinephrine. It covers only thepostganglionic sympathetic fibers.2.3 Adrenergic synapsesThe sympathetic postganglionic nerve endings branch at their end and come into con-tact with the effector organ (smooth muscle, in general) through a series of varicosi-ties (Fig. 2.1).We can mimic or block the NA action at different levels:(1) Biosynthesis(2) Release(3) Storage in vesicles(4) Acting on receptors(5) Metabolism (inactivation) by monoamine oxidase (MAO) and catechol-O-methyl-transferase (COMT) enzymes(6) Reuptakehttps://doi.org/10.1515/9783111316888-002
© 2024 Walter de Gruyter GmbH, Berlin/Boston

2 Noradrenaline (norepinephrine)2.1 Goals–To introduce the reader to the concept of false neurotransmitter–To introduce the reader to the concept of structure–activity correlation as a toolfor designing new drugs (responseβversusα, size of the substituents on the ni-trogen atom, etc., from norepinephrine)–To introduce the reader to antihypertensive drugs, peripheral vasodilators, etc.2.2 IntroductionAs indicated in the previous chapter, the ANS is divided into:1. Cholinergic nerves (releasing ACh in their synapses), which cover all the pregangli-onic, parasympathetic postganglionic, and some sympathetic postganglionic fibers,such as those innervating the sweat glands and certain peripheral blood vessels.2. Adrenergic nerves, in which the mediating action was attributed for a long timeto adrenaline (A), secretion of the adrenal medulla, to which Barger and Dale as-signed sympathomimetic properties in 1910. It is now known that the neurotrans-mitter is noradrenaline (NA), also known as norepinephrine. It covers only thepostganglionic sympathetic fibers.2.3 Adrenergic synapsesThe sympathetic postganglionic nerve endings branch at their end and come into con-tact with the effector organ (smooth muscle, in general) through a series of varicosi-ties (Fig. 2.1).We can mimic or block the NA action at different levels:(1) Biosynthesis(2) Release(3) Storage in vesicles(4) Acting on receptors(5) Metabolism (inactivation) by monoamine oxidase (MAO) and catechol-O-methyl-transferase (COMT) enzymes(6) Reuptakehttps://doi.org/10.1515/9783111316888-002
© 2024 Walter de Gruyter GmbH, Berlin/Boston

Chapters in this book

  1. Frontmatter I
  2. Preface to the first edition VII
  3. Preface to the second edition XIII
  4. Contents XV
  5. About the author XXIII
  6. 1 Acetylcholine 1
  7. 2 Noradrenaline (norepinephrine) 37
  8. 3 Dopamine 63
  9. 4 Serotonin and reuptake inhibitors of biogenic amines 83
  10. 5 Amino acid neurotransmitters 97
  11. 6 Peptides as neurotransmitters: narcotic analgesics 115
  12. 7 Histamine and antihistamines 141
  13. 8 Enzymatic inhibitors I 175
  14. 9 Enzymatic inhibitors II 185
  15. 10 Design of drugs acting on transport through biological membranes 200
  16. 11 Enzymatic inhibition: inhibitors of the biosynthesis of the cellular wall 212
  17. 12 Enzymatic inhibition: other antibacterial agents 239
  18. 13 Enzymatic inhibition: inhibitors of biosynthesis of nitrogenous bases 259
  19. Index 277
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https://doi.org/10.1515/9783111316888-002

Chapters in this book

  1. Frontmatter I
  2. Preface to the first edition VII
  3. Preface to the second edition XIII
  4. Contents XV
  5. About the author XXIII
  6. 1 Acetylcholine 1
  7. 2 Noradrenaline (norepinephrine) 37
  8. 3 Dopamine 63
  9. 4 Serotonin and reuptake inhibitors of biogenic amines 83
  10. 5 Amino acid neurotransmitters 97
  11. 6 Peptides as neurotransmitters: narcotic analgesics 115
  12. 7 Histamine and antihistamines 141
  13. 8 Enzymatic inhibitors I 175
  14. 9 Enzymatic inhibitors II 185
  15. 10 Design of drugs acting on transport through biological membranes 200
  16. 11 Enzymatic inhibition: inhibitors of the biosynthesis of the cellular wall 212
  17. 12 Enzymatic inhibition: other antibacterial agents 239
  18. 13 Enzymatic inhibition: inhibitors of biosynthesis of nitrogenous bases 259
  19. Index 277
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