11777 - Medicinal and Toxicological Chemistry 2

Academic Year 2011/2012

  • Teaching Mode: Traditional lectures
  • Campus: Bologna
  • Corso: First cycle degree programme (L) in Applied Pharmaceutical Sciences (cod. 0914)

Course contents

Drugs Affecting Cholinergic Neurotrasmission.

Acetylcholine neurochemistry. Characterization of acetylcholine receptors.

Nicotinic agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Nicotinic antagonists. Neuromuscolar Blocking Agents. Muscarinic agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Acethylcholinesterase inhibitors. Mechanism of action. Structure-activity Relationships. Muscarinic antagonists. Mechanism of action. Structure-activity Relationships.

Drugs Affecting Adrenergic Neurotrasmission.

Biosynthesis, metabolism and function of norepinephrine and epinephrine. Characterization of adrenergic receptor subtypes. Therapeutic relevance of adrenergic receptor subtypes.

alpha1 and alpha2-adrenergic Agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. alpha-adrenergic Antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. Drugs affecting catecholamine biosynthesis, storage, reuptake and metabolism. Therapeutic application. Mechanism of action. Structure-activity Relationships. beta-adrenergic Agonists. Therapeutic application. Mechanism of action. Structure-activity Relationships. beta-adrenergic Antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships.

Drugs Affecting Dopaminergic Neurotrasmission.

Biosynthesis, metabolism and function of dopamine. Characterization of dopaminergic receptors. Therapeutic relevance of dopaminergic receptors.

Dopaminergic receptor Agonists. Anti-Parkinson drugs. Mechanism of action. Structure-activity Relationships.   Dopaminergic receptor Antagonists.  Neuroleptics. Mechanism of action. Structure-activity Relationships. 

Drugs Affecting Histamine Neurotrasmission.

Histamine biosynthesis, catabolism and function. Characterization of histamine receptors. H1 receptor antagonists (first and second generation). Therapeutic application. Mechanism of action. Structure-activity Relationships. H2 receptor antagonists (antiulcer agents). Therapeutic application. Mechanism of action. Structure-activity Relationships.

Drugs Acting on Opioid Receptors.

Endogenous opioid peptides. Fisiological functions. Characterization of opioid receptors.

Opioid receptor agonists (analgesics). Therapeutic application. Mechanism of action. Mixed agonist-antagonists. Therapeutic application. Mechanism of action. Structure-activity Relationships.

Drugs Acting on GABAA receptor complex.

Biosynthesis, metabolism and function of gamma-aminobutiric acid. Benzodiazepines (Anxiolytics). Therapeutic application. Mechanism of action. Structure-activity Relationships.

Readings/Bibliography

D. A Williams e T. L. Lemke, Foye's principi di Chimica Farmaceutica, IV Ed. italiana, Ed. Piccin, 2009 (ISBN: 8829920347).
G. L. Patrick, Introduzione alla Chimica Farmaceutica, II Ed. Italiana, Ed. EdiSES, 2010 (ISBN: 8879596632).

Slides and lesson notes

Assessment methods

A comprehensive oral final exam is given at the end of the semester

Teaching tools

Video-projector, PC, slides, Internet

Office hours

See the website of Maria Laura Bolognesi