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Lectures 2-3
Drug Targets
(Receptors)
DOSE
DRUG IN
TISSUES
DRUG IN
SYSTEMIC
CIRCULATION
EXCRETION
AND
METABOLISM
ABSORPTION
ELIMINATION
DISTRIBUTION
ADME
• Cell Membrane Lipids
• Proteins
• Receptors
• Enzymes
• Carrier proteins
• Structural proteins
• Nucleic acids
• DNA
• R...
Receptors
Drug-Receptor Interactions
1. Ionic (Electrostatic) Interactions
Drug-Receptor Interactions
Ion-Dipole and Dipole- Dipole Interactions
Drug-Receptor Interactions
Hydrogen Bonds
Drug-Receptor Interactions
Drug-Receptor Interactions
Drug-Receptor Interactions
Drug-Receptor Interactions
Charge-Transfer Hydrophobic Interactions
Drug-Receptor Interactions
π- π stacking Cation- π Interation
Drug-Receptor Interactions
Halogen Bonding
Drug-Receptor Interactions
Constitutive Receptor Activity
Drug-Receptor Interactions
Theories of Drug-Receptor Interactions
• Occupancy Theory
–The intensity of the body’s response to the drug is directly re...
Theories of Drug-Receptor Interactions
• Rate Theory
• Pharmacological response is not dependent on drug-receptor complex
...
Drug-Receptor Interactions
• Two-state (Multi-state) Receptor Model
• R and R* are in equilibrium (equilibrium
constant L)...
Drug Chirality
Conformational Isomers
Conformational Isomers
Diastereomers
Receptor Chirality
Roger A.H. Adan. Nature, Volume 27, Issue 4, 2006, 183–186
Topographical and Stereochemical
Considerations
Topographical and Stereochemical
Considerations
Allosteric Modulators
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Lectures 2 3 (receptors)

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Drug receptor targets

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Lectures 2 3 (receptors)

  1. 1. Lectures 2-3 Drug Targets (Receptors)
  2. 2. DOSE DRUG IN TISSUES DRUG IN SYSTEMIC CIRCULATION EXCRETION AND METABOLISM ABSORPTION ELIMINATION DISTRIBUTION ADME
  3. 3. • Cell Membrane Lipids • Proteins • Receptors • Enzymes • Carrier proteins • Structural proteins • Nucleic acids • DNA • RNA • Carbohydrates • Cell surface carbohydrates • Antigen and recognition molecules Drug Targets Konrad H. Bleicher, Hans-Joachim Böhm, Klaus Müller & Alexander I. Alanine Nature Reviews Drug Discovery 2, 369-378 (May 2003)
  4. 4. Receptors
  5. 5. Drug-Receptor Interactions 1. Ionic (Electrostatic) Interactions
  6. 6. Drug-Receptor Interactions Ion-Dipole and Dipole- Dipole Interactions
  7. 7. Drug-Receptor Interactions Hydrogen Bonds
  8. 8. Drug-Receptor Interactions
  9. 9. Drug-Receptor Interactions
  10. 10. Drug-Receptor Interactions
  11. 11. Drug-Receptor Interactions Charge-Transfer Hydrophobic Interactions
  12. 12. Drug-Receptor Interactions π- π stacking Cation- π Interation
  13. 13. Drug-Receptor Interactions Halogen Bonding
  14. 14. Drug-Receptor Interactions
  15. 15. Constitutive Receptor Activity
  16. 16. Drug-Receptor Interactions
  17. 17. Theories of Drug-Receptor Interactions • Occupancy Theory –The intensity of the body’s response to the drug is directly related to the number of receptors occupied by the drug. –The maximum response occurs when all of the receptors have drug molecules attached.
  18. 18. Theories of Drug-Receptor Interactions • Rate Theory • Pharmacological response is not dependent on drug-receptor complex concentration but rather depends upon rate of association of drug and receptor.
  19. 19. Drug-Receptor Interactions • Two-state (Multi-state) Receptor Model • R and R* are in equilibrium (equilibrium constant L), which defines the basal activity of the receptor. • Full agonists bind only to R* • Partial agonists bind preferentially to R* • Full inverse agonists bind only to R • Partial inverse agonists bind preferentially to R • Antagonists have equal affinities for both R and R* (no effect on basal activity) • In the multi-state model there is more than one R state to account for variable agonist and inverse agonist behavior for the same receptor type.
  20. 20. Drug Chirality
  21. 21. Conformational Isomers
  22. 22. Conformational Isomers
  23. 23. Diastereomers
  24. 24. Receptor Chirality Roger A.H. Adan. Nature, Volume 27, Issue 4, 2006, 183–186
  25. 25. Topographical and Stereochemical Considerations
  26. 26. Topographical and Stereochemical Considerations
  27. 27. Allosteric Modulators

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