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Receptor :
Protein macromolecules on cell surface or cytoplasm
Affinity :
Capability of drug to bind to receptor
Intrinsic activity :
Ability of drug to elicit response after binding to
receptor
Agonist
High affinity and high IA
Antagonist
High affinity and IA absent
Partial agonist
High affinity and low IA
Inverse agonist
Produce effect opposite to agonist
1. Ion channel receptor
2. G- protein coupled receptor (Metabotropic)
3. Kinase linked receptor
4. Intra cellular receptors
Present on cell membrane
Coupled to an ion channel
Open when receptor occupied by agonist
Eg : Benzodiazepine
Receptor bound to effector system through GTP binding
protein
G protein- α,β, Subunits
Effector mechanisms
Adenylate cyclase
Phospholipase C
Ion channel
Types- Gs, Gi
Eg. Adrenergic drugs
Receptor directly linked to tyrosine kinase
Autophosphorylation
Eg, Insulin
Located in cytoplasm
Alteration in gene transcription
Eg : steroid hormone
Desentisation
After reaching high level response decreases over time
Reversible
Up regulation
Prolonged exposure to high concentration of agonist
causes reduction in number of receptors
Down regulation
Prolonged exposure to high concentration of antagonist
causes increase in number of receptors
Spare receptors
Unoccupied receptors serving as reserve
Receptor related diseases
Diabetes
Myasthenia gravis
Familial hypercholesterolemia
Receptor Types, Mechanisms, and Concepts

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Receptor Types, Mechanisms, and Concepts

  • 1.
  • 2. Receptor : Protein macromolecules on cell surface or cytoplasm Affinity : Capability of drug to bind to receptor Intrinsic activity : Ability of drug to elicit response after binding to receptor
  • 3. Agonist High affinity and high IA Antagonist High affinity and IA absent Partial agonist High affinity and low IA Inverse agonist Produce effect opposite to agonist
  • 4. 1. Ion channel receptor 2. G- protein coupled receptor (Metabotropic) 3. Kinase linked receptor 4. Intra cellular receptors
  • 5. Present on cell membrane Coupled to an ion channel Open when receptor occupied by agonist Eg : Benzodiazepine
  • 6. Receptor bound to effector system through GTP binding protein G protein- α,β, Subunits Effector mechanisms Adenylate cyclase Phospholipase C Ion channel Types- Gs, Gi Eg. Adrenergic drugs
  • 7. Receptor directly linked to tyrosine kinase Autophosphorylation Eg, Insulin
  • 8. Located in cytoplasm Alteration in gene transcription Eg : steroid hormone
  • 9. Desentisation After reaching high level response decreases over time Reversible Up regulation Prolonged exposure to high concentration of agonist causes reduction in number of receptors Down regulation Prolonged exposure to high concentration of antagonist causes increase in number of receptors
  • 10. Spare receptors Unoccupied receptors serving as reserve Receptor related diseases Diabetes Myasthenia gravis Familial hypercholesterolemia