l20_rcep_cas_sdy

l20_rcep_cas_sdy - 20.201 Lecture #20 11/7/05 Page 1 20.201...

Info iconThis preview shows pages 1–6. Sign up to view the full content.

View Full Document Right Arrow Icon
20. 201 Lecture # 20 11/7/05 Page 1 Lecture # 20 : Omeprazole Case Study November 7, 2005 20. 201 Mechanisms of Drug Action
Background image of page 1

Info iconThis preview has intentionally blurred sections. Sign up to view the full version.

View Full DocumentRight Arrow Icon
Review of Lecture #1 9 • Covered the concepts of PBPK’s • Constructed a PBPK model based on cisplatin Today • Brief lecture on receptors and drug-receptor interactions • Begin omeprazole case study
Background image of page 2
20. 201 Lecture # 20 11/7/05 Page 3 Drug-receptor interactions Pharmacodynamics - Quantitative relationship between drug binding to a receptor and the pharmacological effect Definition of a receptor - Cellular macromolecule that specifically (chemically) recognizes a ligand and carries out a function in response to ligand binding. Limitations: Fat cells are not receptors for lipophilic drugs: no specific function follows • Receptors provide means to "amplify" drug ~ Example: 70 μg sufentanil causes respiratory arrest ~ 1 billionth the mass of 70 kg adult Types of receptors - Trans membrane ion channels: conduct ions across membrane in response to ligand binding, voltage gradient or second messenger; e.g., H + /K + -ATP’ase - Transmembrane linked to intracellular G protein; e.g., adrenergic receptors - Transmembrane with enzymatic cytosolic domain; e.g., receptor tyrosine kinases - Intracellular: cytoplasm or nucleus; e.g., DNA, estrogen receptor • Drugs not acting through “receptors” - ethanol (?) - general anesthetics -antac ids
Background image of page 3

Info iconThis preview has intentionally blurred sections. Sign up to view the full version.

View Full DocumentRight Arrow Icon
20 .201 Lecture # 20 11/7/05 Page 4 • Trans membrane ion channels: ~ conduct ions across membrane in response to ligand binding, voltage gradient or second messenger ~ e.g., H + /K + -ATP’ase • Transmembrane linked to intracellular G protein; e.g., adrenergic receptors •Transmembrane with enzymatic cytosolic domain; e.g., receptor tyrosine kinases • Intracellular: cytoplasm or nucleus; e.g., DNA, estrogen receptor Types of receptors Agonist Agonist Agonist Agonist Na Na Activation of conductance G-protein activation Phosphorylation of tyrosines on key signaling molecules Transport to the nucleus Activation of transcription and translation Activation of cell signaling Generation of second messenger Activation of cell signaling 1 2 3 4 Figure by MIT OCW.
Background image of page 4
20 .201 Lecture # 20 11/7/05 Page 5 Characteristics of a Receptor
Background image of page 5

Info iconThis preview has intentionally blurred sections. Sign up to view the full version.

View Full DocumentRight Arrow Icon
Image of page 6
This is the end of the preview. Sign up to access the rest of the document.

Page1 / 16

l20_rcep_cas_sdy - 20.201 Lecture #20 11/7/05 Page 1 20.201...

This preview shows document pages 1 - 6. Sign up to view the full document.

View Full Document Right Arrow Icon
Ask a homework question - tutors are online