PHRM 623 Fundamentals of Pharmacology

Time:                       Monday, Tuesday, Wednesday, and Thursday, 4:00–5:00 P.M.

Location:                 Pharmacology Seminar Room, M100 John Morgan

Course Director:    David Manning (8-1775; manning@pharm.med.upenn.edu)

Starting Date:         September 6, 2007

Thu          9/6                    Introduction to the Course: Targets of                  Manning

                                               Drug Action

Mon         9/10           1.    Signaling:  An Overview                                        Manning

Tue          9/11           2.    G Protein-coupled Receptors                               Manning

Wed        9/12           3.    G Proteins                                                               Manning

Thu          9/13           4     Dose-response Relationships                              Manning

Mon         9/17           5.    GPCRs: Ternary Complex Models                      Manning

Tue          9/18           6.    Analysis of Radioligand Binding                          Manning

Wed        9/19           7.    Agonist-induced Desensitization                         Manning

Thu          9/20           8.    Selected Reading(s): GPCRs as Drug               Manning
                                               Targets

Mon         9/24           9.    Problem Set Due                                                   Manning

Tue          9/25         10.    Enzyme-linked Receptors I                                   Field

Wed        9/26         11.    Enzyme-linked Receptors II                                  Field

Thu          9/27         12.    Enzyme-linked Receptors III                                  Field

Mon         10/1         13.    Protein-Protein Interaction Motifs                         Field

Tue          10/2         14.    Selected Reading(s): Enzyme-linked                  Field

                                               Receptors as Drug Targets                            

Wed        10/3         15.    Problem Set Due                                                   Field

Thu          10/4                  Review: Manning and Field

Mon         10/8                  TEST: 1-15

Tue          10/9         16.    Arachidonic Acid Metabolites                              Smyth

Wed        10/10       17.    Arachidonic Acid Metabolites                              Smyth

Thu          10/11       18.    Arachidonic Acid Metabolites                              Smyth

Mon         10/15       19.    Selected Reading(s): Arachidonic Acid              Smyth

                                             Metabolism as a Drug Target

Tue          10/16       20.    Problem Set Due                                                   Smyth

Wed        10/17       21.    Membrane Electric Potential                                Lindstrom

Thu          10/18       22.    Action Potential and Conduction                          Lindstrom

Mon         10/22       23.    Voltage-gated Ion Channel Structure                   Lindstrom
                                               and Pharmacology

Tue          10/23       24.    Synaptic Transmission and Ligand-gated          Lindstrom

                                               Ion Channels

Wed        10/24       25.    Ligand-gated Ion Channel Structure and             Lindstrom

                                               Pharmacology

Thu          10/25       26.    Selected Reading(s): Conduction as                  Lindstrom
                                               a Drug Target

Mon         10/29       27.    Problem Set Due                                                   Lindstrom

Tue          10/30                Review: Smyth and Lindstrom

Wed        10/31                TEST: 16-27

Thu          11/01                No Class (GGPS Symposium)

Mon         11/05       28.    Michaelis-Menten Kinetics                                    Penning

Tue          11/06       29.    Reversible Inhibitors as Drugs                             Penning

Wed        11/07       30.    Reversible Inhibitors as Drugs                             Penning

Thu          11/08       31.    Bisubstrate Kinetics                                              Penning

Mon         11/12       32.    Transition State Analogs and Tight                      Penning
                                             Binding Inhibitors

Tue          11/13       33.    Irreversible Inhibitors as Drugs                             Penning

Wed        11/14       34.    Suicide Substrates as Drugs                               Penning

Thu          11/15       35.    Selected Reading(s)                                             Penning

Mon         11/19       36.    Eukaryotic Transcription Activators I                   Kaestner

Tue          11/20       37.    Eukaryotic Transcription Activators II                   Kaestner

                                 38.*  Problem Set Due                                                   Penning

Wed        11/21                No Class

Thu          11/22                No Class

Mon         11/26       39.    Regulation of Transcription: Steroids and           Lazar
                                               PPARs

Tue          11/27       40.    Selected Reading(s): Transcription as                Kaestner
                                               a Drug Target

Wed        11/28       41.    Review: Penning and Kaestner

Thu          11/29                No class

Mon         12/3         42.    Integrins I                                                                 Bennett

Tue          12/4         43.    Integrins II                                                                Bennett

Wed        12/5                  No Class

Thu          12/6                  TEST: 28-43

*Class time extended to 6 pm.