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ADRB1 and Its Pharmaceutical Ligands

A PChem Finals Presentation (Warning: May cause motion sickness~)

Michael Hwang

on 9 March 2013

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Transcript of ADRB1 and Its Pharmaceutical Ligands

ADRB1 and 3 of Its Pharmaceutical Ligands- A Comparison Karen Cham
Michael Hwang
Sophie Xia The Beta-1 Adrenergic Receptor It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein. Beta-2 Adrenoreceptor 3 Pharmaceutical Ligands of ADRB1 ADRB1 Overview ADRB1 Overview After Ligand Binding 3 Pharmaceutical Ligands of ADRB1 Binding Mechanisms References & Acknowledgments Background courtesy of Wi6791lly of DeviantArt.com <http://wi6791lly.deviantart.com/>
Golan, David E (editor). “Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy”, 2nd edition. LWW: 2008.
Katzung, B. “Basic & Clinical Pharmacology”, 10th Edition. Mc Graw Hill Medical: 2007
Harvey, Richard; Champe, Pamela (series editors). “Lippincott illustrated reviews: Pharmacology”, 4th edition. LWW: 2009
http://download.springer.com/static/pdf/521/art%253A10.1007%252FBF00515556.pdf?auth66=1363945271_592810483186b7e7e302374ad20b77ed&ext=.pdf http://books.google.com/books?hl=en&lr=&id=dUNfJmllmqwC&oi=fnd&pg=PA233&dq=pindolol+state+functions+gibbs+free+energy&ots=cSsO7j9YXE&sig=8vwuAyY53U_fJaZj8VUuiEmeGFU#v=onepage&q=pindolol&f=false
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=33624#x29 ADRB1 changes conformation
Gs protein then activates adenylate cyclase,producing cAMP
cAMP activates the cAMP dependent pathway
Increase heart rate and stroke volume It is located in the cell membrane as a multi-pass protein. Pindolol Timolol Isoprenaline Location: Lungs, GI tract, skeletal muscle, liver, blood vessels Like ADRB1, it is a G-protein coupled receptor embedded in cell membrane Binding leads to relaxation of smooth muscles PK/PD Drug Interactions Timolol Pindolol Isoprenaline CYP 1A1 Inhibitor
APAP, Caffeine, Nicotine
Tamoxifen, Warfarin
Monoamine Oxidase
Catechol-O-methyl transferase
ADRB1/ADRB2 agonist
tachyarrhythmia, coronary arteriosclerosis CYP 2D6
Acetaminophen, Atenolol
Carvedilol, Celecoxib
CYP 2C19
Amoxicillin, Atoravastatin
Diazepam, Ibuprofen
ADRB1/ADRB2 antagonist
bradyarrhythmia, heart failure, hypotension CYP 2D6
Acetaminophen, Atenolol
Carvedilol, Celecoxib
ADRB1/ADRB2 antagonist
edema, heart failure Timolol Pindolol Isoprenaline The isopropyl amine group in isoprenaline makes it selective for β receptors β receptors have a large lipophilic binding pocket adjacent to the amine binding aspartic acid.
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