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Relative Pharmacodynamic Potency of Selected Enantiomers: Compound Relative Activity Biological Response

The document summarizes data on the relative pharmacodynamic potency of selected enantiomers. It shows that for several compounds, such as terbutaline, propranolol, and pindolol, one enantiomer is significantly more potent than the other in producing specific biological responses, with relative activity ratios ranging from 100:1 to 3000:1. The data is from two sources and demonstrates that enantiomers can differ substantially in their pharmacological effects.

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49 views4 pages

Relative Pharmacodynamic Potency of Selected Enantiomers: Compound Relative Activity Biological Response

The document summarizes data on the relative pharmacodynamic potency of selected enantiomers. It shows that for several compounds, such as terbutaline, propranolol, and pindolol, one enantiomer is significantly more potent than the other in producing specific biological responses, with relative activity ratios ranging from 100:1 to 3000:1. The data is from two sources and demonstrates that enantiomers can differ substantially in their pharmacological effects.

Uploaded by

Christina
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Relative Pharmacodynamic Potency of Selected

Enantiomers

Compound Relative Activity Biological Response

terbutaline - > + (3000:1) trachea relaxation


propranolol S > R (100:1) block tachycardia
pindolol - > + (200:1) inhibit tachycardia
methadone - > + (3:1) respiratory depression
ketamine S > R (4:1) anesthesia
tocainide R > S (3:1) antiarrhythmic
flecainide +=- antiarrhythmic
propafenone +=- antiarrhythmic
disopyramide S>R antiarrhythmic
disopyramide S>R anticholinergic
warfarin S > R (8:1) anticoagulant
verapamil - > + (5-18:1) block AV conduction

Data from: Jamali F, et al. J Pharm Sci 78:695, 1989.


1
From: Olbe et al, Nat Rev Drug Discovery 2:132, 2003 2
Different actions of R,S-enantiomer (1)
Different actions of R,S-enantiomer (2)

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