JPET Celsis microsomes equal better data

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Benson, W. M.
Right arrow Articles by Randall, L. O.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Benson, W. M.
Right arrow Articles by Randall, L. O.
Journal of Pharmacology And Experimental Therapeutics, Vol. 109, Issue 2, 189-200, 1953
Copyright © 1953 by American Society for Pharmacology and Experimental Therapeutics

COMPARATIVE PHARMACOLOGY OF LEVORPHAN, RACEMORPHAN AND DEXTRORPHAN AND RELATED METHYL ETHERS

Wilbur M. Benson 1, Paul L. Stefko 1, and Lowell O. Randall 1

1 Department of Pharmacology, Hoffmann-La Roche Inc., Nutley 10, New Jersey

1. Analgesic studies on six members of the morphinan series confirmed the fact that levorphan has twice the potency of racemorphan. The methyl ether, levomethorphan, also was found to have twice the activity of its racemate, racemethorphan. These methyl ethers had one-tenth the potency of the corresponding parent compounds. The dextro-rotatory isomers, dextrorphan and dextromethorphan, were found to have negligible, if any, analgesic activity.

2. Acute toxicity tests showed that the levo-rotatory isomers were more toxic than their corresponding racemates. These in turn were more toxic than their dextro-rotatory forms. The methyl ethers were more toxic than the parent compounds. Chronic toxicity studies have been carried out in rats and dogs on the racemates and in rats on levorphan and dextromethorphan.

3. Respiratory studies showed that the depressant characteristics of the racemates were due to the levo-rotatory isomers. The dextro-rotatory forms had little effect.

4. Antitussive studies demonstrated that the levo-rotatory isomers and the racemates were cough inhibitors but only so in doses that produced lethargy, ataxia or sleep. The dextro-rotatory isomers, particularly dextromethorphan, exerted significant antitussive activity without inducing such effects.

5. Levorphan is of interest because it has twice the analgesic potency of racemorphan but is not twice as toxic. Dextromethorphan is of interest because it possesses high antitussive activity without associated analgesia and cerebral depression.

Submitted on May 22, 1953




This article has been cited by other articles:


Home page
 J. Pharmacol. Exp. Ther.Home page
R. N. Pechnick and R. E. Poland
Comparison of the Effects of Dextromethorphan, Dextrorphan, and Levorphanol on the Hypothalamo-Pituitary-Adrenal Axis
J. Pharmacol. Exp. Ther., May 1, 2004; 309(2): 515 - 522.
[Abstract] [Full Text] [PDF]

Home page
 Canadian J. AnesthesiaHome page
A. A. Weinbroum, V. Rudick, G. Paret, and R. Ben-Abraham
The role of dextromethorphan in pain control
Can J Anesth, June 1, 2000; 47(6): 585 - 596.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
V. K. Shukla and S. Lemaire
N-Methyl-D-aspartate Antagonist Activity of alpha - and beta -Sulfallorphans
J. Pharmacol. Exp. Ther., January 1, 1997; 280(1): 357 - 365.
[Abstract] [Full Text]

Home page
 ScienceHome page
E. J. Simon
Inhibition of Bacterial Growth by Drugs of the Morphine Series
Science, May 1, 1964; 144(3618): 543 - 544.
[Abstract] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1953 by the American Society for Pharmacology and Experimental Therapeutics.