MolPharm xPharm- The Comprehensive Pharmacology Reference

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 ZHELYASKOV, D. K.
Right arrow Articles by UDENFRIEND, S.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by ZHELYASKOV, D. K.
Right arrow Articles by UDENFRIEND, S.

Molecular Pharmacology, Vol 4, 445-451, Copyright © 1968 by the American Society for Pharmacology and Experimental Therapeutics

Tryptophan Derivatives as Inhibitors of Tyrosine Hydroxylase in Vivo and in Vitro

DELTCHO K. ZHELYASKOV 1, MORTON LEVITT 1, and SIDNEY UDENFRIEND 1

1 Laboratory of Clinical Biochemistry, National Heart Institute, National Institutes of Health, Bethesda, Maryland 20014

Certain typtophan analogs were found to be potent inhibitors of tyrosine hydroxylase and to act by a mechanism that is not competitive with substrate. The most active compounds in these studies were those with a hydroxyl group at the 5 position on the indole ring. The most potent inhibitor was agr-methyl-5-hydroxytryptophan. Amines or acids resulting from metabolism of the parent compounds were found to be inactive. Tyrosine hydroxylase activity was inhibited in vivo after a 50 mg/kg dose of agr-methyl-5-hydroxytryptophan; a single dose of 200 mg/kg inhibited the enzyme up to 48 hr. Administration of this compound resulted in depletion of tissue stores of catecholamines as well as in sedation.

Submitted on February 2, 1968




This article has been cited by other articles:


Home page
 ScienceHome page
G. Stefano, E Catapane, and E Aiello
Dopaminergic agents: influence on serotonin in the molluscan nervous system
Science, October 29, 1976; 194(4264): 539 - 541.
[Abstract] [PDF]


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

Copyright © 1968 by the American Society for Pharmacology and Experimental Therapeutics