Document Detail


Lipophilic peptides: synthesis of lauroyl thyrotropin-releasing hormone and its biological activity.
MedLine Citation:
PMID:  1866381     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Thyrotropin-releasing hormone (TRH) was derivatized by chemical attachment of lauric acid to the N-terminal pyroglutamyl group. The product was confirmed to be more lipophilic than TRH by high-performance liquid chromatography and measurement of partition coefficients. The central nervous system activity and endocrine activity of the lauroyl derivative were only slightly reduced, to 81 and 64% of the parent TRH, respectively. Lipophilic derivatization may be generally applicable to transmembrane delivery of peptides.
Authors:
S Muranishi; A Sakai; K Yamada; M Murakami; K Takada; Y Kiso
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Pharmaceutical research     Volume:  8     ISSN:  0724-8741     ISO Abbreviation:  Pharm. Res.     Publication Date:  1991 May 
Date Detail:
Created Date:  1991-09-09     Completed Date:  1991-09-09     Revised Date:  2005-11-17    
Medline Journal Info:
Nlm Unique ID:  8406521     Medline TA:  Pharm Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  649-52     Citation Subset:  IM    
Affiliation:
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan.
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MeSH Terms
Descriptor/Qualifier:
Amino Acid Sequence
Animals
Male
Mice
Mice, Inbred ICR
Molecular Sequence Data
Rats
Rats, Inbred Strains
Sleep / drug effects
Thyrotropin / secretion
Thyrotropin-Releasing Hormone / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology
Chemical
Reg. No./Substance:
24305-27-9/Thyrotropin-Releasing Hormone; 9002-71-5/Thyrotropin

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