PL EN


Preferences help
enabled [disable] Abstract
Number of results
1993 | 45 | 1 | 83-94
Article title

RH analogs with 4-nitro- and 4-N-butyloxycarbonylamino-1-methyl-2-pyrolylcarboxylic acid in position 1. Synthesis and logical properties

Content
Title variants
Languages of publication
EN
Abstracts
EN
Two new analogs of thyrotropin-releasing hormone TRH, obtained by the replacement of the L-pyroglutamic acid residue with 4-nitro- or 4-N-butyloxycarbonylamino-1-methyl-2-pyrolyl-carboxylic acid (analogs 1, 3), and three related derivatives, in which also the L-histidine residue was replaced with L-norvaline (analogs 2, 4) or L-norleucine (analog 5), were synthesized and tested for endocrine and central nervous system (CNS) activity. The replacement of the L-pyroglutamic acid residue with 4-nitro-1-methyl-2-pyrolylcarboxylic acid (analogs 1 and 2) resulted in the separation of the endocrine from the direct CNS activity. The effect of these analogs on the sleeping time rectal temperature and breathing frequency, was either the same or greater than that of TRH. However, neither the correlation between the binding of analogs to TRH receptors in the brain nor their activity on the CNS parameters measured was found. Analogs 3, 4 and 5, containing 4-butyloxycarbonylamino-1-methyl-2-pyrolylcarboxylic acid in place of L-pyroglutamic acid, were inactive.
Year
Volume
45
Issue
1
Pages
83-94
Physical description
References
Document Type
article
Publication order reference
YADDA identifier
bwmeta1.element.element-from-psjc-36e33847-211d-382b-a180-9d96afbaba78
Identifiers
JavaScript is turned off in your web browser. Turn it on to take full advantage of this site, then refresh the page.