| Pharmacological studies of neurotensin, several fragments and analogous in the isolated perfused rat heart. | |
| | |
MedLine Citation:
|
PMID: 7418719 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Neurotensin (NT) induced a dose-dependent increase of the coronary perfusion pressure (CPP) in the isolated perfused rat heart. This effect was not modified by pretreating the organ with methysergide (8.5 x 10(-6) M), atropine (3.4 x 10(-6) M), a mixture of phentolamine (3.1 x 10(-6) M) and practolol (1.5 x 10(-5) M), 8-leucine-angiomine (2.9 x 10(-5) M) thus suggesting the existence of specific NT receptors in the coronary vessels of rat. The structure-activity studies performed using several NT fragments and analogues in the isolated perfused rat heart led us to the following conclusions: (1) the minimum structure required for the full expression of the biological activity of NT is H-Arg9-Pro10-Tyr11-Ile12-Leu13-OH; (2) the amino acid Tyr in position 11 appears to play a key role in the process of NT receptor activation. The replacement of Tyr11 with Tyr(Me) gave a compound which inhibits selectively the increase in coronary perfusion pressure induced by NT, but still exhibits some NT-like activity, specially when used in concentrations higher than 10(-6) M. [Tyr(Me)11]NT did not antagonize the stimulant effects of NT in rat stomach strips and guinea pig atria, thus suggesting that the receptors mediating the constrictor effect of NT in coronary vessels of the rat are pharmacologically different from those subserving the stimulant effect of NT in rat stomach strip and guinea pig atria. |
| | |
Authors:
|
R Quirion; F Rioux; D Regoli; S St-Pierre |
Related Documents
:
|
653519 - Metabolism of synthetic human heptadecapeptide gastrin by the isolated perfused rat liver. 462529 - Improved performance of the isolated rat liver when perfused with purified bovine serum... 21787099 - Summation of reinforcement rates when conditioned stimuli are presented in compound. 6793079 - Secretion of lipoproteins, apolipoprotein a-i and apolipoprotein e by isolated and perf... 19173069 - High temporal resolution coupling of low-flow push-pull perfusion to capillary electrop... 6205639 - Structure-function relationships of protoporphyrin-induced liver injury. 4087919 - Antihepatotoxic actions of tannins. 9085259 - Distribution of succinic semialdehyde reductase in rat brain. 8095379 - Defective glucoregulation of brain alpha 2-adrenoceptors in obesity-prone rats. |
Publication Detail:
|
Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
|
Title: European journal of pharmacology Volume: 66 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 1980 Sep |
Date Detail:
|
Created Date: 1980-12-16 Completed Date: 1980-12-16 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: NETHERLANDS |
Other Details:
|
Languages: eng Pagination: 257-66 Citation Subset: IM |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Blood Pressure / drug effects Coronary Circulation / drug effects Drug Interactions Female Heart / drug effects* Male Neurotensin / analogs & derivatives*, pharmacology* Peptide Fragments / pharmacology Rats Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
|
0/Peptide Fragments; 39379-15-2/Neurotensin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: A hand-held calculator program for individualized dosage adjustment of intravenous theophylline in a...
Next Document: Pharmacological properties of two analogues of angiotensin II containing carboranylalanine (Car).