Linked Life Data

9774494

Source:http://linkedlifedata.com/resource/pubmed/id/9774494

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1998-11-20
pubmed:abstractText
The secretory, biosynthetic and cationic effects of a novel insulinotropic agent with an imidazoline structure, 2-(N-phenyl-indoyl)imidazole hydrochloride (RX 871024) was investigated in rat pancreatic islets. In the 1.0-10-microM range, this agent augmented, in a concentration-related manner, the release of insulin from islets incubated at intermediate concentrations of d-glucose (4.0-7.0 mm), this enhancing action fading out at both lower a nd higher d-glucose levels. When the concentration of RX 871024 was raised to 1.0 mm, severe inhibition of glucose-stimulated insulin output was observed. The imidazole derivative (10 microM) failed to enhance glucose-stimulated biosynthetic activity in islets exposed to l-[4-3H]phenylalanine; a modest inhibition of the islet peptide tritiation was even recorded at 4.0 mm d-glucose. The positive insulinotropic action of RX 871024 (10 microM) coincided with a decrease in 45Ca net uptake, unchanged outflow of 86Rb and stimulation of 45Ca efflux from prelabelled islets, the latter effect being only partially suppressed in the absence of extracellular Ca2+. These findings suggest a multifactorial mode of action of RX 871024 in islet cells, with emphasis on both an apparent stimulation of Ca2+ influx and, independently of this effect, an intracellular redistribution of the divalent cation. The imidazole compound is proposed, therefore, to display suitable attributes to bypass site-specific defects of d-glucose metabolism in the B-cell of non-insulin-dependent diabetic patients.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
1043-6618
pubmed:author
pubmed:copyrightInfo
Copyright 1998 The Italian Pharmacological Society
pubmed:issnType
Print
pubmed:volume
38
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
305-10
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
1998
pubmed:articleTitle
Secretory, biosynthetic and cationic responses to 2-(N-PHENYL-INDOYL)IMIDAZOLE in rat pancreatic islets.
pubmed:affiliation
Laboratory of Experimental Medicine, Brussels Free University, 808 Route de Lennik, Brussels, B-1070, Belgium.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't