|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:dateCreated |
1992-7-7
|
|
pubmed:abstractText |
The presynaptic terminal autoreceptors which modulate the release of noradrenaline through a negative feed-back mechanism correspond to the alpha 2-subtype of adrenoceptors. These receptors are also present post-synaptically in the pancreatic islets were they mediate inhibition of the glucose-induced release of insulin. The sympathetic innervation of the pancreatic islets involves alpha 2-adrenoceptors both presynaptically as well as postsynaptically. SL 84.0418 is a novel alpha 2-adrenoceptor antagonist with preferential effects in the periphery and with at least a 10-fold higher selectivity ratio between alpha 2 and alpha 1-adrenoceptors when compared with idazoxan. SL 84.0418 antagonizes the hyperglycemia and the inhibition of insulin release induced by the alpha 2-adrenoceptor agonist UK 14304. The administration of SL 84.0418 significantly reduces the glucose evoked hyperglycemia in several species including man. It is proposed that SL 84.0418 may represent a useful and novel hypoglycemic drug in the treatment of type II diabetes.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Azepines,
http://linkedlifedata.com/resource/pubmed/chemical/B-HT 933,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxanes,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoglycemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Idazoxan,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Insulin,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha
|
|
pubmed:status |
MEDLINE
|
|
pubmed:issn |
0303-6995
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:volume |
34
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
171-7
|
|
pubmed:dateRevised |
2011-11-17
|
|
pubmed:meshHeading |
pubmed-meshheading:1687782-Adrenergic alpha-Agonists,
pubmed-meshheading:1687782-Adrenergic alpha-Antagonists,
pubmed-meshheading:1687782-Animals,
pubmed-meshheading:1687782-Azepines,
pubmed-meshheading:1687782-Dioxanes,
pubmed-meshheading:1687782-Dogs,
pubmed-meshheading:1687782-Hyperglycemia,
pubmed-meshheading:1687782-Hypoglycemic Agents,
pubmed-meshheading:1687782-Hypothalamus,
pubmed-meshheading:1687782-Idazoxan,
pubmed-meshheading:1687782-Indoles,
pubmed-meshheading:1687782-Insulin,
pubmed-meshheading:1687782-Islets of Langerhans,
pubmed-meshheading:1687782-Male,
pubmed-meshheading:1687782-Muscle, Smooth,
pubmed-meshheading:1687782-Muscle, Smooth, Vascular,
pubmed-meshheading:1687782-Muscle Contraction,
pubmed-meshheading:1687782-Norepinephrine,
pubmed-meshheading:1687782-Pyrroles,
pubmed-meshheading:1687782-Rats,
pubmed-meshheading:1687782-Receptors, Adrenergic, alpha,
pubmed-meshheading:1687782-Synapses
|
|
pubmed:year |
1991
|
|
pubmed:articleTitle |
Pre- and postsynaptic alpha-2 adrenoceptors as target for drug discovery.
|
|
pubmed:affiliation |
Department of Biology, Synthélabo Recherche (LERS), Paris, France.
|
|
pubmed:publicationType |
Journal Article,
In Vitro
|
