Linked Life Data

7781714

Source:http://linkedlifedata.com/resource/pubmed/id/7781714

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1995-7-14
pubmed:abstractText
The alpha 1-adrenoceptor subtype present in human liver membranes was studied using radioligand binding techniques. [3H]Prazosin binding was rapid, saturable and reversible. A kinetically derived Kd of 0.22 nM was obtained. Rosenthal analysis of saturation isotherms indicated a single class of binding sites with a Kd of 0.47 nM and a Bmax of 70 fmol/mg of protein. Membrane preincubation with chloroethylclonidine markedly decreased total binding (62% decrease) without altering the Kd for the radioligand. Binding competition experiments were performed and the order of potency for agonists was: oxymetazoline > epinephrine > or = norepinephrine > methoxamine. The binding affinity for epinephrine was modulated by the GTP analogue guanosine-5'-(beta,gamma-imido)triphosphate. For antagonists the potency order was: WB4101 > or = prazosin > or = (+)-niguldipine = 5-methylurapidil > or = benoxathian > or = phentolamine. The pharmacological profile of the [3H]prazosin binding sites of human liver membranes suggests that alpha 1A-adrenoceptors predominate (75%-85% of the alpha 1-adrenoceptors) in this tissue.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
289
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
81-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
Characterization of the human liver alpha 1-adrenoceptors: predominance of the alpha 1A subtype.
pubmed:affiliation
Departamento de Bioenergética, Universidad Nacional Autónoma de México, México, D.F.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't