Linked Life Data

7903535

Source:http://linkedlifedata.com/resource/pubmed/id/7903535

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
1994-1-24
pubmed:abstractText
The alpha 2-adrenergic receptor-mediated stimulation of GTPase activity was investigated in human platelet membranes. The stimulatory effect of (-)-epinephrine was strictly dependent on Mg2+ and derived from a high-affinity GTPase activation. (-)-Epinephrine and (-)-norepinephrine stimulated GTPase activity in a concentration-dependent manner with EC50 values of 200 and 600 nM, respectively. These effects were stereospecific, since (+/-)-epinephrine, (+/-)-norepinephrine, and (+)-epinephrine were less potent in stimulating the enzyme activity with EC50 values of 4, 1 and 3 microM, respectively. Thrombin also stimulated GTPase activity concentration dependently with an EC50 value of 0.02 U/mL. The maximal effects of (-)-epinephrine, (-)-norepinephrine, and thrombin were not additive in any combination. Clonidine did not stimulate GTPase activity, whereas another synthetic alpha 2-adrenergic agonist, p-aminoclonidine, had the characteristics of a partial agonist. The rank order of potency for antagonists to inhibit the activation of GTPase by 1 microM (-)-epinephrine was yohimbine = rauwolscine > idazoxan = oxymetazoline = phentolamine = WB4101 = (+)-mianserin > (-)-mianserin > prazosin > (-)-propranolol. Negative logarithms of the IC50 values of these antagonists corresponded well with the negative logarithmic values of Ki(pKi) for the alpha 2A-adrenergic receptors determined by a receptor-binding technique in human platelets. These results indicate that epinephrine stimulates high-affinity GTPase activity of G proteins (putatively Gi2), which are also coupled with thrombin receptors, in a Mg(2+)-dependent and stereospecific manner, via alpha 2A-adrenergic receptor activation in human platelet membrane preparations.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
3
pubmed:volume
46
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2021-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1993
pubmed:articleTitle
Pharmacological characterization of epinephrine-stimulated GTPase activity in human platelet membranes.
pubmed:affiliation
Department of Psychiatry and Neurology, Hokkaido University School of Medicine, Sapporo, Japan.
pubmed:publicationType
Journal Article, Comparative Study