Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1991-9-11
pubmed:abstractText
To examine the relative efficacy of spinally administered alpha-2 adrenergic agonists [dexmedetomidine, clonidine and ST-91 (2-[2,6- diethylphenylamino]-2-imidazole)] on the 52.5 degrees C hot plate in rats, EEDQ (N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline), an irreversible alpha-2 antagonist, was administered intrathecally (in doses of 0, 8.1, 81 and 810 nmol) 24 hr before the administration of these agonists. EEDQ alone results in an acute mild hyperalgesic effect. Intrathecal dexmedetomidine, clonidine and ST-91 result in a dose-dependent increase in the hot plate response latency: ED50 (95% confidence interval) = 13 (2.1-73), 120 (52-310) and 21 (1.3-240) nmol, respectively. Pretreatment with intrathecal EEDQ (8.1-810 nmol) caused a rightward shift of dose-response curve and reduction of maximal effect of alpha-2 agonists used. For example, 24 hr after 81 nmol of EEDQ, the degree of the rightward shift and the depression of slope was ST-91 greater than clonidine greater than dexmedetomidine. Analysis of the double reciprocal plot indicated that at the ED50, intrathecal dexmedetomidine, clonidine and ST-91 required an apparent occupancy of 10, 36 and 30%, respectively. These results suggest that dexmedetomidine has a higher intrinsic efficacy than clonidine or ST-91.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
258
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
438-46
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Relative efficacy of spinal alpha-2 agonists, dexmedetomidine, clonidine and ST-91, determined in vivo by using N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline, an irreversible antagonist.
pubmed:affiliation
Department of Anesthesiology, University of California, San Diego, La Jolla.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't