Linked Life Data

2822899

Source:http://linkedlifedata.com/resource/pubmed/id/2822899

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1987-12-9
pubmed:abstractText
The possibility that the kappa agonists, U50,488H, ethylketazocine and tifluadom, might act as opioid antagonists was studied using the inhibition of the anesthetized rat micturition reflex in vivo as a pharmacological endpoint. Intracerebroventricular administration of equieffective doses of the mu agonists [D-Ala2, NMePhe4, Gly-ol]enkephalin (0.01 nmol), [N-MePhe3, D-Pro4]enkephalin (0.03 nmol), morphine (0.08 nmol), normorphine (0.3 nmol), sufentanil (0.002 nmol), etorphine (0.004 nmol), phenazocine (17 nmol) and meperidine (176 nmol) inhibited spontaneous bladder contractions for a duration of approximately 20 to 30 min. Similarly, i.c.v. administration of the delta-selective agonist (D-Pen2, D-Pen5]enkephalin (15 nmol) inhibited the micturition reflex for approximately the same duration. The kappa agonists U50,488H (22 nmol), ethylketazocine (3 nmol) and tifluadom (3 nmol) did not alter bladder activity after i.c.v. administration. Higher doses of ethylketazocine (10 nmol) or tifluadom (20 nmol), but not U50,488H, produced consistent suppression of bladder contractions. Pretreatment of rats (-15 min, i.c.v.) with doses of U50,488H, ethylketazocine or tifluadom which did not produce an agonist effect consistently blocked the inhibitory actions of the mu agonists morphine and normorphine on bladder motility, but failed to antagonize the similar actions of the mu agonists [D-Ala2, NMePhe4, Gly-ol]enkephalin, [N-MePhe3, D-Pro4]enkephalin, phenazocine, meperidine or those of the delta agonist [D-Pen2, D-Pen5]enkephalin. Centrally initiated bladder effects of the mu agonists etorphine and sufentanil were antagonized by U50,488H but unaffected by ethylketazocine or tifluadom. In addition, administration of U50,488H (i.c.v.) during a morphine-induced bladder shutdown resulted in either an immediate recovery of bladder activity or a shortened duration of action.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/3,4-Dichloro-N-methyl-N-(2-(1-pyrrol..., http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepines, http://linkedlifedata.com/resource/pubmed/chemical/Cyclazocine, http://linkedlifedata.com/resource/pubmed/chemical/Ethylketocyclazocine, http://linkedlifedata.com/resource/pubmed/chemical/Morphine, http://linkedlifedata.com/resource/pubmed/chemical/Morphine Derivatives, http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu, http://linkedlifedata.com/resource/pubmed/chemical/tifluadom
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
243
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
234-40
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Mu antagonist properties of kappa agonists in a model of rat urinary bladder motility in vivo.
pubmed:affiliation
Department of Pharmacology, University of Arizona Health Sciences Center, Tucson.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.