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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1987-4-2
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pubmed:abstractText |
The effects of N-(cyclopropylmethyl)-19-isopentylnororvinol hydrochloride (M320) on urine excretion by rats were investigated. Further studies, using rabbit isolated vas deferens, investigated its interactions with kappa-opiate receptors. The output of urine for a 2 h period after M320, administered subcutaneously to normally hydrated Long Evans rats, showed a bell-shaped dose-response relationship, the maximum effect occurring after 10 micrograms kg-1. Urinary retention contributed to but did not fully account for the weaker diuresis after high doses. Attenuation of the ascending portion of the dose-response curve to M320 occurred after 1 and 10 mg kg-1 but not 0.1 mg kg-1 of naltrexone intraperitoneally. M320 in low doses (3-10 micrograms kg-1) caused a small but significant increase in sodium excretion. M320 (30 micrograms kg-1) reduced both sodium and potassium excretion. M320 (10 micrograms kg-1 s.c.) did not increase the volume of urine voided in 2 h by Brattleboro rats showing diabetes insipidus, even when urine excretion was reduced to normal by 1 week of vasopressin replacement. The volume of urine voided in 4 h by Brattleboro rats was progressively reduced to zero by M320 (10-100 micrograms kg-1 s.c.). Urinary retention contributed to but did not account for this reduction. Plasma levels of immunoreactive arginine vasopressin (ir-AVP) were reduced in both normal and dehydrated Long Evans rats after doses greater than 1 microgram kg-1 M320 s.c. In vitro, M320 caused persistent inhibition of twitches of the electrically stimulated rabbit vas deferens (IC50 1.7 nM). 8 These data suggest that M320 has potent opioid agonist activity at K-receptors and at higher concentrations stimulates mu- receptors. In the rat, its activity on K-receptors is associated with diuresis and suppression of plasma vasopressin levels. The antidiuresis seen after high doses may be due to its activity on mu-receptors, possibly at a central site.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-1223660,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-14334338,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-4958020,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-574456,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6094203,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6094211,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6121047,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6137557,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6253759,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6258694,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6273188,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6294284,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6356937,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6714302,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-6722535,
http://linkedlifedata.com/resource/pubmed/commentcorrection/3028550-7083068
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0007-1188
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
89
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
759-67
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pubmed:dateRevised |
2010-5-12
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pubmed:meshHeading |
pubmed-meshheading:3028550-Animals,
pubmed-meshheading:3028550-Female,
pubmed-meshheading:3028550-Male,
pubmed-meshheading:3028550-Morphinans,
pubmed-meshheading:3028550-Rats,
pubmed-meshheading:3028550-Rats, Brattleboro,
pubmed-meshheading:3028550-Receptors, Opioid,
pubmed-meshheading:3028550-Receptors, Opioid, kappa,
pubmed-meshheading:3028550-Receptors, Opioid, mu,
pubmed-meshheading:3028550-Urination
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pubmed:year |
1986
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pubmed:articleTitle |
The effects of N-(cyclopropylmethyl)-19-isopentylnororvinol (M320), a potent agonist at kappa- and mu-opiate receptors, on urine excretion of rats.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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