Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
|
pubmed:dateCreated |
1992-7-31
|
pubmed:abstractText |
An orally effective, nonpeptide vasopressin V1 receptor antagonist, OPC-21268 was produced for possible human use. We investigated the effects of OPC-21268 on the vascular effects of intra-arterially infused arginine vasopressin in human forearm vessels. The brachial artery was cannulated for drug infusions and direct measurement of arterial pressure. Forearm blood flow was measured by a strain gauge plethysmograph, and forearm vascular resistance was calculated. Arginine vasopressin was infused intra-arterially at doses of 0.02, 0.06, 0.09, 0.2, 0.6, and 1.2 ng/kg/min. The lower doses of arginine vasopressin increased, whereas the higher doses of arginine vasopressin decreased forearm vascular resistance (p less than 0.01). Intra-arterial infusion of phenylephrine at doses of 0.2, 0.4, and 2.4 micrograms/min increased forearm vascular resistance dose-dependently (p less than 0.01). OPC-21268 (50 mg for two, 100 mg for six, and 200 mg for two subjects) given orally did not alter resting arterial pressure, forearm vascular resistance, or heart rate. OPC-21268 decreased vasoconstrictor responses to arginine vasopressin at doses of 0.02 (p less than 0.02) and 0.09 (p less than 0.05) ng/kg/min and augmented vasodilator responses to arginine vasopressin at a dose of 1.2 ng/kg/min (p less than 0.01). However, the vasoconstrictor responses to phenylephrine were not altered by OPC-21268. These results demonstrated that OPC-21268 effectively and specifically antagonized the V1 receptor-mediated vasoconstriction in human forearm resistance vessels. These results suggest that OPC-21268 may be useful therapeutically to antagonize the vasoconstriction caused by arginine vasopressin in some pathological states.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Angiotensin Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Arginine Vasopressin,
http://linkedlifedata.com/resource/pubmed/chemical/OPC 21268,
http://linkedlifedata.com/resource/pubmed/chemical/Phenylephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolones,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Vasopressin
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jul
|
pubmed:issn |
0194-911X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
20
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
54-8
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:1319959-Administration, Oral,
pubmed-meshheading:1319959-Adult,
pubmed-meshheading:1319959-Angiotensin Receptor Antagonists,
pubmed-meshheading:1319959-Arginine Vasopressin,
pubmed-meshheading:1319959-Dose-Response Relationship, Drug,
pubmed-meshheading:1319959-Forearm,
pubmed-meshheading:1319959-Humans,
pubmed-meshheading:1319959-Injections, Intra-Arterial,
pubmed-meshheading:1319959-Male,
pubmed-meshheading:1319959-Phenylephrine,
pubmed-meshheading:1319959-Piperidines,
pubmed-meshheading:1319959-Quinolones,
pubmed-meshheading:1319959-Receptors, Vasopressin,
pubmed-meshheading:1319959-Regional Blood Flow,
pubmed-meshheading:1319959-Vascular Resistance
|
pubmed:year |
1992
|
pubmed:articleTitle |
Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans.
|
pubmed:affiliation |
Research Institute of Angiocardiology, Faculty of Medicine, Kyushu University, Fukuoka, Japan.
|
pubmed:publicationType |
Journal Article
|