|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
2
|
|
pubmed:dateCreated |
1994-2-4
|
|
pubmed:abstractText |
The anti-platelet actions of 1-[(4,5-bis(4-methoxyphenyl)-2- thiazoyl)carbonyl]-4-methylpiperazine hydrochloride (FR122047) were investigated in vitro and in vivo. FR122047 was 100 times more potent than aspirin against arachidonic acid- and collagen-induced human and guinea-pig platelet aggregation in vitro. Its actions on platelets were a result of cyclooxygenase inhibition. The single oral dose of FR122047 inhibited arachidonic acid- and collagen-induced aggregation with an ED50 of 280 micrograms/kg and 530 micrograms/kg, respectively, in guinea-pigs. The anti-platelet action was augmented 5-10 times by repeated administration for 4 days. At 1 mg/kg the inhibitory actions were prolonged for 48 h and the drug concentration was < 0.1 ng/ml in platelet-poor plasma at 24 h and 0.282 ng/ml in platelet-rich plasma at 48 h. The safety margin in rats (minimum ulcerogenic dose/ED50 for anti-platelet aggregation) of FR122047 was more than 70, while that of aspirin was only 1.2. These results indicate that FR122047 is concentrated in platelets and may be a useful anti-platelet agent.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
|
|
pubmed:issn |
0014-2999
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
19
|
|
pubmed:volume |
243
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
179-84
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:8276067-Animals,
pubmed-meshheading:8276067-Aspirin,
pubmed-meshheading:8276067-Blood Platelets,
pubmed-meshheading:8276067-Cyclooxygenase Inhibitors,
pubmed-meshheading:8276067-Guinea Pigs,
pubmed-meshheading:8276067-Humans,
pubmed-meshheading:8276067-Irritants,
pubmed-meshheading:8276067-Male,
pubmed-meshheading:8276067-Malondialdehyde,
pubmed-meshheading:8276067-Microsomes,
pubmed-meshheading:8276067-Piperazines,
pubmed-meshheading:8276067-Platelet Aggregation,
pubmed-meshheading:8276067-Platelet Aggregation Inhibitors,
pubmed-meshheading:8276067-Prostaglandins,
pubmed-meshheading:8276067-Rabbits,
pubmed-meshheading:8276067-Rats,
pubmed-meshheading:8276067-Rats, Sprague-Dawley,
pubmed-meshheading:8276067-Seminal Vesicles,
pubmed-meshheading:8276067-Sheep,
pubmed-meshheading:8276067-Stomach Ulcer,
pubmed-meshheading:8276067-Thiazoles
|
|
pubmed:year |
1993
|
|
pubmed:articleTitle |
The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor.
|
|
pubmed:affiliation |
New Drug Research Laboratories, Fujisawa Pharmaceutical Company, Ltd., Osaka, Japan.
|
|
pubmed:publicationType |
Journal Article,
In Vitro
|
