The (+)-enantiomer is responsible for the antiplatelet and anti-inflammatory activity of (+/-)-indobufen.
The racemic compound indobufen and its (+)- and (-)-enantiomers have been compared for their effects on blood platelet function and rat carrageenan pleurisy. The antiplatelet properties were studied in-vitro in human platelets by measuring the inhibition of platelet aggregation and generation of serum thromboxane (Tx) B2. In-vivo, the antiplatelet and anti-inflammatory properties were studied in rats by measuring the inhibition of serum TxB2, the amount of 6-keto-PGF1 alpha in pleural exudate and pleural exudate volume. In all tests the (+)-enantiomer was slightly more potent than the racemate, while the (-)-enantiomer was far less potent. In the same rats, treatment with the lowest doses of the compounds giving 90% inhibition of serum thromboxane B2 generation was associated with occasional macroscopic lesions of the gastric mucosa.
Cerletti
C
C
Istituto di Ricerche Farmacologiche Mario Negri, Santa Maria Imbaro, Italy.
Manarini
S
S
Colombo
M
M
Tavani
A
A
D000818:Animals; D005753:Gastric Mucosa / Q000187:drug effects; D006801:Humans; D054833:Isoindoles; D010654:Phenylbutyrates / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D010998:Pleurisy / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D013929:Thromboxane B2 / Q000096:biosynthesis* / Q000097:blood
D054833:Isoindoles; D010654:Phenylbutyrates; D010975:Platelet Aggregation Inhibitors; D013929:Thromboxane B2; C020371:indobufen