Carbaprostacyclin is a stable analog of PGI2. When infused in rabbits or dogs, it inhibits ex vivo platelet aggregation, but the effect persists only 10 minutes after termination of the infusion. This implies rapid metabolic inactivation of carbaprostacyclin.1 Carbaprostacyclin inhibits platelet aggregation with 10% of the molar potency exhibited by PGI2.1,2 The ED50 of carbaprostacyclin for the in vitro inhibition of ADP-induced platelet aggregation in human PRP is 47 nM.3 It was also shown to effect terminal differentiation of preadipose into adipose cells and enhance the expression of angiotensinogen and adipose fatty acid binding protein with an EC50 of about 0.5 µM.4
1
Whittle, B.J.R., Moncada, S., Whiting, F., et al. Carbacyclin - a potent stable prostacyclin analogue for the inhibition of platelet aggregation. Prostaglandins19605-627(1980).
2
Aiken, J.W., and Shebuski, R.J. Comparison in anesthetized dogs of the anti-aggregatory and hemodynamic effects of prostacyclin and a chemically stable prostacyclin analog, 6a-carba-PGI2 (carbacyclin). Prostaglandins19629-643(1980).
3
Adaikan, P.G., Karim, S.M.M., and Lau, L.C. Platelet and other effects of carbaprostacyclin - a stable prostacyclin analogue. Prostaglandins Med5307-320(1980).
4
Aubert, J., Ailhaud, G., and Negrel, R. Evidence for a novel regulatory pathway activated by (carba)prostacyclin in preadipose and adipose cells. FEBS Lett397117-121(1996).
Whittle, B.J.R., Moncada, S., Whiting, F., et al. Carbacyclin - a potent stable prostacyclin analogue for the inhibition of platelet aggregation. Prostaglandins19605-627(1980).
Adaikan, P.G., Karim, S.M.M., and Lau, L.C. Platelet and other effects of carbaprostacyclin - a stable prostacyclin analogue. Prostaglandins Med5307-320(1980).
Aiken, J.W., and Shebuski, R.J. Comparison in anesthetized dogs of the anti-aggregatory and hemodynamic effects of prostacyclin and a chemically stable prostacyclin analog, 6a-carba-PGI2 (carbacyclin). Prostaglandins19629-643(1980).
Aubert, J., Ailhaud, G., and Negrel, R. Evidence for a novel regulatory pathway activated by (carba)prostacyclin in preadipose and adipose cells. FEBS Lett397117-121(1996).