Description
6β-
PGI
1 is a stable PGI
2 analog resistant to hydrolysis in aqueous solutions. 6β-
PGI
1 has a much longer half-
life than PGI
2, but a greatly reduced molar potency for receptor mediated function. 6β-
PGI
1 has a K
act for adenylate cyclase in NCB-
20 cells of 4.2 μM compared with 18 nM for PGI
2. The potency for vasodilation and inhibition of platelet aggregation is about 1% of PGI
2.
1,2
References
1. Whittle, B.J.R., Moncada, S., Whiting, F., et al.
Carbacyclin — a potent stable prostacyclin analogue for the inhibition of platelet aggregation Prostaglandins 19(4),605-627(1980).
2. Blair, I.A., Hensby, C.N., and MacDermot, J.
Prostacyclin-dependent activation of adenylate cyclase in a neuronal somatic cell hybrid: Prostanoid structure-activity relationships Br. J. Pharmac. 69(3),519-525(1980).
