The synthesis of 2-(trcms-3-hydroxy-l-octenyl)-3-indoleheptanoic acid (1) is described. The title compound appeared to show a weak prostaglandin-like activity in two different systems. It contracted rat stomach fundus strips and guinea-pig ileum preparations only at concentrations about 103- and 102-fold higher, respectively, than PGE1 Moreover, it stimulated adenylate cyclase from rat liver plasma membrane, but the relative potency was 4-5 x 102-fold lower than the natural compound. The title compound showed also a certain degree of PGE1 antagonism. © 1978, American Chemical Society. All rights reserved.
The synthesis of 2-(trans-3-hydroxy-l-octenyl)-3-indoleheptanoic acid (1) is described. The title compound appeared to show a weak prostaglandin-like activity in two different systems. It contracted rat stomach fundus strips and guinea-pig ileum preparations only at concentrations about lo3- and 102-fold higher, respectively, than PGE]. Moreover, it stimulated adenylate cyclase from rat liver plasma membrane, but the relative potency was 4-5 X 102-fold lower than the natural compound. The title compound showed also a certain degree of PGE, antagonism.
Synthesis and Prostaglandin-like Activity of 2-(trans-3-Hydroxy-1-octenyl)-3-indolheptanoic Acid
BARCO, Achille;BENETTI, Simonetta;POLLINI, Gian Piero;BARALDI, Pier Giovanni;GUARNERI, Mario;SIMONI, Daniele;VICENTINI, Chiara Beatrice;BORASIO, Pier Giorgio;CAPUZZO, Antonio
1978
Abstract
The synthesis of 2-(trans-3-hydroxy-l-octenyl)-3-indoleheptanoic acid (1) is described. The title compound appeared to show a weak prostaglandin-like activity in two different systems. It contracted rat stomach fundus strips and guinea-pig ileum preparations only at concentrations about lo3- and 102-fold higher, respectively, than PGE]. Moreover, it stimulated adenylate cyclase from rat liver plasma membrane, but the relative potency was 4-5 X 102-fold lower than the natural compound. The title compound showed also a certain degree of PGE, antagonism.File | Dimensione | Formato | |
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