Use of Female Sex Hormone Receptor Antagonist

Similarly, there are a number of pharmacological agents that have been used to block estrogen receptors (Martel et al., 1998; Tremblay et al., 1998; Angele et al., 2000; Katzenellenbogen and Katzenellenbogen, 2000; Stauffer et al., 2000; Meyers et al., 2001; Yokoyama et al., 2002; Chaudry et al., 2003). Among them, ICI 182,780 and EM-800 were used in many studies dealing with the role of estrogen in trauma (Angele et al., 2000; Yokoyama et al., 2002; Chaudry et al., 2003). EM-800 is an estrogen receptor antagonist that blocks the transcriptional functions of estrogen receptor a and ß (Luo et al., 1997; Martel et al., 1998; Tremblay et al., 1998). ICI 182,780 on the other hand inhibits estrogen binding to the receptor complex. ICI is 10 times more potent than EM-800 and can be administered orally or subcutaneously. In addition, there are compounds that work as an agonist and are recognized for their specificity toward ER-a and ER-ß. Propyl pyrazole triol (PPT) is a potent ER-a agonist that does not activate ER-ß (Martel et al.,1998;Tremblay et al., 1998;Angele et al., 2000; Katzenellenbogen and Katzenellenbogen, 2000; Stauffer et al., 2000; Meyers et al., 2001; Yokoyama et al., 2002; Chaudry et al., 2003). In contrast, the compound diarylpropionitrile (DPN) is a potency-selective agonist for ER-ß with a more than 70-fold higher binding affinity for ER-ß than ER-a. Tamoxifen is another agent that has been used in breast-cancer patients with estrogen receptor-positive tumors. These agents can be used to block specific receptors and thus will allow for evaluating their role both in cancer as well as in experimental models of trauma.

Was this article helpful?

0 0

Post a comment