Non-steroidal agonists

Katzenellenbogen studied several steroid receptors [21,144]. Estrogen receptor is one of the most frequently investigated receptors by PAL. Hexestrol is a non-steroidal agonist, which was modified with a diazirine photophore via a sulfide linkage (52, Fig. 18). The photoprobe efficiently (30%) labeled the... 

Several steroidal and non-steroidal glucocorticoid receptor selective dissociated agonists are in development by many pharmaceutical companies and some are now in clinical development. This suggests that the development of dissociated glucocorticoids with a greater margin of safety is possible and may even lead to the development of oral compounds that do not have significant adverse effects. 

The opioid analgesics, such os codeine, tramadol and fentanyl may cause drowsiness. Sumatriptan, which is a serotonin agonist, also tends to cause drowsiness. Modern non-steroidal anti-inflammatory drugs, such as diclofenac, do not cause drowsiness. 

In one case, a complex cyst, thought to be due to ovarian hyperstimulation, resolved after monthly administration of a depot gonadorelin (GnRH) receptor agonist without abandoning tamoxifen (72). One might expect some patients to react to tamoxifen with ovarian hyperstimulation, since another non-steroidal antiestrogen (that is clomiphene) is used for ovarian stimulation and also on occasion produces cysts. 

Table 11.2 Cytosolic non-steroid hormone receptor agonists and antagonists...

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