Potent agonist and antagonist analogues of luliberin containing an azaglycine residue in position 10

Anti-tumour activity of ICI 118630, a new potent luteinizing hormone-releasing hormone agonist

“…The present report investigates the anti-tumour properties of one such compound, [D-Ser(But)6Azgly 1 0]-luteinizing hormone-releasing hormone (ICI 118630), a new and potent luteinizing hormonereleasing hormone (LH-RH) agonist (Dutta et al, 1978a;. Administration of ICI 118630 at high dose levels (0.5 and 5 jug twice daily) in rats reduces plasma oestradiol levels (Maynard & Nicholson, 1979) and decreases the weight of the uterus in both human -chorionic -gonadotrophin -treated (Dutta et al, 1978a) and untreated animals (Maynard & Nicholson, 1979).…”

Effects of high doses of a series of new luteinizing hormone-releasing hormone analogues in intact female rats

“…injection of doses as low as 5 ng/rat. When given at higher doses (0.5 to 5 0 ug/ rat) it inhibited HCG-stimulated uterine growth in rats (Dutta et al, 1978a). These properties are similar to those of another LH-RH analogue, [D-LeU6, des-GlyNH210 Proethylamide9]LH-RH (A43818) (Rippel et al, 1975;Rippel & Johnson, 1976).…”

“…The effect of LH-RH agonists of inhibiting HCG-induced uterine growth when administered at high doses (Rippel & Johnson, 1976;Dutta et al, 1978a) prompted a more detailed investigation into the biological results of such treatment with LH-RH agonists containing the AzglylO modification. From studies of the time course of plasma LH levels after injection of ICI 118630 (Figs.…”

“…Recently a new series of LH-RH analogues containing an azaglycine residue in Position 10 has been synthesized (Dutta et al, 1978a). One of these compounds, [D-Ser(But)6, Azglyl°]LH-RH (ICI 118630) induced ovulation in androgen-sterilized constant-oestrus rats after i.v.…”

The clinical and endocrine effects of 4-hydroxyandrostenedione alone and in combination with goserelin in premenopausal women with advanced breast cancer

“…Leutinising hormone releasing hormone (LHRH) analogues such as goserelin inhibit gondadotrophin release from the pituitary when administered repeatedly (Dutta et al, 1978). In premenopausal women they have the effect of suppressing ovarian oestrogen synthesis, and have been used as an alternative to surgical oophorectomy in the treatment of advanced breast cancer (Klijn et al, 1982;Nicholson et al, 1984;Williams et al, 1986 We report here on the endocrine and therapeutic effects of 40HA on its own, and in combination with goserelin in premenopausal women with advanced breast cancer.…”