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  • Title: Inhibition of LH-release by synthetic analogues of LH-RH in rat pituitary cell culture.
    Author: Nikolics K, Bieglmayer C, Spona J, Sepródi J, Teplán I.
    Journal: Peptides; 1981; 2(1):65-73. PubMed ID: 7017623.
    Abstract:
    Conditions for testing the inhibitory activity of synthetic analogues of LH-RH in monolayer cultures of rat pituitary cells were optimized. Nine synthetic derivatives of LH-RH were tested to evaluate their inhibitory dose50(ID50) values. The peptide antagonists tested included linear, branched-chain, dimeric and tetrameric derivatives of LH-RH, Ac-D-Phe1, D-Cpa2, D-Trp3,6-LH-RH (analogue V) was found to be the most effective competitive inhibitor of the series with an ID50 value of 6 x 10(-9)M in the presence of 10(-9) M LH-RH. The kinetics of the LH-RH-blocking action of two inhibitors were also studied. Both the linear (analogue I) and the dimeric (analogue VI) peptide showed immediate inhibition of HL-release. Prolonged inhibitory activity of the same two peptides was observed when cells were incubated with LH-Rh subsequent to preincubation with the inhibitors.
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