Androgens decrease LHRH binding sites in rat anterior pituitary cells in culture.

[125I]-[D-Ser(TBU)6]LHRH-EA binds to a single class of high affinity sites in rat anterior pituitary cells in culture at an apparent dissociation constant of 0.25 nM at 0-4C. The order of potency of a representative group of LHRH agonists and antagonists to displace the labeled ligand is similar to their LH-releasing activity. Treatment of pituitary cells for 48 h with 100 nM 5 alpha-dihydrotestosterone leads to a 40% decrease of the number of LHRH receptors with no change of binding affinity. This loss of LHRH receptors is accompanied by a similar decrease of the LH responsiveness to LHRH, thus providing the first evidence for a direct effect of sex steroids on pituitary LHRH receptors as a possible mechanism of feedback action.