Abstract
In vitro autoradiography and radioreceptor assays were used to assess the binding characteristics of the gonadotropin releasing hormone (GnRH) binding sites in rat hippocampus. Competition studies with various GnRH agonists, antagonists, and fragments of GnRH indicate that the structure/binding requirement of the brain GnRH receptors is similar, but not identical, to that described in the pituitary. In the hippocampas, GnRH and the agonist d-Ala(6)-GnRH exhibit an IC(50) for displacement of (125)I-[d-Ser(tBu)(6)-Pro(9)-NHEt]-GnRH (Buserelin, Hoechst) similar to that of the anterior pituitary; in contrast, the antagonist [d-p-Glu(1)-d-Phe(2)-d-Trp(3,6)]-GnRH bound only to the anterior pituitary GnRH receptor. Similarly, [His(5)-Trp(7)-Tyr(8)]-GnRH (chicken II) recognized the pituitary GnRH receptor, but did not bind to hippocampal membranes. The difference in the binding affinities is likely not due to differential metabolism because of the stability of the tracer and of the antagonist and the addition of several enzyme inhibitors to the incubation buffer. The GnRH fragments [4-10]GnRH, [5-10]-GnRH, and [Ac5-10]-GnRH and [Gln(8)]GnRH (chicken I), [Trp(7)-Leu(8)]-GnRH (salmon), and [Tyr(3)-Leu(5)-Glu(6)-Trp(7)-Lys(8)]-GnRH (lampr...Continue Reading
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