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- W2122869360 abstract "In this study membrane oestradiol (E) binding sites in the medial preoptic area‐anterior hypothalamus (MPOA‐AH) of ovariectomized (OVX) rats were characterized using standard radioligand binding techniques employing E conjugated to bovine serum albumin (BSA) at position 6 and radiolabeled with 125 I (E‐6‐[ 125 I‐BSA]). In previous studies binding of a radioactive conjugate of progesterone (P) and BSA (P‐3‐[ 125 I‐BSA]) was examined using the same membrane preparation. E‐6‐[ 125 I‐BSA] binding was linear across a tissue concentration range of 0.005–0.02 mg protein/0.1 ml of membrane suspension. An association T 1/2 of 9.5 min and a dissociation T 1/2 of 52.1 min for E‐6‐[ 125 I‐BSA] were derived from kinetic experiments. Competition binding experiments revealed high (Ki=0.63±(0.50 nM) and low (Ki=161.5(96.5 nM) affinity binding sites for E‐6‐[ 125 I‐BSA], demonstrating different binding parameters than shown in our previous work for P‐3‐[ 125 I‐BSA] binding. Further studies on MPOA‐AH membranes treated with cholera toxin (CTX) and GTP γ S suggested that E‐6‐BSA binding sites are associated with G proteins. E‐6‐[ 125 I‐BSA] binding demonstrated both high‐and low‐affinity sites. GTP γ S added to the assay reduced both E‐6‐[ 125 I‐BSA] and P‐3‐[ 125 I‐BSA] binding suggesting that G proteins are associated with both binding sites. Extensive analysis of both E‐6‐[ 125 I‐BSA] and P‐3‐[ 125 I‐BSA] binding sites demonstrated a reciprocal relationship such that high‐affinity E‐6‐[ 125 I‐BSA] binding sites exhibit low affinity for P‐3‐[ 125 I‐BSA] and low‐affinity E‐6‐[ 125 I‐BSA] binding sites exhibit high affinity for P‐3‐[ 125 I‐BSA]. Preincubating membranes with CTX or GTP γ S reduced high‐affinity E‐6‐[ 125 I‐BSA] binding and enhanced high‐affinity P‐3‐[ 125 I‐BSA] binding. These results suggest that, in the MPOA‐AH, membrane steroid binding sites exist in two interconvertible conformations that preferentially bind either E‐6‐BSA or P‐3‐BSA, depending on their association with a G protein. Additional studies with free steroids revealed that: (1) oestrogens (17 β ‐oestradiol, diethylstilbestrol) as well as synthetic oestrogen antagonists tamoxifen and ICI 182 780 displaced P‐3‐[ 125 I‐BSA] further suggesting a relationship between membrane binding sites for E and P‐3‐[ 125 I‐BSA] binding sites; and (2) treatment of OVX rats with E decreased displacement by P‐3‐BSA and increased displacement by ICI 182,780 and tamoxifen suggesting these antagonists affect membrane P‐3‐[ 125 I‐BSA] binding sites after in‐vivo E treatment. The membrane binding sites for E and P demonstrate interrelationships not demonstrated by their nuclear receptors." @default.
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- W2122869360 date "1999-06-01" @default.
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- W2122869360 title "Radioligand Assays for Oestradiol and Progesterone Conjugated to Protein Reveal Evidence for a Common Membrane Binding Site in the Medial Preoptic Area‐Anterior Hypothalamus and Differential Modulation by Cholera Toxin and GTP γ S" @default.
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- W2122869360 doi "https://doi.org/10.1046/j.1365-2826.1999.00356.x" @default.
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