Perrin M H, Haas Y, Rivier J E, Vale W W
Endocrinology. 1983 Apr;112(4):1538-40. doi: 10.1210/endo-112-4-1538.
The plasma membrane receptor for GnRH in bovine anterior pituitaries has been solubilized with the cholic acid derivative detergent 3([3-cholamidopropyl)dimethylammonio]propane sulfonate. The soluble receptor in the supernatant from a 100,000 x g x 90 min centrifugation displays high affinity, saturability and specific binding to the agonist, [DA1a6,N alpha MeLeu7, Pro9-NEt]-GnRH. The dissociation constant, KD, for the soluble receptor is 0.56 +/- 0.07 nM (mean +/- SEM) and the number of sites, Ro, is 85 +/- 17 fmols/mg protein. For the membrane-bound receptor the KD is 0.50 +/- 0.04 nM and Ro is 300 +/- 18 fmols/mg protein. The relative potencies of GnRH and the potent antagonist, [Ac-delta 3Pro1,pFDPhe2, DTrp3,6]-GnRH are similar for both the soluble and membrane-bound receptor.
