caa a22 4500 469078537 CHVBK 20180323132942.0 cr unu---uuuuu 170328e19921101xx s 000 0 eng 10.1007/BF00169007 doi (NATIONALLICENCE)springer-10.1007/BF00169007 Comparison between the interaction of steroids with [35S]TBPS binding to cerebral cortical and to pituitary membranes: correlation with inhibition of prolactin release [Elektronische Daten] [Monique Vincens, Christine Shu, Michel Fortin, Daniel Philibert, Martine Gaillard-Moguilewsky] Summary: It has been shown previously that 5α-pregnan-3α-ol-20-one (5α3αP) can inhibit prolactin release from anterior pituitary gland cells in culture through an interaction with a specific modulatory site on the GABAA receptor complex in anterior pituitary gland membranes. In the present work, this receptor site has been labelled with [35S]t-butylbicyclophosphorothionate ([35S]TBPS) to enable a study of the relative binding affinities (RBA) of different steroids for the GABAA receptor complex to be made. We have found a high correlation (r = + 0.88) between the inhibition of [35S]TBPS binding to anterior pituitary membranes and the inhibition of [35S]TBPS binding to cerebral cortical membranes by nine different steroids. There was also a high correlation between the inhibition of prolactin release from anterior pituitary gland cells in culture by these steroids and the inhibition of [35S]TBPS binding to anterior pituitary membranes (r = + 0.99) or to cortical membranes (r = + 0.81). These observations suggest that the measurement of prolactin release from anterior pituitary gland cells in culture is a good indicator of the functional activity of drugs that bind to the allosteric modulatory TBPS-binding site on the GABAA-receptor complex. Springer-Verlag, 1992 Steroids nationallicence [35S]TBPS binding nationallicence Cortical membranes nationallicence Prolactin nationallicence Pituitary nationallicence GABAA receptor complex nationallicence Vincens Monique Pharmacologie Endocrinienne, Hopital Lariboisiere, 2 rue Ambroise Parè, F-75010, Paris, France aut Shu Christine Pharmacologie Endocrinienne, Hopital Lariboisiere, 2 rue Ambroise Parè, F-75010, Paris, France aut Fortin Michel Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut Philibert Daniel Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut Gaillard-Moguilewsky Martine Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/5(1992-11-01), 523-526 0028-1298 346:5<523 1992 346 210 https://doi.org/10.1007/BF00169007 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00169007 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Vincens Monique Pharmacologie Endocrinienne, Hopital Lariboisiere, 2 rue Ambroise Parè, F-75010, Paris, France aut NATIONALLICENCE 700 1- Shu Christine Pharmacologie Endocrinienne, Hopital Lariboisiere, 2 rue Ambroise Parè, F-75010, Paris, France aut NATIONALLICENCE 700 1- Fortin Michel Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut NATIONALLICENCE 700 1- Philibert Daniel Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut NATIONALLICENCE 700 1- Gaillard-Moguilewsky Martine Centre de Recherches Roussel Uclaf, 111 route de Noisy, F-93230, Romainville, France aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/5(1992-11-01), 523-526 0028-1298 346:5<523 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer