Advances in basic biological research have proceeded rapidly in recent years. The fields of molecular genetics and immunology have experienced dramatic breakthroughs, capturing the imagination of both the scientific community and the general public. With less public notice, receptor biology has brought a cascade of new discoveries and insights. The entire science of pharmacology has been virtually rewritten in terms of receptor phenomenology. In particular, the discovery of specific receptors for steroid and protein hormones has been of seminal importance. With this new information, we have advanced our understanding of the mechanism and specifity of hormone action. We can now explain how hormones interact selectively with specific target cells and how hormones alter biochemical events within the target cells. These facts have already impacted on applied problems of clinical medicine, particularly in diagnosis and treatment of cancer and some metabolic diseases. Now, a new and important application of basic receptor biology and chemistry looms ahead.
Within a few short years since the discovery of the progesterone receptor, chemists have synthesized molecules with a greater affinity for the receptor than progesterone itself and which, while occupying the receptor, fail to trigger the events which transform a target cell from the unstimulated to the stimulated state. This is the basis of the competitive inhibitory action of the anti-progestational agent, synthesized by the chemists at Roussel Uc1af, Paris, and designated RU 486.
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Springer Science+Business Media
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77 black & white illustrations, biography
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978-0-306-42103-7 (9780306421037)
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Schweitzer Klassifikation
Ru 486: An Antiprogestin Steroid With Contragestive Activity In Women.- Analogues Of Ru 486 For The Mapping Of The Progestin Receptor: Synthetic And Structural Aspects.- Pharmacological Profile Of Ru 486 In Animals.- The Use Of The Antiprogesterone Compound Ru 486 To Control Timing Of Parturition In Rats.- In Vivo Assessment Of Antiprogesterone And Antiglucocorticoid Activities Of Ru 486 In Rats: Efficacy In Terminating Early Pregnancy In The Rat.- Histopharmacology Of Ru 486.- Biochemical Profile Of Ru 486.- Radioimmunoassay Of Ru 486.- Pharmacokinetics Of Ru 486.- Toxicological Study On Ru 486.- Non-human Primate Studies With Ru 486.- Studies On The Antireproductive Mechanism Of Action Of Ru 486.- Effects Of The Antiprogesterone Agent Ru 486 On The Natural Cycle And Gestation In Intact Cynomolgus Monkeys.- Behavioral And Endocrine Consequences Of Long-term Antiprogesterone (ru 486) Administration To Cynomolgus Monkeys: Preliminary Results.- Effects Of The Antiprogesterone Ru 486 In Early Pregnancy And During The Menstrual Cycle.- Interruption Of Early Pregnancy By The Antiprogestational Compound Ru 486.- Clinical Study Of Ru 486 In Early Pregnancy.- Termination Of Very Early Pregnancy With Different Doses Of Ru 486: A Phase I Controlled Clinical Trial.- Clinical Effects Of Ru 486 Administered For Seven Days In Early Pregnancy.- The Use Of Ru 486 As An Abortifacient In Early Pregnancy.- Pharmacokinetic And Clinical Studies Of Ru 486 For Fertility Regulation.- Ru 486 Stimulation Of PGF2 Production In Isolated Endometrial Cells In Short Term Culture.- The Demonstration Of The Antiprogestin Effects Of Ru 486 When Administered To The Human During Hcg-induced Pseudopregnancy.- Ru 486 In Women With Normal Or Anovulatory Cycles.- Use Of Single Doses Of The Antiprogesterone Steroid Ru 486 For Induction Of Menstruation In Normal Women.- Endocrinologic Effects Of The Antiprogesterone Ru 486 In The Luteal Phase Of Normal Women.- Endometrial And Pituitary Responses To The Steroidal Antiprogestin Ru 486 In Postmenopausal Women.- Ru 486: A Full Progestin Antagonist In Human Breast Cancer Cell Lines.- Effect Of Ru 486 On The Pituitary-adrenal Axis In The Dog.- Ru 486: Studies Of Its Antiglucocorticosteroid Activity In Man.- Use Of The Glucocorticoid Agonist Ru 486 In The Treatment Of Cushing's Syndrome.- Clinical Update.
