Related Experiment Video
Updated: Sep 27, 2026

Reproductive Techniques for Ovarian Monitoring and Control in Amphibians
Published on: May 12, 2019
CP8668, a novel orally active nonsteroidal progesterone receptor modulator with tetrahydrobenzindolone skeleton
Yuji Tabata1, Yumiko Iizuka, Rie Shinei
1Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan. yuji_tabata@meiji.co.jp
Abstract:
We investigated progestational activity of a new nonsteroidal compound, CP8668, ((4aR,5R,6R,7R)-7-methoxy-6-(N-propylaminocarbonyl)oxy-4a,5,6,7-tetrahydro-1,3,4a,5-tetramethylbenz[f]indol-2(4H)-one). CP8668 showed selective affinity for human progesterone receptor equal in strength to other steroidal progestins. CP8668 showed no significant affinity for human glucocorticoid receptor or human estrogen receptor and very weak affinity for rat androgen receptor. In endogenous and exogenous progesterone-dependent enzyme expression assays using human mammary carcinoma T47D, CP8668 showed mixed agonist-antagonist activity. However, in a rabbit endometrial transformation test, CP8668 showed good progestational activity following s.c. and p.o. administration. These results suggest that CP8668 is a selective and orally active progesterone receptor modulator, which shows mixed agonist-antagonist activity in in vitro transcription tests and agonist activity in endometrial transformation assays in rabbits, and that it is potentially a promising lead compound for a new type of orally active progesterone receptor modulator.
More Related Videos
Related Concept Videos
Prodrugs
Prodrugs help overcome...
Gonadal and Placental Hormones
In males, testosterone is the primary gonadal androgen. It plays a central role in the maturation of male reproductive organs — the penis and testes. Additionally, testosterone is instrumental in the development of secondary sexual characteristics — a deep voice as well as facial and pubic hair growth — and...
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Adrenergic Antagonists: Chemistry and Classification of β-Receptor Blockers
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Directing and Steric Effects in Disubstituted Benzene Derivatives

