Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.

doi:10.1021/JM049676L

Paper

Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.

Published Mar 24, 2005 · N. V. van Straten, T. V. van Berkel, Dennis Demont

Journal of medicinal chemistry

Q1 SJR score

73

Citations

3

Influential Citations

Full textSemantic Scholar

Abstract

Substituted 6-amino-4-phenyl-tetrahydroquinoline derivatives are described that are antagonists for the G(s)-protein-coupled human follicle-stimulating hormone (FSH) receptor. These compounds show high antagonistic efficacy in vitro using a CHO cell line expressing the human FSH receptor. Antagonist 10 also showed a submicromolar IC(50) in a more physiologically relevant rat granulosa cell assay and was found to significantly inhibit follicle growth and ovulation in an ex vivo mouse model. This compound class may open the way toward a novel, nonsteroidal approach for contraception.

Highly Cited

Study Snapshot

Substituted 6-amino-4-phenyl-tetrahydroquinoline derivatives show high antagonistic efficacy for the human follicle-stimulating hormone receptor, potentially offering a novel, nonsteroidal approach for contraception.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Paper

Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.

Sign up to use Study Snapshot

References

Citations

Allosteric modulation of gonadotropin receptors

Allosteric modulation of gonadotropin receptors offers potential for new compounds with unique pharmacological characteristics, potentially benefiting clinical purposes.

Contributions of nonconventional intramolecular hydrogen bond on the bioactivity of a series of substituted 6-amino, 4-phenyl, tetrahydroquinoline derivatives

Nonconventional intramolecular hydrogen bond disruption in the aqueous compartment of the two-layered membrane enhances drug absorption through entropy increasing mechanisms in the human follicle-stimulating hormone (FSH) receptor.

Glycoprotein hormone receptors in GtoPdb v.2023.1

Glycoprotein hormone receptors are activated by a non-covalent heterodimeric glycoprotein, with binding cross-reactivity across endogenous agonists, and deglycosylated hormones showing reduced efficacy.

Overview of follicle stimulating hormone and its receptors in reproduction and in stem cells and cancer stem cells

Follicle stimulating hormone (FSH) and its receptor (FSHR) play a crucial role in reproduction, stem cell differentiation, and cancer, with potential as an anti-cancer therapeutic target.

Mapping of FSHR agonists and antagonists binding sites to identify potential peptidomimetic modulators.

This study identified six potential peptidomimetic modulators for follicle stimulating hormone receptor, which may be useful for developing fertility regulators.