AI Article Synopsis
- Researchers discovered new 6-amino-4-phenyl-tetrahydroquinoline derivatives that block the human follicle-stimulating hormone (FSH) receptor, which is important for reproductive functions.
- One of the tested compounds demonstrated strong effectiveness at low concentrations in both cell cultures and rat cell assays, indicating its potential for practical applications.
- This class of compounds could lead to innovative nonsteroidal contraceptive methods by inhibiting follicle growth and ovulation in lab models.
Article 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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm049676l | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Current drawbacks and future perspectives in the diagnosis and treatment of male factor infertility, with a focus on FSH treatment: an expert opinion.
J Endocrinol Invest
January 2025
Department of Medicine, University of Padova, Padua, Italy.
Purpose: Infertility is defined as the inability to conceive after 1 year of unprotected intercourse, affecting approximately 15-20% of couples in Western countries. It is a shared problem within the couple; when the main issue lies with one of the partners, it is preferable to refer to "male factor" or "female factor" infertility rather than simply male or female infertility. Despite male factor infertility accounting for half of all couple infertility cases, the clinical approach to the male partner is not uniformly standardized across international guidelines.
View Article and Find Full Text PDFRadiotherapy-induced Hypothalamic-Pituitary axis dysfunction in adult Brain, head and neck and skull base tumor patients - A systematic review and Meta-Analysis.
Clin Transl Radiat Oncol
March 2025
Department of Radiation Oncology (Maastro), GROW Research Institute for Oncology and Reproduction, Maastricht University Medical Centre+, Maastricht, the Netherlands.
Background And Purpose: Radiotherapy for brain, head & neck (HN), and skull base (SB) tumors may deliver significant radiation dose to the hypothalamic-pituitary axis (HPA), leading to impaired functioning of this region and hence, to endocrine disorders. The purpose of this systematic review and -analysis is to investigate literature on HP dysfunction after radiation for non-pituitary brain, HN, or SB tumors at adult age, aiming to give insight in the prevalence of HP dysfunction related to radiation dose.
Materials And Methods: Literature search of the PubMed database was performed for HP dysfunction after radiotherapy in adult patients.
FSH enhances the inflammatory response of macrophages in the knee joint possibly through the NFκB pathway.
FEBS Open Bio
January 2025
Key Laboratory of Endocrine Glucose & Lipids Metabolism and Brain Aging, Ministry of Education, Jinan, China.
Previous studies have suggested that women with higher follicle-stimulating hormone (FSH) levels have a greater incidence of osteoarthritis (OA) compared to women with lower FSH despite normal estrogen levels. Our previous studies also showed that FSH has a negative effect on cartilage in postmenopausal OA. However, no studies have investigated the effect of FSH on the synovium.
View Article and Find Full Text PDFThe role of luteinizing hormone activity in spermatogenesis: from physiology to clinical practice.
Reprod Biol Endocrinol
January 2025
Department of Clinical Medicine, Faculty of Health, Aarhus University, Aarhus, Denmark.
The production of spermatozoa, a process known as spermatogenesis, is primarily controlled by follicle-stimulating hormone (FSH) and luteinizing hormone (LH)-driven testosterone. LH acts on the Leydig cells, stimulating steroid production, predominantly testosterone, and activating critical inter-related spermatogenesis regulatory pathways. Despite evidence that exogenous gonadotropins containing LH activity can effectively restore spermatogenesis in males with hypogonadotropic hypogonadism, the use of these drugs to treat other forms of male infertility is the subject of an ongoing debate.
View Article and Find Full Text PDFObjective: We aimed to compare highly purified human menopausal gonadotropin (hp-hMG) and recombinant follicle stimulating hormone (rFSH) in short antagonist in vitro fertilization (IVF) cycles of patients with poor ovarian reserve (POR). Limited research exists on this comparison in short antagonist cycles for this patient group.
Materials And Methods: This retrospective cohort study involved 165 POR patients aged 18-45 years who underwent IVF between 2018 and 2022.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!