Cyclic adenosine monophosphate (cAMP) plays a pivotal role in gonadotrope responses in the pituitary. Gonadotropin-releasing hormone (GnRH) mediated synthesis and secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) are regulated by both the G/cAMP and G/Ca signaling pathways. Pituitary adenylate cyclase-activating polypeptide (PACAP) also regulates GnRH responsiveness in gonadotropes through the PACAP receptor, which activates the G/cAMP signaling pathway. Therefore, measuring intracellular cAMP levels is important for elucidating the molecular mechanisms of FSH and LH synthesis and secretion in gonadotropes. The GloSensor cAMP assay is useful for detecting cAMP levels in intact, living cells. In this study, we found that increased GloSensor luminescence intensity did not correlate with cAMP accumulation in LβT2 cells under low pH conditions. This result indicates that cell type and condition must be considered when using GloSensor cAMP.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6708853 | PMC |
| http://dx.doi.org/10.1262/jrd.2018-153 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Synthesis, Pharmacological Characterization, and Binding Mode Analysis of 8-Hydroxy-Tetrahydroisoquinolines as 5-HT Receptor Inverse Agonists.
ACS Chem Neurosci
January 2025
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Jagtvej 160, 2100 Copenhagen, Denmark.
The serotonin 7 receptor (5-HTR) regulates various processes in the central nervous system, including mood, learning, and circadian rhythm control, among others. Receptor activation can lead to activation of the Gα protein and a subsequent increase of intracellular cyclic adenosine monophosphate (cAMP). Receptor interaction with inverse agonists results in a decrease of basal cAMP levels and therefore a downstream effect of reduced neuronal excitability and neurotransmission.
View Article and Find Full Text PDFAllosteric Inhibition of the β-Adrenergic Receptor: Design and Synthesis of Cmpd-15 Analogs.
Chem Biodivers
January 2025
School of Pharmacy, Changzhou University, Jiangsu, 213164, China.
We designed and synthesized 27 new amide and dipeptide derivatives containing a substituted phenylalanine as negative allosteric modulators (NAMs) for the beta-2 adrenergic receptor (βAR). These analogs aimed to improve the activity of our lead compound, Cmpd-15, by introducing variations in three key regions: the meta-bromobenzyl methylbenzamide (S1), para-formamidophenylalanine (S2), and 1-cyclohexyl-1-phenylacetyl (S3) groups. The synthesis involved the Pd-catalyzed β-C(sp)-H arylation of N-acetylglycine with 1-iodo-4-substituent-benzenes as the key step.
View Article and Find Full Text PDFDiscovery and structure - activity relationships of 2,4,5-trimethoxyphenyl pyrimidine derivatives as selective D5 receptor partial agonists.
Bioorg Chem
December 2024
Neuroscience and Ageing Biology Division, CSIR-Central Drug Research Institute, Lucknow, U.P., (226031), India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, U.P., (201002), India. Electronic address:
Article Synopsis
- Dopamine receptors are being targeted for treating neurological disorders like Parkinson's and Alzheimer's, with a focus on developing selective D5 receptor agonists.
- Researchers designed and tested forty new pyrimidine derivatives, finding four that act as selective partial agonists for the D5 receptor, with compound 5j showing the most promising activity.
- Compound 5j demonstrated stability and the ability to improve memory in mice without toxicity, suggesting it could be a viable therapeutic option for cognitive impairment.
Ectopically expressed rhodopsin is not sensitive to X-rays.
BMC Neurosci
August 2024
Department of Radiology, University of Alabama at Birmingham, Birmingham, AL, 35294, USA.
Visual perception of X-radiation is a well-documented, but poorly understood phenomenon. Scotopic rod cells and rhodopsin have been implicated in visual responses to X-rays, however, some evidence suggests that X-rays excite the retina via a different mechanism than visible light. While rhodopsin's role in X-ray perception is unclear, the possibility that it could function as an X-ray receptor has led to speculation that it could act as a transgenically expressed X-ray receptor.
View Article and Find Full Text PDFThe Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors.
Biosensors (Basel)
May 2024
Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao 266073, China.
Phosphodiesterases (PDEs), a superfamily of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), are recognized as a therapeutic target for various diseases. However, the current screening methods for PDE inhibitors usually experience problems due to complex operations and/or high costs, which are not conducive to drug development in respect of this target. In this study, a new method for screening PDE inhibitors based on GloSensor technology was successfully established and applied, resulting in the discovery of several novel compounds of different structural types with PDE inhibitory activity.
View Article and Find Full Text PDFWant 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!