Fast excitatory neurotransmission in the mammalian central nervous system is largely carried out by AMPA-sensitive ionotropic glutamate receptors. Localized within the postsynaptic density of glutamatergic spines, AMPA receptors are composed of heterotetrameric receptor assemblies associated with auxiliary subunits, the most common of which are transmembrane AMPA-receptor regulatory proteins (T...

Dopamine D3 receptor pharmacology differs from that of the dopamine D2 receptor despite a high degree of receptor sequence similarity. The greatest divergence of the primary sequences of D3 and D2 receptors occurs in the predicted third intracellular loops of the receptors, a region implicated in G protein binding and function. To determine whether this domain specifies the distinct ligand bind...

The class C G protein-coupled sweet taste receptor (STR) is responsible for the perception of sweet-tasting molecules. Considered an obligate heterodimer, it consists 1 2 and 3 subunits. Interest in STR has steadily grown, especially since its discovery extraoral tissues hints at a metabolic role receptor. It now known that many pharmacologically exploitable binding sites exist across extracell...

Pharmacological analysis alone has failed to clarify the role of the three alpha(1)-adrenoceptor subtypes in modulating vascular tone, due to a lack of sufficiently selective antagonists, particularly for the alpha (1B)-adrenoceptor, and the complexity when three receptor subtypes are potentially activated by the same agonist. We adopted a combined genetics/ pharmacology strategy based on the a...

The androgen receptor (AR) is a major therapeutic target in prostate cancer pharmacology. Progression of prostate cancer has been linked to elevated expression of AR in malignant tissue, suggesting that AR plays a central role in prostate cancer cell biology. Potent therapeutic agents can be precisely crafted to specifically target AR, potentially averting systemic toxicities associated with no...

This study aims to explore the material basis and mechanism of Baoyuan decoction in treatment chronic heart failure by network pharmacology molecular docking technology. There are 144 effective active ingredients 253 targets decoction. The key mainly include flavonoids such as quercetin, naringenin glazin. 240 intersecting between Baoyuantang failure, its core jun proto-oncogene, signal transdu...

Yiqi Yangyin complex (YYC), the homology of medicine and food, is comprised Polygonati Rhizoma, Lycii Fructus, Codonopsis Pilosula, Rehmanniae Radix. Herein, YYC polysaccharide treatment effectively attenuated progression MGH in a mice model-induced with estrogen progestogen. significantly relived hormonal disorders by reducing levels receptor α (ERα) progesterone (PR), substantially elevated p...

Ezrin-anchored PKA Coordinates Phosphorylation-dependent Disassembly of a NHERF1 Ternary Complex to Regulate Hormone-sensitive Phosphate Transport Bin Wang, Chris K. Means, Yanmei Yang, Tatyana Mamonova, Alessandro Bisello, Daniel L. Altschuler, John D. Scott, and Peter A. Friedman From the Laboratory for G Protein-Coupled Receptor Biology, Department of Pharmacology & Chemical Biology, Univers...

Headache is a common problem which besets most of us at some time or the other. The pharmacology of headache is complex in an overall sense but can be understood in terms of the anatomy and physiology of the pain-producing structures. Migraine can be used as a template to understand the activation of nociceptive systems in the head and thus their neurotransmitter mediation and modulation. In re...