The physiological demands of parturition and lactation lead to the increased pulsatile release of oxytocin (OT) into the circulation from the neurohypophysial axons of OT neurones in the supraoptic (SON) and paraventricular (PVN) nuclei. These states of increased OT release are accompanied by a significant plasticity in magnocellular OT neurones and their synaptic connections, and many of these changes require activation of a central OT receptor. The mitogen-activated protein kinase/extracellular signal-regulated kinase pathway (MAPK/ERK) is assumed to be up-regulated in the PVN during lactation, and many of the effects of OT in peripheral and brain tissue are mediated through a MAPK/ERK pathway.
View Article and Find Full Text PDFG protein-coupled receptor (GPCR) family C group 6 member A (GPRC6A) is a multiligand GPCR that is activated by cations, L-amino acids, and osteocalcin. GPRC6A plays an important role in the regulation of testosterone (T) production and energy metabolism in mice. T has rapid, transcription-independent (nongenomic) effects that are mediated by a putative GPCR.
View Article and Find Full Text PDFDopaminergic transmission is fundamental to many neural pathways of clinical interest. We have analyzed the alternatively-spliced isoforms of the D(2) dopamine receptor, D(2) long (D(2l)) and D(2) short (D(2s)), which differ only by a 29-amino acid insertion in the third cytoplasmic loop. Well-known determinants for GPCR signal transduction--the third intracellular loop regions--were co-expressed with the wild-type receptors to test for their ability to antagonize parent receptor function.
View Article and Find Full Text PDFDopamine acts through a family of G protein-coupled receptors to exert its myriad effects. The D3 Dopamine receptor is one member of the D2-like dopamine receptors. We have previously demonstrated in human embryonic kidney (HEK293) cells that D3 receptor stimulation of phospholipase D (PLD) activity is pertussis toxin insensitive [Everett and Senogles.
View Article and Find Full Text PDFAnticancer Drugs
August 2007
The D2 dopamine receptor agonist bromocriptine has been used clinically for reducing tumor mass of pituitary adenomas arising from lactotroph origins. As well, bromocriptine has been shown to have an antiproliferative effect on primary lactotrophs and lactotroph-derived cell lines. The presence of D2 dopamine-like receptors on NCI-H69 cells was previously established by the use of [(125)I]iodosulpride binding and has been confirmed in this study by use of reverse transcription PCR with receptor-specific primers.
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