Cell Line

The orphan receptor ChemR23 (also referred to as CMKLR1 or DEZ) is a G-protein coupled receptor (GPCR) with homology to neuropeptide and chemoattractant receptors. ChemR23 is also a Gαi-linked receptor expressed primarily by monocytes, MΦs, and plasmacytoid dendritic cells. CMKLR1 has been shown to be expressed by DC generated in vitro from monocytes, to mediate their migration to the proteolytically regulated chemoattractant chemerin, and CMKLR1 may be a key mediator of pDC recruitment from the blood into tissue sites enriched in active chemerin.

The µ-opioid receptor (oprm1) is the principal site of action in the brain by which morphine, other opiate drugs of abuse, and endogenous opioid peptides effect analgesia and alter mood. Opioid receptors belong to the rhodopsin family of G protein-coupled receptors (GPCRs). The three types of opioid receptors (μ, δ, and κ) have been shown to associate with each other in a homotypic or heterotypic fashion when expressed in heterologous cells. A member of the seven-transmembrane domain (TM) G protein-coupled receptor (GPCR) superfamily, the µ-opioid receptor modulates ion channels and second messenger effectors in an opioid agonist-dependent fashion that is reversible by the classic opiate antagonist naloxone.

CHO-K1/FPRL1/Gα15 Stable Cell Line,2vials

Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3, and H4. Specifically, the histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. As an integral membrane protein, it stimulates gastric acid secretion and regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation.

The glucagon-like peptides include glucagon, GLP-1, and GLP-2 exert diverse actions on nutrient intake, gastrointestinal motility, islet hormone secretion, cell proliferation and apoptosis, as well as nutrient absorptionand assimilation. Glucagon-like peptide (GLP)-2, a product of the proglucagon gene, is expressed in enteroendocrine cells of the small and large intestine and is trophic to the gastrointestinal mucosa. GLP-2 also inhibits gastric acid secretion and emptying and up-regulates intestinal hexose transport. GLP-2 acts via binding to a single G protein-coupled GLP-2 receptor (GLP-2R).

The thromboxane A2 (TxA2) receptor (TP) is a member of the G protein-coupled receptor (GPCR) superfamily which mediates TxA2-induced platelet aggregation and vasoconstriction. Dysregulation of TxA2 synthesis and function has been implicated in the pathogenesis of a number of disease states including myocardial ischemia, asthma, pregnancy-induced hypertension, and a variety of kidney diseases. TP receptors (Thromboxane A2 receptors) are widely distributed among different organ systems and localized on both cell membranes and in intracellular structures. Two isoforms of human TPs have been cloned from placenta (TPα) and endothelium (TPβ) that differ in their mechanisms and kinetics of desensitization and internalization. The TPs are linked via the Gq/G11 class of G proteins to phospholipase C (PLC), which hydrolyzes phosphoinositides to two potent second messengers: inositol 1,4,5-trisphosphate, which leads to an increase in cytoplasmic free calcium, and diacylglycerol (DAG), which

IP1 receptor is a receptor for prostaglandin I2 or prostacyclin. When binding with a prostacyclin molecule, the receptor changes conformation and activates Gs. Prostaglandin I2, the major product of cyclooxygenase in macrovascular endothelium, mediates a potent vasodilation and inhibition of platelet aggregation by binding to this receptor.

Prostaglandin (PG) E2 exerts its actions by acting on a group of G-protein-coupled receptors (GPCRs). There are four GPCRs responding to PGE2 designated subtypes EP1, EP2, EP3, and EP4 and multiple splicing isoforms of the subtype EP3. The EP subtypes exhibit differences in signal transduction, tissue localization, and expression regulation. Studies have identified that EP2 mediates many processes, such as facilitating ovulation and fertilization, suppressing dendritic cell differentiation, and promoting amyloid-β formation in Alzheimer's disease.

Melatonin is a neurohormone that plays a key role in the synchronisation of circadian and seasonal functions with cyclic environmental variations. In mammals, two melatonin receptors, MT1 and MT2, have been cloned. Activation of MT2 melatonin receptors phase shift circadian rhythms of neuronal firing in the suprachiasmatic nucleus, inhibit dopamine release in retina, induce vasodilation and inhibition of leukocyte rolling in arterial beds, and enhance immune responses.