Cell Line

The GPR68 is a proton-sensing receptor involved in pH homeostasis. A study revealed that in osteosarcoma cells and primary human osteoblast precursors which expression of GPR68 exhibit strong PH-dependent inositol phosphate formation.

CHO-K1/5-HT4/Gα15 Stable Cell Line,2vials

Proteinase-activated receptors (PAR) are a subfamily of G-protein coupled, seven-transmembrane domain receptors, which are cleaved within the aminoterminal exodomain by certain serine proteinases at a specific peptide bond. Trypsin and mast cell tryptase, and more recently, the activated coagulation factors VIIa and Xa, have been identified as serine proteinases able to activate mammalian PAR-2. As already indicated, PAR-2 is believed to be involved in inflammation. This role for PAR-2 implies that elastase and cathepsin G would paradoxically display an anti-inflammatory property by disarming PAR-2.

Following the cloning of the classical opioid receptors (mu, delta and kappa), the opiate receptor like-1 (ORL1) was identified as a G-protein coupled receptor (GPCR) with 65% structure homology to the other members of the opioid family. OPRL1 is a receptor for the 17 aa neuropeptide nociceptin/orphanin FQ and may be involved in the regulation of numerous brain activities, particularly instinctive and emotional behaviors. Recently, new study results are consistent with the reported high density of ORL1 receptor mRNA in dorsal raphe nucleus and with inhibitory actions of nociceptin in cells expressing ORL1.

GLP1R binds specifically the glucagon-like peptide-1 (GLP1) and has much lower affinity for related peptides such as the gastric inhibitory polypeptide and glucagon. GLP1R is known to be expressed in pancreatic beta cells. Activated GLP1R stimulates the adenylyl cyclase pathway which results in increased insulin synthesis and release of insulin. Consequently, GLP1R has been suggested as a potential target for the treatment of diabetes. GLP1R is also expressed in the brain where it is involved in the control of appetite. Furthermore, mice which over express GLP1R display improved memory and learning.

DP1 is a G_s-coupled GPCR expressed in the colon, eye, platelets, eosinophils, that bind to PGD2 and PGE2. DP1 can inhibit platelet aggregation, and also inhibit leukotriene B4 and superoxide anion (O2-) release from human neutrophils. It can relax smooth muscle and regulate eosinophil apoptosis. DP receptor knockout OVA-challenged mice exhibit reduced Th2 cytokine levels and lymphocyte accumulation in the lung. In addition, they failed to produce asthmatic responses.

Adrenoceptors are 7-transmembrane receptors which mediate the central and peripheral actions of the neurotransmitter, noradrenaline (norepinephrine), and the hormone and neurotransmitter, adrenaline (epinephrine). Based on both pharmacological and molecular evidence, they are divided into three major types - α1, α2, and β. The α2 adrenoceptors include 3 subtypes - α2A, α2B, and α2C - each of which couples to G_i/o protein primarily. <br>The α2B adrenoceptors (ADRA2B) is expressed in the kidney, liver, brain, lung, heart, and skeletal muscle. The development of α2B and α2C knock-out mice has shown that these two subtypes are not involved in the central hypotensive response to α2 agonists.

Angiotensin receptor 1 (AT1 receptor) is a member of angiotensin receptors which are responsible for the signal transduction of the main effecter hormone. Effects mediated by the AT1 receptor include vasoconstriction, aldosterone synthesis and secretion, increased vasopressin secretion, cardiac hypertrophy, augmentation of peripheral noradrenergic activity, vascular smooth muscle cells proliferation, decreased renal blood flow, renal renin inhibition, renal tubular sodium reuptake, modulation of central sympathetic nervous system activity, cardiac contractility, central osmocontrol and extracellular matrix formation.

The NPY family consists of three 36-amino acid peptides, neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP), which bind to the NPY receptors. At present five distinct NPY receptors, Y1, Y2, Y4, Y5, and y6, have been established by receptor cloning studies and all of them are G_i-coupled GPCRs. Activation of NPY receptors mediate a variety physiological effects including stimulation of food intake, inhibition of anxiety in the CNS, presynaptic inhibition of neurotransmitter release in the CNS and periphery, modulation of circadian rhythm, release of pituitary hormones, modulation of hippocampal activity, pain transmission, vasoconstriction, inhibition of insulin release and modulation of renal function. With regard to endogenous agonists, the receptors Y2 preferentially bind NPY and PYY.