Human

The protein encoded by this gene is a member of the G protein-coupled receptor family 1. It is also an integral plasma membrane protein that binds melanin-concentrating hormone. The encoded protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Melanin-concentrating hormone (MCH) is an important neuropeptide hormone involved in multiple physiological processes. Peptide derivatives of MCH have been developed as tools to aid researches that involve potent radioligands, receptor selective agonists, and potent antagonists. These tools have been used to further understand the role of MCH's physiology primarily in rodents.

Human

Tachykinins are peptides sharing a common C-terminal amino acid sequence: Phe-X-Gly-Leu-Met-NH2. This neuropeptide family is composed of substance P, neurokinin A, and neurokinin B, which are widely distributed in mammalian central and peripheral nervous systems. These three molecules serve as both neurotransmitters and neuromodulators. Their actions are mediated by binding with three distinct receptors, namely NK1, NK2, and NK3. In particular, NK2 is expressed in gastrointestinal tract. Activation of NK2 is chiefly responsible for the regulation of intestinal motor functions (both excitatory and inhibitory), secretions, inflammation, and visceral sensitivity. Antagonists of NK2 may be useful in the treatment of irritable bowel syndrome.

Human

The Vasoactive intestinal polypeptide receptor 2 (VPAC2) is a Gs-coupled receptor expressed in the stroma of uterus and prostate; smooth muscles in gastrointestinal tract, seminal vesicles and skin; blood vessels; thymus. VPAC2 is an essential regulator of the circadian pacemaker of the hypothalamic suprachiasmatic nuclei.

Human

The bombesin receptor family is a member of the G protein-coupled receptor superfamily and consists of three subtypes of receptors: BB1 (neuromedin B receptor), BB2 (gastrin-releasing peptide receptor), and BB3. These receptors are widely distributed in mammals especially in the CNS and gastrointestinal tract and have numerous effects both physiologically and in pathologic processes including having an autocrine growth action on normal tissues and tumors; potent CNS effects (satiety, circadian rhythm, various behaviors); and potent effects in the immune, gastrointestinal, respiratory and urogenital systems.The human BB1 receptor has a greater than 100-fold higher affinity for neuromedin B than gastrin-releasing peptide. Interaction of ligand and BB1 activates the Gαq/11 pathway and increase the intracellular calcium concentration. GenScript's BB1-expressing stable cell line was made in CHO-K1 host cell and optimized for calcium assays.

Human

The apelin receptor AGTRL1 is Gi/Go-coupled GPCRs expressed in the heart, coronary artery, aorta, internal mammary artery, pulmonary artery and saphenous vein, it also expressed in lung, kidney and adrenal gland. In AGTRL1 receptor knockout mice baseline blood pressure is not changed compared to wild-type animals. Vasoconstrictor responses to angiotensin II however are significantly more pronounced in the knockout animals.

Human

The Vasoactive intestinal Peptide/Pituitary Adenylate Cyclase Activating Polypeptide (VPAC) receptor is G protein-coupled and has been divided into at least three types: PAC1, VPAC1, and VPAC2. High expression of PAC1 is observed in CNS and the adrenal medulla. Several splice variants of PAC1 result in proteins that differ at the N-terminus and third intracellular loop; these variants differ in their affinities for PACAP and abilities to activate Gq and Gs. This manual describes establishment of a cell line and a protocol of pharmacologically validated human PAC1 GPCR receptor (Genebank Accession Number: NM_003382).

Human

The melanocortin receptor 5, MC5 receptor, is Gs-coupled GPCRs expressed in the adrenal gland, fat cells, kidney, leukocytes, lung, lymph node, mammary gland, ovary, pituitary, testis and uterus. Mice with targeted deletion of the MC5 receptor have a defect in water and thermoregulation secondary to their decreased production of sebaceous lipids.

Human

Opioid receptor family includes three classic receptors, μ, δ, and κ, also known as OP1, OP2 and OP3, respectively. The receptors are Gi/o-coupled GPCRs which will reduce intracellular cAMP levels after activation. δ-opioid receptor modulates many kinase cascades including ERKs, Akts, JNKs, STAT3, P38 involving Src, Ras, Rac, Raf-1, Cdc42, RTKs. In addition, δ-opioid receptor has also been proposed to interact with μ receptors. The observed pharmacological cross-talk may partially arise from agonist cross-reactivity.

Human

The P2Y receptor 12 (P2Y12) is a Gi-coupled GPCR expressed in platelets, brain tissues, vascular smooth muscle cells. P2Y12 can sustain platelet aggregation and promote thrombus growth and stabilization. It also plays a function in dense and alpha granule secretion, p-selectin expression and microparticle formation.

Human

Muscarinic acetylcholine receptors belong to a superfamily of seven-TM-domain receptors that interact with G-proteins to initiate intracellular responses. Five muscarinic receptor subtypes have been identified and named from M1 to M5. The M4 muscarinic receptor couples to Gi/o to inhibit cAMP production. GenScript co-transfected human M4 with Gα15 in the CHO-K1 which supports high levels of recombinant M4 expression on the cell surface and contains high levels of Gα15 to couple the receptor to the calcium signaling pathway.