Cell Line

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.

The apelin receptor AGTRL1 is G_i/G_o-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.

The adenosine receptors ADORA2A is Gs-coupled GPCRs expressed in the thymus gland, heart, lung, kedney, brain, platelets, spleen and leukocytes. ADORA2A down-regulates chemokine receptor function and inhibits platelet aggregation. ADORA2A antagonists may be useful as therapy for Parkinson's disease.

Dopamine is the predominant catecholamine neurotransmitter found in mammalian brain, where it controls a variety of functions including locomotor activity, cognition, emotion, positive reinforcement, food intake, and endocrine regulation. It also plays multiple roles in the periphery as a modulator of cardiovascular function, catecholamine release, hormone secretion, vascular tone, renal function, and gastrointestinal motility. The dopamine receptor family consists of five members, which are classified into two groups, D1-like (D1 and D5) and D2-like (D2, D3, and D4).

5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2B which couples to Gq/11 is expressed in embryonic and adult cardiovascular tissues, gut, and brain from the rat, mouse, and human species. 5-HT2B receptors are responsible for many cardiovascular and central nervous system functions, such as blood vessel contraction, platelet shape changes, neuronal sensitization to tactile stimuli, and mediation of the hallucinogenic effects of phenylisopropylamin hallucinogens. It has also been shown to be required for heart develo

5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal, and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2A which couples to Gq/11 is expressed throughout the central nervous system in the neocortex and olfactory tubercle. 5-HT2A receptor agonists may have important clinical value in the treatment of various disorders, such as depression, anxiety, bipolar disorder, and schizophrenia. GenScript's cloned human 5-HT2A–expressing cell line is generated in the CHO-K1 host.

The adrenoceptors ADRA2C is expressed in the brain, kidney, aorta, lung, skeletal muscle, heart and spleen. ADRA2C knockout mice exhibited disrupts presynaptic inhibition of noradrenaline release at low stimulation frequencies.

5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal, and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2C is expressed in the brain and spinal cord, especially the choroid plexus. 5-HT2C receptor agonists may have important clinical value in the treatment of mental and eating disorders, such as depression, panic anxiety, OCD, bulimia, and obesity. GenScript's cloned human 5-HT2C-expressing cell line is generated in the CHO-K1 host.

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.<br>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 G_αq/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.