5-HT6 Human Serotonin GPCR Cell Based Antagonist Arrestin LeadHunter Assay - US

Background Information:

Serotonin (5-hydroxytryptamine, 5-HT) is one of the best known examples of a neurotransmitter that mediates a wide variety of physiological effects, including peripheral and central actions. At least four classes of 5-HT receptors have been distinguished pharmacologically, reflecting the second messenger system to which the receptor is coupled. The first subfamily of 5-HT1 and 5-HT5 interacts negatively with adenylyl cyclase. The second subfamily of 5-HT2 is coupled to the activation of the phospholipase C. The third subfamily, 5-HT3, is a ligand-gated ion channel. The fourth subfamily, including 5-HT4, 5-HT6, and 5-HT7, activates adenylyl cyclase to increase intracellular cAMP.

PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gs & Gq

Protein Name:

5-HT6

Uniprot Number:

P50406

Protein Aliases:

5-HT6|Serotonin receptor 6

Gene Name:

HTR6

Gene ID:

3362

Gene Aliases:

5-HT6|5-HT6R

Accession Number:

AY429105

Organism:

Human

Cell Type:

DLD1