5-Hydroxytryptamine GPCR Assays

Background of 5-Hydroxytryptamine Receptors

5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter and local hormone generated from L-tryptophan in serotonergic neurons and enterochromaffin cells along the gastrointestinal tract. It is the endogenous ligands of 5-hydroxytryptamine receptors. The family of 5-HT receptors is a group of G protein-coupled receptors. 5-HT receptors are classified into 6 groups, including 5-HT₁, 5-HT₂, 5-HT₄, 5-HT₅, 5-HT₆, and 5-HT₇ receptors.

Fig.1 Signal transduction of 5-HT receptor subtypes. (Ohno, 2015)

Distributions and Functions of 5-Hydroxytryptamine Receptors

5-HT₁ receptors are distributed throughout the central nervous system. 5-HT₂ receptors are expressed in the brain, heart, and serotonin neurons, which play an important role in psychotropic pharmacology for antipsychotics, increased appetite and metabolic syndrome, and migraine. Agonists of 5-HT₄ receptors are effective drugs for gastroesophageal reflux, constipation, and irritable bowel syndrome. Agonists of 5-HT₆ and 5-HT₇ receptors are non-selective drugs used to treat schizophrenia.

Subtypes and Mechanisms of 5-Hydroxytryptamine Receptors

5-HT receptors are a group of G protein-coupled receptors classified into 6 groups, including 5-HT₁, 5-HT₂, 5-HT₄, 5-HT₅, 5-HT₆, and 5-HT₇ receptors. There are several subtypes in each group. The group of 5-HT₁ receptors contains five subtypes of receptors, coupling to G_i/G_o proteins, which inhibit adenylyl cyclase. The group of 5-HT₂ receptors contains three subtypes of receptors, coupling to G_q/G₁₁ proteins, which stimulate phospholipase C. 5-HT₄, 5-HT₆, and 5-HT₇ receptors couple G_s proteins. 5-HT₅ receptors couple G_i/G_o proteins and G_q/G₁₁ proteins.

Assay List of 5-Hydroxytryptamine Receptors

Creative Biolabs can provide a range of assays of 5-Hydroxytryptamine receptors. You can choose the assay in the list or contact us for more information:

Published Data

References

1. Ohno Y.; et al. New insight into the therapeutic role of the serotonergic system in Parkinson's disease. Prog Neurobiol. 2015, 134: 104-21.
2. Chan, J. D.; et al. Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist. International Journal for Parasitology: Drugs and Drug Resistance. 2016, 6(3): 364-370.