Human TACR3

Figure. Concentration-dependent activation of TACR3 by neurokinin A

Reporter cells were transfected with either the expression plasmid for human tachykinin receptor 3 (TACR3) or the mock plasmid and treated with various concentrations of neurokinin A. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 27 nM.

Nomenclature
tachykinin receptor 3
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Endocrinology/Metabolism, Neurology, Ophthalmology, Musculoskeletal, Urology/Reproduction, Human non-orphan GPCRs

Tachykinin receptors

Tachykinin receptors are activated by the endogenous peptides substance P (SP), neurokinin A (NKA; previously known as substance K, neurokinin α, neuromedin L), neurokinin B (NKB; previously known as neurokinin β, neuromedin K), neuropeptide K and neuropeptide γ (N-terminally extended forms of neurokinin A). The neurokinins (A and B) are mammalian members of the tachykinin family, which includes peptides of mammalian and nonmammalian origin containing the consensus sequence: Phe-x-Gly-Leu-Met. Marked species differences in in vitro pharmacology exist for all three receptors, in the context of nonpeptide ligands. Antagonists such as aprepitant and fosaprepitant were approved by FDA and EMA, in combination with other antiemetic agents, for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

Filters Sort results
Reset Apply