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Target intelligence / Profile preview
Neurokinin 3 Receptor (NK3R)
- Target
- NK3R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Tachykinin receptor
01
Overview
The neurokinin 3 receptor (NK3R) is a class A GPCR that is primarily activated by the endogenous neuropeptide neurokinin B (NKB). It plays a crucial role in thermoregulation, particularly in mediating menopausal hot flashes through its action on hypothalamic KNDy neurons. NK3R is also involved in regulating reproductive hormone secretion via GnRH modulation. Selective NK3R antagonists, such as fezolinetant, are approved for the treatment of menopausal vasomotor symptoms, while other investigational agents are being explored for broader therapeutic applications, including oncology.
- Other names
- NK3 ReceptorNK-3 ReceptorNeurokinin B ReceptorTACR3
02
Mechanism of action
Selective antagonism of the neurokinin 3 receptor, leading to decreased activity of KNDy neurons in the hypothalamus and reduced hot flash frequency.
03
Biological functions
ThermoregulationGonadotropin-releasing hormone (GnRH) regulationSmooth muscle contraction/relaxationVasodilationSecretion processesImmune system modulationPain transmissionNeurogenic inflammationSignal transduction
04
Disease associations
Menopausal vasomotor symptomsReproductive disordersCentral nervous system disordersOncology (potential)
05
Safety considerations
Transient liver enzyme elevations (with some NK3R antagonists)Potential off-target effects due to structural similarity to other GPCRs (minimized with highly selective antagonists)
06
Interacting drugs
Neurokinin B (NKB)
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